Healthy Volunteers
Conditions
Keywords
Drug therapy
Brief summary
The purpose of this study is to estimate phosphodiesterase 10A (PDE10A) occupancy in brain following a single dose of TAK-063.
Detailed description
The drug being tested in this study is called TAK-063. TAK-063 is was tested to estimate phosphodiesterase10A (PDE10A) occupancy in the brain following a single dose of TAK-063. This study used positron emission tomography (PET) scans to look at changes in the volume of tissue distribution before and after TAK-063 administration to calculate PDE10A occupancy in the brain. The study enrolled 13 participants. Participants were assigned to a treatment group based on an enrollment schedule. The first 4 participants were assigned to the Pilot Cohort and received one dose of TAK-063 30 mg or 1000 mg tablets. The remaining participants were enrolled into the Main Cohort and received one dose of TAK-063 at 3, 10, 30 or 100 mg. Participants in both cohorts also received 3 separate intravenous infusions of \[\^11C\]T-773 \<8 μg; 400MBq ± 10% followed by a PET scan. This single-centre trial was conducted in Sweden. The overall time to participate in this study was 46 days. Participants made 3 visits to the clinic, including one 3-day period of confinement to the clinic. Participants were contacted by phone on Day 16 for follow-up safety assessments.
Interventions
DRUGTAK-063
TAK-063 tablets
DRUG[^11C]T-773
\[\^11C\]T-773 IV solution
Sponsors
Takeda
Study design
Allocation
NON_RANDOMIZED
Intervention model
PARALLEL
Primary purpose
TREATMENT
Masking
NONE
Eligibility
Sex/Gender
MALE
Age
20 Years to 45 Years
Healthy volunteers
Yes
Inclusion criteria
1. Has never previously participated in a positron emission tomography (PET) study (lifetime). 2. In the opinion of the investigator, the participant is capable of understanding and complying with protocol requirements. 3. The participant, informed consent form and any required privacy authorization prior to the initiation of any study procedures. 4. Is a healthy adult male, as determined by a physician based upon medical history and physical examination findings at Screening. 5. Is aged 20 to 45 years, inclusive, at the time of informed consent. 6. Weighs at least 50 kg and less than 100 kg and has a body mass index (BMI) between 18 and 32 kg/m\^2 inclusive at Screening. 7. A male participant who is nonsterilized and sexually active with a female partner of childbearing potential agrees to use adequate contraception from signing of informed consent throughout the duration of the study and for 12 weeks after last dose. 8. Has clinical laboratory evaluations (including clinical chemistry, hematology and complete urinalysis) within the reference range for the testing laboratory, unless the results are deemed not to be clinically significant (CS) by the investigator or sponsor at screening. Participants must have normal hemoglobin levels. 9. Has a normal magnetic resonance imaging (MRI) scan or findings that are deemed not clinically significant at screening (the MRI scan may be performed on a day after other screening activities have been performed but before dosing).
Exclusion criteria
1. Has received any investigational compound within 90 days prior to Screening. 2. Has received TAK-063 in a previous clinical study or as a therapeutic agent. 3. Is an immediate family member, study site employee, or in a dependant relationship with a study site employee who is involved in the conduct of this study (eg, spouse, parent, child, sibling) or may consent under duress. 4. Has uncontrolled, clinically significant neurologic, cardiovascular, pulmonary, hepatic, renal, metabolic, gastrointestinal, urologic, immunologic, endocrine disease, or psychiatric disorder, or other abnormality, which may impact the ability of the participant to participate or potentially confound the study results. 5. Has a known hypersensitivity to any component of the formulation of TAK-063 or \[\^11C\]T-773. 6. Has a positive urine drug result for drugs of abuse or a positive breathalyzer test for alcohol at Screening or Day -1. 7. Has a history of drug abuse (defined as any illicit drug use) or a history of alcohol abuse within 1 year prior to the screening visit or is unwilling to agree to abstain from alcohol until discharge from the Phase 1 unit and drugs throughout the study. 8. Has taken any excluded medication, supplements, or food products listed in the Excluded Medications and Dietary Products table. 9. Intends to donate sperm during the course of the study or within 12 weeks after last dose. 10. Has evidence of current cardiovascular, central nervous system, hepatic, hematopoietic disease, renal dysfunction, metabolic or endocrine dysfunction, serious allergy, asthma hypoxemia, hypertension, seizures, or allergic skin rash. There is any finding in the participant's medical history, physical examination, or safety laboratory tests giving reasonable suspicion of a disease that would contraindicate taking TAK-063 or a similar drug in the same class, or that might interfere with the conduct of the study. This includes, but is not limited to, peptic ulcer disease, seizure disorders, and cardiac arrhythmias. 11. The participant, in the opinion of the investigator, has current or recent (within 6 months) gastrointestinal disease that would be expected to influence the absorption of drugs (ie, a history of malabsorption, esophageal reflux, peptic ulcer disease, erosive esophagitis frequent \[more than once per week\] occurrence of heartburn, or any surgical intervention \[eg, cholecystectomy\]). 12. Has a history of cancer, except basal cell carcinoma which has been in remission for at least 5 years prior to Day 1. 13. Has a positive test result for hepatitis B surface antigen (HBsAg), hepatitis C antibody (HCV), human immunodeficiency virus (HIV) antibody/antigen, at Screening. 14. Has used nicotine-containing products (including but not limited to cigarettes, pipes, cigars, chewing tobacco, nicotine patch or nicotine gum) within 28 days prior to Check-In Day -1. 15. Has poor peripheral arterial/venous access or recent arm or wrist trauma. 16. Has donated or lost 450 mL or more of his blood volume (including plasmapheresis), or had a transfusion of any blood product within 3 months prior to Day 1. 17. Has a Screening or Check-in (Day -1) abnormal (clinically significant) electrocardiogram (ECG). 18. Has a supine blood pressure outside the ranges of 90 to 140 mm Hg for systolic and 50 to 90 mm Hg for diastolic, if out of range may be repeated once for eligibility determination within a maximum of 5 minutes, at the Screening Visit or Check-in (Day -1). 19. Has a resting heart rate outside the range 45 to 90 beats per minute (bpm), if out of range may be repeated once for eligibility determination within a maximum of 5 minutes, at the Screening Visit or Check-in (Day -1). 20. Has an increase in pulse of ≥30 beats per minute or an increase in pulse ≥120 beats per minute within 3 minutes of standing at Screening. 21. Has a decrease of ≥20 mm Hg in systolic blood pressure or a decrease of ≥10 mm Hg in diastolic blood pressure within 3 minutes of standing at Screening. 22. Has a QT interval with Fridericia correction method (QTcF) \>430 ms or PQ interval outside the range 120 to 220 ms, if out of range may be repeated once for eligibility determination within a maximum of 5 minutes, at the Screening Visit or Check-in (Day -1) Visit. 23. Has abnormal Screening laboratory values that suggest a clinically significant underlying disease or participant with the following lab abnormalities: alanine aminotransferase (ALT) and/or aspartate aminotransferase (AST) \>1.5 the upper limits of normal. 24. Has had administration of radioactive substances or exposure to significant radiation (eg, serial x-ray or computed tomography \[CT\] scans, barium meal) within the past 12 months prior to Day 1 predose. 25. Has any condition that would prevent an MRI from accurately or safely being performed (eg, claustrophobia, cardiac pacemaker, metallic implants or clips) 26. Has any condition that would prevent the performance of a safe or accurate PET scan. 27. Has any clinically significant MRI finding that in the opinion of the investigator would exclude the participant. 28. Is unwilling to refrain from strenuous exercise from 120 hours before Check-in (Day -1) until discharge from the Phase 1 unit. 29. Has a risk of suicide according to the Investigator's clinical judgment (eg, per Columbia-Suicide Severity Rating Scale (C-SSRS) or has made a suicide attempt in the previous 6 months. 30. Has abnormal international normalized ratio (INR) or activated prothrombin time (aPTT) or other risk of bleeding disorder.
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| Phosphodiesterase 10A (PDE10A) Occupancy of Brain Regions With [^11C]T-773 at 3 Hours Following a Single Dose of TAK-063 | 3 hours post-dose | Volume of tissue distribution (Vt) values will be estimated by several quantitative methods for each positron emission tomography (PET) scan. Based on the change in Vt before and after TAK-063 administration, PDE10A occupancy will be calculated. PET scan #2 in the Pilot Cohort and PET scan #1 in the Main Cohort will be used as a baseline for the occupancy calculation. Occupancy is reported for putamen only. |
Secondary
| Measure | Time frame | Description |
|---|---|---|
| Percentage of Participants With Markedly Abnormal Safety Laboratory Findings | From Day 1 to Day 16 | The percentage of participants with any markedly abnormal standard safety laboratory values was collected throughout study. |
| Percentage of Participants With Markedly Abnormal Vital Sign Measurements | From Day 1 to Day 16 | The percentage of participants with any markedly abnormal standard vital sign measurements was collected throughout study. BL=baseline. bpm=beats per minute. |
| Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | From Day 1 to Day 16 | The percentage of participants with any markedly abnormal standard 12-lead ECG measurements. QTc - Bazett's Interval (msec) is ≥500 msec OR ≥30 msec change from Baseline and ≥450 msec |
| Cmax: Maximum Observed Plasma Concentration for TAK-063 and TAK-063 Metabolite M-I | Pilot Cohort: Day 2 predose and at multiple time points (up to 24 hours) post-dose. Main Cohort: Day 1 predose and at multiple time points (up to 24 hours) post-dose. | Maximum observed plasma concentration (Cmax) is the peak plasma concentration of a drug after administration, obtained directly from the plasma concentration-time curve. |
| Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-063 and TAK-063 Metabolite M-I | Pilot Cohort: Day 2 predose and at multiple time points (up to 24 hours) post-dose. Main Cohort: Day 1 predose and at multiple time points (up to 24 hours) post-dose. | Time to reach the maximum plasma concentration (Cmax), equal to time (hours) to Cmax. |
| AUC(0-tlqc): Area Under the Plasma Concentration-Time Curve From Time 0 to the Time of the Last Quantifiable Concentration for TAK-063 and TAK-063 Metabolite M-I | Pilot Cohort: Day 2 predose and at multiple time points (up to 24 hours) post-dose. Main Cohort: Day 1 predose and at multiple time points (up to 24 hours) post-dose. | (AUC(0-tlqc) is a measure of total plasma exposure to the drug from Time 0 to Time of the Last Quantifiable Concentration (AUC\[0-tlqc\]). |
| AUC(0-24): Area Under the Plasma Concentration-Time Curve From Time 0 to 24 Hours Postdose for TAK-063 and TAK-063 Metabolite M-I | Pilot Cohort: Day 2 predose and at multiple time points (up to 24 hours) post-dose. Main Cohort: Day 1 predose and at multiple time points (up to 24 hours) post-dose. | AUC(0-24) is a measure of total plasma exposure to the drug from Time 0 to 24 hours post-dose. |
| Average Plasma Concentration on Day 1 (Cavg) for TAK-063 and TAK-063 Metabolite M-I | Pilot Cohort: Day 2 predose and at multiple time points (up to 24 hours) post-dose. Main Cohort: Day 1 predose and at multiple time points (up to 24 hours) post-dose. | Cavg is the average plasma concentration on Day 1, calculated as AUC(0-24)/24. |
| CL/F: Oral Clearance of TAK-063 | Pilot Cohort: Day 2 predose and at multiple time points (up to 24 hours) post-dose. Main Cohort: Day 1 predose and at multiple time points (up to 24 hours) post-dose. | CL/F is apparent clearance of the drug from the plasma, calculated as the drug dose divided by area under the curve from time 0 to 24 hours post-dose, after multiple dosing (at steady state). |
| Ratio of TAK-063 Metabolite Cmax to TAK-063 Cmax | Pilot Cohort: Day 2 predose and at multiple time points (up to 24 hours) post-dose. Main Cohort: Day 1 predose and at multiple time points (up to 24 hours) post-dose. | Cmax Ratio is the ratio of Cmax values of the metabolite compared to the parent calculated by dividing Cmax values of metabolite M-I with those of the parent drug TAK-063. |
| Ratio of TAK-063 Metabolite M-I AUC( 0-24) to TAK-063 AUC (0-24) | Pilot Cohort: Day 2 predose and at multiple time points (up to 24 hours) post-dose. Main Cohort: Day 1 predose and at multiple time points (up to 24 hours) post-dose. | AUC Ratio is the ratio of AUC values of the metabolite compared to the parent calculated by dividing AUC values of metabolite M-I with those of the parent drug TAK-063. |
| AUC During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 3 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I | 3 hours post-dose | AUC values of TAK-063 and TAK-063 metabolite M-I during the PET scan at approximately 3 hours post TAK-063 administration. |
| Cavg During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 3 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I | 3 hours post-dose | Cavg values of TAK-063 and TAK-063 metabolite M-I during the PET scan at approximately 3 hours post TAK-063 administration. |
| AUC During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 23 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I | 23 hours post-dose | AUC values of TAK-063 and TAK-063 metabolite M-I during the PET scan at approximately 23 hours post TAK-063 administration. Data was not available for participants in the pilot cohort. |
| Cavg During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 23 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I | 23 hours post-dose | Cavg values of TAK-063 and TAK-063 metabolite M-I during the PET scan at approximately 23 hours post TAK-063 administration. Data is not available for the pilot cohort. |
| Percentage of Participants Who Experienced at Least 1 Treatment-Emergent Adverse Event | First dose of study drug to 30 days after last dose of study drug (up to 46 days) | An adverse event (AE) is defined as any untoward medical occurrence in a clinical investigation participant administered a drug; it does not necessarily have to have a causal relationship with this treatment. An AE can therefore be any unfavorable and unintended sign (eg, a clinically significant abnormal laboratory finding), symptom, or disease temporally associated with the use of a drug, whether or not it is considered related to the drug. A treatment-emergent adverse event is defined as an adverse event with an onset that occurs after receiving study drug. |
| Phosphodiesterase 10A (PDE10A) Occupancy of Brain Regions With [^11C]T-773 at 23 Hours Following a Single Dose of TAK-063 | 23 hours post-dose | Volume of tissue distribution (Vt) values will be estimated by several quantitative methods for each positron emission tomography (PET) scan. Based on the change in Vt before and after TAK-063 administration, PDE10A occupancy will be calculated. PET scan #2 in the Pilot Cohort and PET scan #1 in the Main Cohort will be used as a baseline for the occupancy calculation. Data was not available for participants in the pilot cohort. Occupancy is reported for putamen only. |
Contacts
STUDY_DIRECTORMedical Director Clinical Science
Takeda (Note: This product was divested to Axsome in 2026)
Participant flow
Recruitment details
Participants took part in the study at 1 investigative site in Sweden from 13 August 2013 to 12 March 2014.
Pre-assignment details
Healthy Volunteers received 1 of 5 treatments: 11C T-773,Tak-063 3 mg, Tak-063 10 mg, Tak-063 30 mg, Tak-063 100 mg or Tak-063 1000 mg.
Participants by arm
| Arm | Count |
|---|---|
| [^11C]T-773 \[\^11C\]T-773 \<8 μg; 400MBq ± 10%, intravenous (IV), once on Days 1 and 2 only. | 1 |
| TAK-063 3 mg + [^11C]T-773 TAK-063 3 mg, tablets, orally, once, on Day 1, and \[\^11C\]T-773 \<8 μg; 400MBq ± 10%, intravenously (IV), prior to PET scans, twice on Day 1 (before and after administration of TAK-063) and once on Day 2. | 2 |
| TAK-063 10 mg + [^11C]T-773 TAK-063 10 mg, tablets, orally, once, on Day 1, and \[\^11C\]T-773 \<8 μg; 400MBq ± 10%, intravenously (IV), prior to PET scans, twice on Day 1 (before and after administration of TAK-063) and once on Day 2. | 2 |
| TAK-063 30 mg + [^11C]T-773 For main cohort, TAK-063 30 mg, tablets, orally, once, on Day 1, and \[\^11C\]T-773 \<8 μg; 400MBq ± 10%, intravenously (IV), prior to PET scans, twice on Day 1 (before and after administration of TAK-063) and once on Day 2. For pilot cohort, TAK-063 30 mg, tablets, orally, once on Day 2, and \[\^11C\]T-773 \<8 μg; 400MBq ± 10%, intravenously (IV), prior to PET scans, once on Day 1 (before and after administration of TAK-063) and twice on Day 2. | 3 |
| TAK-063 100 mg + [^11C]T-773 TAK-063 100 mg, tablets, orally, once, on Day 1, and \[\^11C\]T-773 \<8 μg; 400MBq ± 10%, intravenously (IV), prior to PET scans, twice on Day 1 (before and after administration of TAK-063) and once on Day 2. | 3 |
| TAK-063 1000 mg + [^11C]T-773 TAK-063 1000 mg, tablets, orally, once, on Day 2, and \[\^11C\]T-773 \<8 μg; 400MBq ± 10%, intravenously (IV), prior to PET scans, once on Day 1 and twice on Day 2 (before and after administration of TAK-063). | 2 |
| Total | 13 |
Baseline characteristics
| Characteristic | TAK-063 10 mg + [^11C]T-773 | TAK-063 30 mg + [^11C]T-773 | TAK-063 100 mg + [^11C]T-773 | TAK-063 1000 mg + [^11C]T-773 | Total | [^11C]T-773 | TAK-063 3 mg + [^11C]T-773 |
|---|---|---|---|---|---|---|---|
| Age, Continuous | 26.5 years STANDARD_DEVIATION 0.71 | 37.7 years STANDARD_DEVIATION 7.09 | 26.7 years STANDARD_DEVIATION 3.51 | 27.0 years STANDARD_DEVIATION 1.41 | 29.2 years STANDARD_DEVIATION 6.08 | 24.0 years | 27.5 years STANDARD_DEVIATION 4.95 |
| Body Mass Index (BMI) | 27.92 kg/m^2 STANDARD_DEVIATION 1.089 | 27.27 kg/m^2 STANDARD_DEVIATION 3.267 | 25.86 kg/m^2 STANDARD_DEVIATION 4.584 | 25.80 kg/m^2 STANDARD_DEVIATION 2.701 | 26.04 kg/m^2 STANDARD_DEVIATION 2.883 | 24.78 kg/m^2 | 23.47 kg/m^2 STANDARD_DEVIATION 1.117 |
| Height | 180.0 cm STANDARD_DEVIATION 1.41 | 178.0 cm STANDARD_DEVIATION 8.19 | 179.3 cm STANDARD_DEVIATION 7.51 | 177.0 cm STANDARD_DEVIATION 4.24 | 179.2 cm STANDARD_DEVIATION 5.2 | 183.0 cm | 180.5 cm STANDARD_DEVIATION 4.95 |
| Race/Ethnicity, Customized White | 2 participants | 3 participants | 3 participants | 2 participants | 13 participants | 1 participants | 2 participants |
| Region of Enrollment Sweden | 2 participants | 3 participants | 3 participants | 2 participants | 13 participants | 1 participants | 2 participants |
| Sex: Female, Male Female | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants | 0 Participants |
| Sex: Female, Male Male | 2 Participants | 3 Participants | 3 Participants | 2 Participants | 13 Participants | 1 Participants | 2 Participants |
| Smoking Classification Current smoker | 0 participants | 0 participants | 0 participants | 0 participants | 0 participants | 0 participants | 0 participants |
| Smoking Classification Ex-smoker | 0 participants | 2 participants | 0 participants | 0 participants | 2 participants | 0 participants | 0 participants |
| Smoking Classification Never smoked | 2 participants | 1 participants | 3 participants | 2 participants | 11 participants | 1 participants | 2 participants |
| Weight | 90.50 kg STANDARD_DEVIATION 4.95 | 85.90 kg STANDARD_DEVIATION 3.651 | 83.27 kg STANDARD_DEVIATION 15.938 | 80.65 kg STANDARD_DEVIATION 4.596 | 83.51 kg STANDARD_DEVIATION 8.233 | 83.00 kg | 76.40 kg STANDARD_DEVIATION 0.566 |
Adverse events
| Event type | EG000 affected / at risk | EG001 affected / at risk |
|---|---|---|
| other Total, other adverse events | 5 / 13 | 9 / 12 |
| serious Total, serious adverse events | 0 / 13 | 0 / 12 |
Outcome results
Primary
Phosphodiesterase 10A (PDE10A) Occupancy of Brain Regions With [^11C]T-773 at 3 Hours Following a Single Dose of TAK-063
Volume of tissue distribution (Vt) values will be estimated by several quantitative methods for each positron emission tomography (PET) scan. Based on the change in Vt before and after TAK-063 administration, PDE10A occupancy will be calculated. PET scan #2 in the Pilot Cohort and PET scan #1 in the Main Cohort will be used as a baseline for the occupancy calculation. Occupancy is reported for putamen only.
Time frame: 3 hours post-dose
Population: Pharmacodynamic Analysis Set includes all participants with data available for pharmacodynamic analysis..
| Arm | Measure | Value (MEAN) | Dispersion |
|---|---|---|---|
| TAK-063 3 mg + [^11C]T-773 | Phosphodiesterase 10A (PDE10A) Occupancy of Brain Regions With [^11C]T-773 at 3 Hours Following a Single Dose of TAK-063 | 14.400 Percent | Standard Deviation 16.4049 |
| TAK-063 10 mg | Phosphodiesterase 10A (PDE10A) Occupancy of Brain Regions With [^11C]T-773 at 3 Hours Following a Single Dose of TAK-063 | 26.650 Percent | Standard Deviation 2.4749 |
| TAK-063 30 mg + [^11C]T-773 | Phosphodiesterase 10A (PDE10A) Occupancy of Brain Regions With [^11C]T-773 at 3 Hours Following a Single Dose of TAK-063 | 39.333 Percent | Standard Deviation 11.1096 |
| TAK-063 100 mg + [^11C]T-773 | Phosphodiesterase 10A (PDE10A) Occupancy of Brain Regions With [^11C]T-773 at 3 Hours Following a Single Dose of TAK-063 | 53.633 Percent | Standard Deviation 0.9074 |
| TAK-063 1000 mg + [^11C]T-773 | Phosphodiesterase 10A (PDE10A) Occupancy of Brain Regions With [^11C]T-773 at 3 Hours Following a Single Dose of TAK-063 | 69.350 Percent | Standard Deviation 3.8891 |
Secondary
AUC(0-24): Area Under the Plasma Concentration-Time Curve From Time 0 to 24 Hours Postdose for TAK-063 and TAK-063 Metabolite M-I
AUC(0-24) is a measure of total plasma exposure to the drug from Time 0 to 24 hours post-dose.
Time frame: Pilot Cohort: Day 2 predose and at multiple time points (up to 24 hours) post-dose. Main Cohort: Day 1 predose and at multiple time points (up to 24 hours) post-dose.
Population: Pharmacokinetic Analysis Set
| Arm | Measure | Group | Value (MEAN) | Dispersion |
|---|---|---|---|---|
| TAK-063 3 mg + [^11C]T-773 | AUC(0-24): Area Under the Plasma Concentration-Time Curve From Time 0 to 24 Hours Postdose for TAK-063 and TAK-063 Metabolite M-I | TAK-063 | 92.55 ng*hr/mL | Standard Deviation 5.348 |
| TAK-063 3 mg + [^11C]T-773 | AUC(0-24): Area Under the Plasma Concentration-Time Curve From Time 0 to 24 Hours Postdose for TAK-063 and TAK-063 Metabolite M-I | TAK-063 Metabolite M-I | 89.64 ng*hr/mL | Standard Deviation 23.672 |
| TAK-063 10 mg | AUC(0-24): Area Under the Plasma Concentration-Time Curve From Time 0 to 24 Hours Postdose for TAK-063 and TAK-063 Metabolite M-I | TAK-063 | 324.98 ng*hr/mL | Standard Deviation 68.303 |
| TAK-063 10 mg | AUC(0-24): Area Under the Plasma Concentration-Time Curve From Time 0 to 24 Hours Postdose for TAK-063 and TAK-063 Metabolite M-I | TAK-063 Metabolite M-I | 249.82 ng*hr/mL | Standard Deviation 31.357 |
| TAK-063 30 mg + [^11C]T-773 | AUC(0-24): Area Under the Plasma Concentration-Time Curve From Time 0 to 24 Hours Postdose for TAK-063 and TAK-063 Metabolite M-I | TAK-063 | 774.44 ng*hr/mL | Standard Deviation 129.997 |
| TAK-063 30 mg + [^11C]T-773 | AUC(0-24): Area Under the Plasma Concentration-Time Curve From Time 0 to 24 Hours Postdose for TAK-063 and TAK-063 Metabolite M-I | TAK-063 Metabolite M-I | 519.82 ng*hr/mL | Standard Deviation 233.869 |
| TAK-063 100 mg + [^11C]T-773 | AUC(0-24): Area Under the Plasma Concentration-Time Curve From Time 0 to 24 Hours Postdose for TAK-063 and TAK-063 Metabolite M-I | TAK-063 Metabolite M-I | 864.14 ng*hr/mL | Standard Deviation 332.414 |
| TAK-063 100 mg + [^11C]T-773 | AUC(0-24): Area Under the Plasma Concentration-Time Curve From Time 0 to 24 Hours Postdose for TAK-063 and TAK-063 Metabolite M-I | TAK-063 | 910.12 ng*hr/mL | Standard Deviation 184.418 |
| TAK-063 1000 mg + [^11C]T-773 | AUC(0-24): Area Under the Plasma Concentration-Time Curve From Time 0 to 24 Hours Postdose for TAK-063 and TAK-063 Metabolite M-I | TAK-063 | 3289.62 ng*hr/mL | Standard Deviation 110.695 |
| TAK-063 1000 mg + [^11C]T-773 | AUC(0-24): Area Under the Plasma Concentration-Time Curve From Time 0 to 24 Hours Postdose for TAK-063 and TAK-063 Metabolite M-I | TAK-063 Metabolite M-I | 1859.97 ng*hr/mL | Standard Deviation 309.411 |
Secondary
AUC(0-tlqc): Area Under the Plasma Concentration-Time Curve From Time 0 to the Time of the Last Quantifiable Concentration for TAK-063 and TAK-063 Metabolite M-I
(AUC(0-tlqc) is a measure of total plasma exposure to the drug from Time 0 to Time of the Last Quantifiable Concentration (AUC\[0-tlqc\]).
Time frame: Pilot Cohort: Day 2 predose and at multiple time points (up to 24 hours) post-dose. Main Cohort: Day 1 predose and at multiple time points (up to 24 hours) post-dose.
Population: Pharmacokinetic Analysis Set
| Arm | Measure | Group | Value (MEAN) | Dispersion |
|---|---|---|---|---|
| TAK-063 3 mg + [^11C]T-773 | AUC(0-tlqc): Area Under the Plasma Concentration-Time Curve From Time 0 to the Time of the Last Quantifiable Concentration for TAK-063 and TAK-063 Metabolite M-I | TAK-063 | 91.42 ng*hr/mL | Standard Deviation 5.795 |
| TAK-063 3 mg + [^11C]T-773 | AUC(0-tlqc): Area Under the Plasma Concentration-Time Curve From Time 0 to the Time of the Last Quantifiable Concentration for TAK-063 and TAK-063 Metabolite M-I | TAK-063 Metabolite M-I | 88.74 ng*hr/mL | Standard Deviation 23.833 |
| TAK-063 10 mg | AUC(0-tlqc): Area Under the Plasma Concentration-Time Curve From Time 0 to the Time of the Last Quantifiable Concentration for TAK-063 and TAK-063 Metabolite M-I | TAK-063 | 318.56 ng*hr/mL | Standard Deviation 66.183 |
| TAK-063 10 mg | AUC(0-tlqc): Area Under the Plasma Concentration-Time Curve From Time 0 to the Time of the Last Quantifiable Concentration for TAK-063 and TAK-063 Metabolite M-I | TAK-063 Metabolite M-I | 245.24 ng*hr/mL | Standard Deviation 30.128 |
| TAK-063 30 mg + [^11C]T-773 | AUC(0-tlqc): Area Under the Plasma Concentration-Time Curve From Time 0 to the Time of the Last Quantifiable Concentration for TAK-063 and TAK-063 Metabolite M-I | TAK-063 | 774.76 ng*hr/mL | Standard Deviation 127.644 |
| TAK-063 30 mg + [^11C]T-773 | AUC(0-tlqc): Area Under the Plasma Concentration-Time Curve From Time 0 to the Time of the Last Quantifiable Concentration for TAK-063 and TAK-063 Metabolite M-I | TAK-063 Metabolite M-I | 519.92 ng*hr/mL | Standard Deviation 233.914 |
| TAK-063 100 mg + [^11C]T-773 | AUC(0-tlqc): Area Under the Plasma Concentration-Time Curve From Time 0 to the Time of the Last Quantifiable Concentration for TAK-063 and TAK-063 Metabolite M-I | TAK-063 Metabolite M-I | 850.26 ng*hr/mL | Standard Deviation 325.161 |
| TAK-063 100 mg + [^11C]T-773 | AUC(0-tlqc): Area Under the Plasma Concentration-Time Curve From Time 0 to the Time of the Last Quantifiable Concentration for TAK-063 and TAK-063 Metabolite M-I | TAK-063 | 897.17 ng*hr/mL | Standard Deviation 181.699 |
| TAK-063 1000 mg + [^11C]T-773 | AUC(0-tlqc): Area Under the Plasma Concentration-Time Curve From Time 0 to the Time of the Last Quantifiable Concentration for TAK-063 and TAK-063 Metabolite M-I | TAK-063 | 3288.62 ng*hr/mL | Standard Deviation 109.282 |
| TAK-063 1000 mg + [^11C]T-773 | AUC(0-tlqc): Area Under the Plasma Concentration-Time Curve From Time 0 to the Time of the Last Quantifiable Concentration for TAK-063 and TAK-063 Metabolite M-I | TAK-063 Metabolite M-I | 1859.28 ng*hr/mL | Standard Deviation 308.436 |
Secondary
AUC During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 23 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I
AUC values of TAK-063 and TAK-063 metabolite M-I during the PET scan at approximately 23 hours post TAK-063 administration. Data was not available for participants in the pilot cohort.
Time frame: 23 hours post-dose
Population: Pharmacokinetic Analysis Set
| Arm | Measure | Group | Value (MEAN) | Dispersion |
|---|---|---|---|---|
| TAK-063 3 mg + [^11C]T-773 | AUC During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 23 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I | TAK-063 | 1.75 ng*hr/mL | Standard Deviation 0.496 |
| TAK-063 3 mg + [^11C]T-773 | AUC During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 23 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I | TAK-063 Metabolite M-I | 1.43 ng*hr/mL | Standard Deviation 0.071 |
| TAK-063 10 mg | AUC During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 23 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I | TAK-063 Metabolite M-I | 8.20 ng*hr/mL | Standard Deviation 2.631 |
| TAK-063 10 mg | AUC During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 23 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I | TAK-063 | 11.44 ng*hr/mL | Standard Deviation 4.243 |
| TAK-063 30 mg + [^11C]T-773 | AUC During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 23 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I | TAK-063 | 21.22 ng*hr/mL | — |
| TAK-063 30 mg + [^11C]T-773 | AUC During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 23 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I | TAK-063 Metabolite M-I | 19.96 ng*hr/mL | — |
| TAK-063 100 mg + [^11C]T-773 | AUC During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 23 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I | TAK-063 | 21.15 ng*hr/mL | Standard Deviation 7.913 |
| TAK-063 100 mg + [^11C]T-773 | AUC During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 23 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I | TAK-063 Metabolite M-I | 22.97 ng*hr/mL | Standard Deviation 15.919 |
Secondary
AUC During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 3 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I
AUC values of TAK-063 and TAK-063 metabolite M-I during the PET scan at approximately 3 hours post TAK-063 administration.
Time frame: 3 hours post-dose
Population: Pharmacokinetic Analysis Set
| Arm | Measure | Group | Value (MEAN) | Dispersion |
|---|---|---|---|---|
| TAK-063 3 mg + [^11C]T-773 | AUC During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 3 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I | TAK-063 | 9.51 ng*hr/mL | Standard Deviation 1.217 |
| TAK-063 3 mg + [^11C]T-773 | AUC During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 3 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I | TAK-063 Metabolite M-I | 10.23 ng*hr/mL | Standard Deviation 3.85 |
| TAK-063 10 mg | AUC During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 3 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I | TAK-063 | 25.68 ng*hr/mL | Standard Deviation 0.97 |
| TAK-063 10 mg | AUC During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 3 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I | TAK-063 Metabolite M-I | 22.56 ng*hr/mL | Standard Deviation 1.272 |
| TAK-063 30 mg + [^11C]T-773 | AUC During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 3 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I | TAK-063 | 63.18 ng*hr/mL | Standard Deviation 13.667 |
| TAK-063 30 mg + [^11C]T-773 | AUC During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 3 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I | TAK-063 Metabolite M-I | 49.09 ng*hr/mL | Standard Deviation 21.273 |
| TAK-063 100 mg + [^11C]T-773 | AUC During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 3 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I | TAK-063 Metabolite M-I | 85.13 ng*hr/mL | Standard Deviation 29.151 |
| TAK-063 100 mg + [^11C]T-773 | AUC During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 3 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I | TAK-063 | 82.25 ng*hr/mL | Standard Deviation 16.404 |
| TAK-063 1000 mg + [^11C]T-773 | AUC During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 3 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I | TAK-063 | 269.32 ng*hr/mL | Standard Deviation 23.429 |
| TAK-063 1000 mg + [^11C]T-773 | AUC During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 3 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I | TAK-063 Metabolite M-I | 162.23 ng*hr/mL | Standard Deviation 6.527 |
Secondary
Average Plasma Concentration on Day 1 (Cavg) for TAK-063 and TAK-063 Metabolite M-I
Cavg is the average plasma concentration on Day 1, calculated as AUC(0-24)/24.
Time frame: Pilot Cohort: Day 2 predose and at multiple time points (up to 24 hours) post-dose. Main Cohort: Day 1 predose and at multiple time points (up to 24 hours) post-dose.
Population: Pharmacokinetic Analysis Set
| Arm | Measure | Group | Value (MEAN) | Dispersion |
|---|---|---|---|---|
| TAK-063 3 mg + [^11C]T-773 | Average Plasma Concentration on Day 1 (Cavg) for TAK-063 and TAK-063 Metabolite M-I | TAK-063 | 3.86 ng/mL | Standard Deviation 0.223 |
| TAK-063 3 mg + [^11C]T-773 | Average Plasma Concentration on Day 1 (Cavg) for TAK-063 and TAK-063 Metabolite M-I | TAK-063 Metabolite M-I | 3.74 ng/mL | Standard Deviation 0.986 |
| TAK-063 10 mg | Average Plasma Concentration on Day 1 (Cavg) for TAK-063 and TAK-063 Metabolite M-I | TAK-063 | 13.54 ng/mL | Standard Deviation 2.846 |
| TAK-063 10 mg | Average Plasma Concentration on Day 1 (Cavg) for TAK-063 and TAK-063 Metabolite M-I | TAK-063 Metabolite M-I | 10.41 ng/mL | Standard Deviation 1.307 |
| TAK-063 30 mg + [^11C]T-773 | Average Plasma Concentration on Day 1 (Cavg) for TAK-063 and TAK-063 Metabolite M-I | TAK-063 | 32.27 ng/mL | Standard Deviation 5.417 |
| TAK-063 30 mg + [^11C]T-773 | Average Plasma Concentration on Day 1 (Cavg) for TAK-063 and TAK-063 Metabolite M-I | TAK-063 Metabolite M-I | 21.66 ng/mL | Standard Deviation 9.745 |
| TAK-063 100 mg + [^11C]T-773 | Average Plasma Concentration on Day 1 (Cavg) for TAK-063 and TAK-063 Metabolite M-I | TAK-063 Metabolite M-I | 36.01 ng/mL | Standard Deviation 13.851 |
| TAK-063 100 mg + [^11C]T-773 | Average Plasma Concentration on Day 1 (Cavg) for TAK-063 and TAK-063 Metabolite M-I | TAK-063 | 37.92 ng/mL | Standard Deviation 7.684 |
| TAK-063 1000 mg + [^11C]T-773 | Average Plasma Concentration on Day 1 (Cavg) for TAK-063 and TAK-063 Metabolite M-I | TAK-063 | 137.07 ng/mL | Standard Deviation 4.612 |
| TAK-063 1000 mg + [^11C]T-773 | Average Plasma Concentration on Day 1 (Cavg) for TAK-063 and TAK-063 Metabolite M-I | TAK-063 Metabolite M-I | 77.50 ng/mL | Standard Deviation 12.892 |
Secondary
Cavg During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 23 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I
Cavg values of TAK-063 and TAK-063 metabolite M-I during the PET scan at approximately 23 hours post TAK-063 administration. Data is not available for the pilot cohort.
Time frame: 23 hours post-dose
Population: Pharmacokinetic Analysis Set
| Arm | Measure | Group | Value (MEAN) | Dispersion |
|---|---|---|---|---|
| TAK-063 3 mg + [^11C]T-773 | Cavg During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 23 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I | TAK-063 | 1.40 ng/mL | Standard Deviation 0.397 |
| TAK-063 3 mg + [^11C]T-773 | Cavg During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 23 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I | TAK-063 Metabolite M- | 1.15 ng/mL | Standard Deviation 0.056 |
| TAK-063 10 mg | Cavg During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 23 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I | TAK-063 Metabolite M- | 6.56 ng/mL | Standard Deviation 2.105 |
| TAK-063 10 mg | Cavg During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 23 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I | TAK-063 | 9.15 ng/mL | Standard Deviation 3.394 |
| TAK-063 30 mg + [^11C]T-773 | Cavg During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 23 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I | TAK-063 Metabolite M- | 15.97 ng/mL | — |
| TAK-063 30 mg + [^11C]T-773 | Cavg During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 23 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I | TAK-063 | 16.97 ng/mL | — |
| TAK-063 100 mg + [^11C]T-773 | Cavg During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 23 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I | TAK-063 | 16.92 ng/mL | Standard Deviation 6.331 |
| TAK-063 100 mg + [^11C]T-773 | Cavg During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 23 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I | TAK-063 Metabolite M- | 18.37 ng/mL | Standard Deviation 12.735 |
Secondary
Cavg During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 3 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I
Cavg values of TAK-063 and TAK-063 metabolite M-I during the PET scan at approximately 3 hours post TAK-063 administration.
Time frame: 3 hours post-dose
Population: Pharmacokinetic Analysis Set
| Arm | Measure | Group | Value (MEAN) | Dispersion |
|---|---|---|---|---|
| TAK-063 3 mg + [^11C]T-773 | Cavg During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 3 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I | TAK-063 | 7.61 ng/mL | Standard Deviation 0.974 |
| TAK-063 3 mg + [^11C]T-773 | Cavg During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 3 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I | TAK-063 Metabolite M-I | 8.18 ng/mL | Standard Deviation 3.08 |
| TAK-063 10 mg | Cavg During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 3 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I | TAK-063 | 20.54 ng/mL | Standard Deviation 0.776 |
| TAK-063 10 mg | Cavg During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 3 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I | TAK-063 Metabolite M-I | 18.05 ng/mL | Standard Deviation 1.018 |
| TAK-063 30 mg + [^11C]T-773 | Cavg During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 3 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I | TAK-063 | 50.54 ng/mL | Standard Deviation 10.934 |
| TAK-063 30 mg + [^11C]T-773 | Cavg During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 3 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I | TAK-063 Metabolite M-I | 39.27 ng/mL | Standard Deviation 17.018 |
| TAK-063 100 mg + [^11C]T-773 | Cavg During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 3 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I | TAK-063 Metabolite M-I | 68.10 ng/mL | Standard Deviation 23.321 |
| TAK-063 100 mg + [^11C]T-773 | Cavg During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 3 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I | TAK-063 | 65.80 ng/mL | Standard Deviation 13.123 |
| TAK-063 1000 mg + [^11C]T-773 | Cavg During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 3 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I | TAK-063 | 215.46 ng/mL | Standard Deviation 18.743 |
| TAK-063 1000 mg + [^11C]T-773 | Cavg During the Positron Emission Tomography (PET) Scan Period (AUC(Scan)) at 3 Hours Post-dose for TAK-063 and TAK-063 Metabolite M-I | TAK-063 Metabolite M-I | 129.78 ng/mL | Standard Deviation 5.222 |
Secondary
CL/F: Oral Clearance of TAK-063
CL/F is apparent clearance of the drug from the plasma, calculated as the drug dose divided by area under the curve from time 0 to 24 hours post-dose, after multiple dosing (at steady state).
Time frame: Pilot Cohort: Day 2 predose and at multiple time points (up to 24 hours) post-dose. Main Cohort: Day 1 predose and at multiple time points (up to 24 hours) post-dose.
Population: Pharmacokinetic Analysis Set
| Arm | Measure | Value (MEAN) | Dispersion |
|---|---|---|---|
| TAK-063 3 mg + [^11C]T-773 | CL/F: Oral Clearance of TAK-063 | 26.19 liter/hour | Standard Deviation 1.099 |
| TAK-063 10 mg | CL/F: Oral Clearance of TAK-063 | 18.31 liter/hour | Standard Deviation 7.477 |
| TAK-063 30 mg + [^11C]T-773 | CL/F: Oral Clearance of TAK-063 | 24.90 liter/hour | Standard Deviation 2.209 |
| TAK-063 100 mg + [^11C]T-773 | CL/F: Oral Clearance of TAK-063 | 88.86 liter/hour | Standard Deviation 25.806 |
| TAK-063 1000 mg + [^11C]T-773 | CL/F: Oral Clearance of TAK-063 | 252.33 liter/hour | Standard Deviation 21.971 |
Secondary
Cmax: Maximum Observed Plasma Concentration for TAK-063 and TAK-063 Metabolite M-I
Maximum observed plasma concentration (Cmax) is the peak plasma concentration of a drug after administration, obtained directly from the plasma concentration-time curve.
Time frame: Pilot Cohort: Day 2 predose and at multiple time points (up to 24 hours) post-dose. Main Cohort: Day 1 predose and at multiple time points (up to 24 hours) post-dose.
Population: Pharmacokinetic Analysis Set
| Arm | Measure | Group | Value (MEAN) | Dispersion |
|---|---|---|---|---|
| TAK-063 3 mg + [^11C]T-773 | Cmax: Maximum Observed Plasma Concentration for TAK-063 and TAK-063 Metabolite M-I | TAK-063 | 11.25 ng/mL | Standard Deviation 3.323 |
| TAK-063 3 mg + [^11C]T-773 | Cmax: Maximum Observed Plasma Concentration for TAK-063 and TAK-063 Metabolite M-I | TAK-063 Metabolite M-I | 15.60 ng/mL | Standard Deviation 7.637 |
| TAK-063 10 mg | Cmax: Maximum Observed Plasma Concentration for TAK-063 and TAK-063 Metabolite M-I | TAK-063 | 22.78 ng/mL | Standard Deviation 0.035 |
| TAK-063 10 mg | Cmax: Maximum Observed Plasma Concentration for TAK-063 and TAK-063 Metabolite M-I | TAK-063 Metabolite M-I | 19.65 ng/mL | Standard Deviation 0.283 |
| TAK-063 30 mg + [^11C]T-773 | Cmax: Maximum Observed Plasma Concentration for TAK-063 and TAK-063 Metabolite M-I | TAK-063 | 80.67 ng/mL | Standard Deviation 35.147 |
| TAK-063 30 mg + [^11C]T-773 | Cmax: Maximum Observed Plasma Concentration for TAK-063 and TAK-063 Metabolite M-I | TAK-063 Metabolite M-I | 49.63 ng/mL | Standard Deviation 18.393 |
| TAK-063 100 mg + [^11C]T-773 | Cmax: Maximum Observed Plasma Concentration for TAK-063 and TAK-063 Metabolite M-I | TAK-063 Metabolite M-I | 80.43 ng/mL | Standard Deviation 26.831 |
| TAK-063 100 mg + [^11C]T-773 | Cmax: Maximum Observed Plasma Concentration for TAK-063 and TAK-063 Metabolite M-I | TAK-063 | 77.05 ng/mL | Standard Deviation 16.898 |
| TAK-063 1000 mg + [^11C]T-773 | Cmax: Maximum Observed Plasma Concentration for TAK-063 and TAK-063 Metabolite M-I | TAK-063 | 258.75 ng/mL | Standard Deviation 18.031 |
| TAK-063 1000 mg + [^11C]T-773 | Cmax: Maximum Observed Plasma Concentration for TAK-063 and TAK-063 Metabolite M-I | TAK-063 Metabolite M-I | 146.50 ng/mL | Standard Deviation 10.607 |
Secondary
Percentage of Participants Who Experienced at Least 1 Treatment-Emergent Adverse Event
An adverse event (AE) is defined as any untoward medical occurrence in a clinical investigation participant administered a drug; it does not necessarily have to have a causal relationship with this treatment. An AE can therefore be any unfavorable and unintended sign (eg, a clinically significant abnormal laboratory finding), symptom, or disease temporally associated with the use of a drug, whether or not it is considered related to the drug. A treatment-emergent adverse event is defined as an adverse event with an onset that occurs after receiving study drug.
Time frame: First dose of study drug to 30 days after last dose of study drug (up to 46 days)
Population: Safety analysis set included all participants who received at least one dose of study drug.
| Arm | Measure | Value (NUMBER) |
|---|---|---|
| TAK-063 3 mg + [^11C]T-773 | Percentage of Participants Who Experienced at Least 1 Treatment-Emergent Adverse Event | 38.5 percentage of participants |
| TAK-063 10 mg | Percentage of Participants Who Experienced at Least 1 Treatment-Emergent Adverse Event | 75.0 percentage of participants |
Secondary
Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters
The percentage of participants with any markedly abnormal standard 12-lead ECG measurements. QTc - Bazett's Interval (msec) is ≥500 msec OR ≥30 msec change from Baseline and ≥450 msec
Time frame: From Day 1 to Day 16
Population: Safety analysis set included all participants who received at least one dose of study drug.
| Arm | Measure | Group | Value (NUMBER) |
|---|---|---|---|
| TAK-063 3 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | RR Interval (msec) - Overall | 0 percentage of participants |
| TAK-063 3 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | Heart Rate (bpm) - Overall | 7.7 percentage of participants |
| TAK-063 3 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | RR Interval (msec) - ≥1440 msec | 0 percentage of participants |
| TAK-063 3 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | RR Interval (msec) - ≤600 msec | 0 percentage of participants |
| TAK-063 3 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | Heart Rate (bpm) - <50 bpm | 7.7 percentage of participants |
| TAK-063 3 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | PR Interval (msec) - ≥200 msec | 0 percentage of participants |
| TAK-063 3 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | PR Interval (msec) - ≤80 msec | 0 percentage of participants |
| TAK-063 3 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | PR Interval (msec) - Overall | 0 percentage of participants |
| TAK-063 3 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | QRS Interval (msec) - ≥180 msec | 0 percentage of participants |
| TAK-063 3 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | QRS Interval (msec) - ≤80 msec | 0 percentage of participants |
| TAK-063 3 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | QRS Interval (msec) - Overall | 0 percentage of participants |
| TAK-063 3 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | QT Interval (msec) - ≥460 msec | 0 percentage of participants |
| TAK-063 3 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | QT Interval (msec) - <280 msec | 0 percentage of participants |
| TAK-063 3 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | QT Interval (msec) - Overall | 0 percentage of participants |
| TAK-063 3 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | QTc - Bazett's Interval (msec) - Overall | 0 percentage of participants |
| TAK-063 3 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | QTc - Fredericia's Interval (msec) - Overall | 0 percentage of participants |
| TAK-063 10 mg | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | RR Interval (msec) - ≤600 msec | 0 percentage of participants |
| TAK-063 10 mg | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | QRS Interval (msec) - ≥180 msec | 0 percentage of participants |
| TAK-063 10 mg | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | PR Interval (msec) - Overall | 0 percentage of participants |
| TAK-063 10 mg | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | PR Interval (msec) - ≤80 msec | 0 percentage of participants |
| TAK-063 10 mg | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | RR Interval (msec) - ≥1440 msec | 0 percentage of participants |
| TAK-063 10 mg | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | Heart Rate (bpm) - <50 bpm | 50.0 percentage of participants |
| TAK-063 10 mg | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | QT Interval (msec) - Overall | 0 percentage of participants |
| TAK-063 10 mg | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | QT Interval (msec) - <280 msec | 0 percentage of participants |
| TAK-063 10 mg | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | QT Interval (msec) - ≥460 msec | 0 percentage of participants |
| TAK-063 10 mg | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | RR Interval (msec) - Overall | 0 percentage of participants |
| TAK-063 10 mg | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | Heart Rate (bpm) - Overall | 50.0 percentage of participants |
| TAK-063 10 mg | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | QTc - Fredericia's Interval (msec) - Overall | 0 percentage of participants |
| TAK-063 10 mg | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | QRS Interval (msec) - Overall | 0 percentage of participants |
| TAK-063 10 mg | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | QRS Interval (msec) - ≤80 msec | 0 percentage of participants |
| TAK-063 10 mg | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | QTc - Bazett's Interval (msec) - Overall | 0 percentage of participants |
| TAK-063 10 mg | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | PR Interval (msec) - ≥200 msec | 0 percentage of participants |
| TAK-063 30 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | QTc - Bazett's Interval (msec) - Overall | 0 percentage of participants |
| TAK-063 30 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | RR Interval (msec) - ≤600 msec | 0 percentage of participants |
| TAK-063 30 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | RR Interval (msec) - Overall | 0 percentage of participants |
| TAK-063 30 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | PR Interval (msec) - ≥200 msec | 0 percentage of participants |
| TAK-063 30 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | PR Interval (msec) - ≤80 msec | 0 percentage of participants |
| TAK-063 30 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | PR Interval (msec) - Overall | 0 percentage of participants |
| TAK-063 30 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | QRS Interval (msec) - ≥180 msec | 0 percentage of participants |
| TAK-063 30 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | QRS Interval (msec) - ≤80 msec | 0 percentage of participants |
| TAK-063 30 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | QRS Interval (msec) - Overall | 0 percentage of participants |
| TAK-063 30 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | QT Interval (msec) - ≥460 msec | 0 percentage of participants |
| TAK-063 30 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | QTc - Fredericia's Interval (msec) - Overall | 0 percentage of participants |
| TAK-063 30 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | QT Interval (msec) - <280 msec | 0 percentage of participants |
| TAK-063 30 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | QT Interval (msec) - Overall | 0 percentage of participants |
| TAK-063 30 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | Heart Rate (bpm) - <50 bpm | 50.0 percentage of participants |
| TAK-063 30 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | Heart Rate (bpm) - Overall | 50.0 percentage of participants |
| TAK-063 30 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | RR Interval (msec) - ≥1440 msec | 0 percentage of participants |
| TAK-063 100 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | RR Interval (msec) - ≤600 msec | 0 percentage of participants |
| TAK-063 100 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | QRS Interval (msec) - ≥180 msec | 0 percentage of participants |
| TAK-063 100 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | RR Interval (msec) - Overall | 33.3 percentage of participants |
| TAK-063 100 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | RR Interval (msec) - ≥1440 msec | 33.3 percentage of participants |
| TAK-063 100 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | Heart Rate (bpm) - Overall | 33.3 percentage of participants |
| TAK-063 100 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | QT Interval (msec) - ≥460 msec | 33.3 percentage of participants |
| TAK-063 100 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | QTc - Bazett's Interval (msec) - Overall | 0 percentage of participants |
| TAK-063 100 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | QT Interval (msec) - Overall | 33.3 percentage of participants |
| TAK-063 100 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | QRS Interval (msec) - Overall | 0 percentage of participants |
| TAK-063 100 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | QRS Interval (msec) - ≤80 msec | 0 percentage of participants |
| TAK-063 100 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | PR Interval (msec) - Overall | 33.3 percentage of participants |
| TAK-063 100 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | QT Interval (msec) - <280 msec | 0 percentage of participants |
| TAK-063 100 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | Heart Rate (bpm) - <50 bpm | 33.3 percentage of participants |
| TAK-063 100 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | PR Interval (msec) - ≥200 msec | 33.3 percentage of participants |
| TAK-063 100 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | QTc - Fredericia's Interval (msec) - Overall | 0 percentage of participants |
| TAK-063 100 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | PR Interval (msec) - ≤80 msec | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | RR Interval (msec) - ≤600 msec | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | RR Interval (msec) - ≥1440 msec | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | RR Interval (msec) - Overall | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | Heart Rate (bpm) - <50 bpm | 66.7 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | PR Interval (msec) - ≤80 msec | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | PR Interval (msec) - ≥200 msec | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | PR Interval (msec) - Overall | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | QTc - Bazett's Interval (msec) - Overall | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | QRS Interval (msec) - Overall | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | QTc - Fredericia's Interval (msec) - Overall | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | QT Interval (msec) - ≥460 msec | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | QRS Interval (msec) - ≥180 msec | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | Heart Rate (bpm) - Overall | 66.7 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | QRS Interval (msec) - ≤80 msec | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | QT Interval (msec) - <280 msec | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | QT Interval (msec) - Overall | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | PR Interval (msec) - Overall | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | QRS Interval (msec) - ≥180 msec | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | QTc - Bazett's Interval (msec) - Overall | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | RR Interval (msec) - Overall | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | QT Interval (msec) - Overall | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | QRS Interval (msec) - ≤80 msec | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | QTc - Fredericia's Interval (msec) - Overall | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | QRS Interval (msec) - Overall | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | QT Interval (msec) - ≥460 msec | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | RR Interval (msec) - ≤600 msec | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | Heart Rate (bpm) - Overall | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | QT Interval (msec) - <280 msec | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | RR Interval (msec) - ≥1440 msec | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | PR Interval (msec) - ≥200 msec | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | PR Interval (msec) - ≤80 msec | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters | Heart Rate (bpm) - <50 bpm | 0 percentage of participants |
Secondary
Percentage of Participants With Markedly Abnormal Safety Laboratory Findings
The percentage of participants with any markedly abnormal standard safety laboratory values was collected throughout study.
Time frame: From Day 1 to Day 16
Population: Safety analysis set included all participants who received at least one dose of study drug.
| Arm | Measure | Value (NUMBER) |
|---|---|---|
| TAK-063 3 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Safety Laboratory Findings | 0 percentage of participants |
| TAK-063 10 mg | Percentage of Participants With Markedly Abnormal Safety Laboratory Findings | 0 percentage of participants |
| TAK-063 30 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Safety Laboratory Findings | 0 percentage of participants |
| TAK-063 100 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Safety Laboratory Findings | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Safety Laboratory Findings | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Safety Laboratory Findings | 0 percentage of participants |
Secondary
Percentage of Participants With Markedly Abnormal Vital Sign Measurements
The percentage of participants with any markedly abnormal standard vital sign measurements was collected throughout study. BL=baseline. bpm=beats per minute.
Time frame: From Day 1 to Day 16
Population: Safety analysis set included all participants who received at least one dose of study drug.
| Arm | Measure | Group | Value (NUMBER) |
|---|---|---|---|
| TAK-063 3 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Systolic Blood Pressure - Decrease of >40 mmHg | 0 percentage of participants |
| TAK-063 3 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | During tx - Overall | 46.2 percentage of participants |
| TAK-063 3 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Diastolic Blood Pressure (mmHg) - >110 mmHg | 0 percentage of participants |
| TAK-063 3 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Pulse (bpm) - Decrease of >30 bpm | 0 percentage of participants |
| TAK-063 3 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Systolic Blood Pressure (mmHg) - >180 mmHg | 0 percentage of participants |
| TAK-063 3 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Temperature (Degree C) - >37.7 C | 0 percentage of participants |
| TAK-063 3 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Diastolic BP (mmHg) - Decrease of >20 mmHg | 0 percentage of participants |
| TAK-063 3 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Pulse (bpm) - >120 bpm | 0 percentage of participants |
| TAK-063 3 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Systolic Blood Pressure (mmHg) - <85 mmHg | 0 percentage of participants |
| TAK-063 3 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Pulse (bpm) - Increase of >30 bpm | 0 percentage of participants |
| TAK-063 3 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | During tx - <Lower Cut-off | 38.5 percentage of participants |
| TAK-063 3 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Systolic Blood Pressure (mmHg) - Overall | 0 percentage of participants |
| TAK-063 3 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Diastolic Blood Pressure (mmHg) - Overall | 7.7 percentage of participants |
| TAK-063 3 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Pulse (bpm) - <50 bpm | 30.8 percentage of participants |
| TAK-063 3 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Temperature (Degree C) - Overall | 7.7 percentage of participants |
| TAK-063 3 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | During tx - Change Relative to BL Upper Criteria | 7.7 percentage of participants |
| TAK-063 3 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Diastolic Blood Pressure (mmHg) - <50 mmHg | 0 percentage of participants |
| TAK-063 3 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Temperature (Degree C) - <35.6 C | 7.7 percentage of participants |
| TAK-063 3 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | During tx - Change Relative to BL Lower Criteria | 0 percentage of participants |
| TAK-063 3 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Systolic Blood Pressure - Increase of >40 mmHg | 0 percentage of participants |
| TAK-063 3 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Pulse (bpm) - Overall | 30.8 percentage of participants |
| TAK-063 3 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Diastolic BP (mmHg) - Increase of >20 mmHg | 7.7 percentage of participants |
| TAK-063 3 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | During Treatment (tx) - >Upper Cut-off | 0 percentage of participants |
| TAK-063 10 mg | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Diastolic BP (mmHg) - Increase of >20 mmHg | 0 percentage of participants |
| TAK-063 10 mg | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Diastolic Blood Pressure (mmHg) - >110 mmHg | 0 percentage of participants |
| TAK-063 10 mg | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Systolic Blood Pressure - Increase of >40 mmHg | 0 percentage of participants |
| TAK-063 10 mg | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Systolic Blood Pressure (mmHg) - Overall | 0 percentage of participants |
| TAK-063 10 mg | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Systolic Blood Pressure - Decrease of >40 mmHg | 0 percentage of participants |
| TAK-063 10 mg | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | During tx - Change Relative to BL Upper Criteria | 0 percentage of participants |
| TAK-063 10 mg | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | During Treatment (tx) - >Upper Cut-off | 0 percentage of participants |
| TAK-063 10 mg | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Temperature (Degree C) - <35.6 C | 50.0 percentage of participants |
| TAK-063 10 mg | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | During tx - Change Relative to BL Lower Criteria | 0 percentage of participants |
| TAK-063 10 mg | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Temperature (Degree C) - >37.7 C | 0 percentage of participants |
| TAK-063 10 mg | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | During tx - Overall | 50.0 percentage of participants |
| TAK-063 10 mg | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Temperature (Degree C) - Overall | 50.0 percentage of participants |
| TAK-063 10 mg | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Pulse (bpm) - >120 bpm | 0 percentage of participants |
| TAK-063 10 mg | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Diastolic Blood Pressure (mmHg) - Overall | 0 percentage of participants |
| TAK-063 10 mg | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Pulse (bpm) - <50 bpm | 50.0 percentage of participants |
| TAK-063 10 mg | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | During tx - <Lower Cut-off | 50.0 percentage of participants |
| TAK-063 10 mg | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Diastolic BP (mmHg) - Decrease of >20 mmHg | 0 percentage of participants |
| TAK-063 10 mg | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Pulse (bpm) - Increase of >30 bpm | 0 percentage of participants |
| TAK-063 10 mg | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Pulse (bpm) - Decrease of >30 bpm | 0 percentage of participants |
| TAK-063 10 mg | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Pulse (bpm) - Overall | 50.0 percentage of participants |
| TAK-063 10 mg | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Diastolic Blood Pressure (mmHg) - <50 mmHg | 0 percentage of participants |
| TAK-063 10 mg | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Systolic Blood Pressure (mmHg) - >180 mmHg | 0 percentage of participants |
| TAK-063 10 mg | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Systolic Blood Pressure (mmHg) - <85 mmHg | 0 percentage of participants |
| TAK-063 30 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Diastolic Blood Pressure (mmHg) - Overall | 50.0 percentage of participants |
| TAK-063 30 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Diastolic BP (mmHg) - Increase of >20 mmHg | 0 percentage of participants |
| TAK-063 30 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | During tx - Overall | 100.0 percentage of participants |
| TAK-063 30 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Systolic Blood Pressure (mmHg) - Overall | 0 percentage of participants |
| TAK-063 30 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Pulse (bpm) - Decrease of >30 bpm | 0 percentage of participants |
| TAK-063 30 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | During Treatment (tx) - >Upper Cut-off | 0 percentage of participants |
| TAK-063 30 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Temperature (Degree C) - >37.7 C | 0 percentage of participants |
| TAK-063 30 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Temperature (Degree C) - Overall | 0 percentage of participants |
| TAK-063 30 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | During tx - Change Relative to BL Lower Criteria | 50.0 percentage of participants |
| TAK-063 30 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Diastolic Blood Pressure (mmHg) - >110 mmHg | 0 percentage of participants |
| TAK-063 30 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Pulse (bpm) - Overall | 50.0 percentage of participants |
| TAK-063 30 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | During tx - Change Relative to BL Upper Criteria | 0 percentage of participants |
| TAK-063 30 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Diastolic Blood Pressure (mmHg) - <50 mmHg | 0 percentage of participants |
| TAK-063 30 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Systolic Blood Pressure - Increase of >40 mmHg | 0 percentage of participants |
| TAK-063 30 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Systolic Blood Pressure - Decrease of >40 mmHg | 0 percentage of participants |
| TAK-063 30 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Pulse (bpm) - <50 bpm | 50.0 percentage of participants |
| TAK-063 30 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Systolic Blood Pressure (mmHg) - <85 mmHg | 0 percentage of participants |
| TAK-063 30 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Diastolic BP (mmHg) - Decrease of >20 mmHg | 50.0 percentage of participants |
| TAK-063 30 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Systolic Blood Pressure (mmHg) - >180 mmHg | 0 percentage of participants |
| TAK-063 30 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Pulse (bpm) - >120 bpm | 0 percentage of participants |
| TAK-063 30 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Temperature (Degree C) - <35.6 C | 0 percentage of participants |
| TAK-063 30 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Pulse (bpm) - Increase of >30 bpm | 0 percentage of participants |
| TAK-063 30 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | During tx - <Lower Cut-off | 50.0 percentage of participants |
| TAK-063 100 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Systolic Blood Pressure (mmHg) - <85 mmHg | 0 percentage of participants |
| TAK-063 100 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | During Treatment (tx) - >Upper Cut-off | 0 percentage of participants |
| TAK-063 100 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | During tx - <Lower Cut-off | 33.3 percentage of participants |
| TAK-063 100 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | During tx - Change Relative to BL Upper Criteria | 0 percentage of participants |
| TAK-063 100 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | During tx - Change Relative to BL Lower Criteria | 0 percentage of participants |
| TAK-063 100 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | During tx - Overall | 33.3 percentage of participants |
| TAK-063 100 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Pulse (bpm) - >120 bpm | 0 percentage of participants |
| TAK-063 100 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Pulse (bpm) - <50 bpm | 33.3 percentage of participants |
| TAK-063 100 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Pulse (bpm) - Increase of >30 bpm | 0 percentage of participants |
| TAK-063 100 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Pulse (bpm) - Decrease of >30 bpm | 0 percentage of participants |
| TAK-063 100 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Pulse (bpm) - Overall | 33.3 percentage of participants |
| TAK-063 100 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Systolic Blood Pressure (mmHg) - >180 mmHg | 0 percentage of participants |
| TAK-063 100 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Systolic Blood Pressure - Increase of >40 mmHg | 0 percentage of participants |
| TAK-063 100 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Systolic Blood Pressure - Decrease of >40 mmHg | 0 percentage of participants |
| TAK-063 100 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Systolic Blood Pressure (mmHg) - Overall | 0 percentage of participants |
| TAK-063 100 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Diastolic Blood Pressure (mmHg) - >110 mmHg | 0 percentage of participants |
| TAK-063 100 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Diastolic Blood Pressure (mmHg) - <50 mmHg | 0 percentage of participants |
| TAK-063 100 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Diastolic BP (mmHg) - Increase of >20 mmHg | 0 percentage of participants |
| TAK-063 100 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Diastolic BP (mmHg) - Decrease of >20 mmHg | 0 percentage of participants |
| TAK-063 100 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Diastolic Blood Pressure (mmHg) - Overall | 0 percentage of participants |
| TAK-063 100 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Temperature (Degree C) - >37.7 C | 0 percentage of participants |
| TAK-063 100 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Temperature (Degree C) - <35.6 C | 0 percentage of participants |
| TAK-063 100 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Temperature (Degree C) - Overall | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Systolic Blood Pressure (mmHg) - <85 mmHg | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Temperature (Degree C) - <35.6 C | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Diastolic Blood Pressure (mmHg) - >110 mmHg | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Systolic Blood Pressure (mmHg) - >180 mmHg | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Pulse (bpm) - Overall | 66.7 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Diastolic Blood Pressure (mmHg) - <50 mmHg | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Pulse (bpm) - Decrease of >30 bpm | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | During tx - <Lower Cut-off | 66.7 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Diastolic BP (mmHg) - Increase of >20 mmHg | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Pulse (bpm) - Increase of >30 bpm | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Pulse (bpm) - <50 bpm | 66.7 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Diastolic BP (mmHg) - Decrease of >20 mmHg | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Pulse (bpm) - >120 bpm | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | During Treatment (tx) - >Upper Cut-off | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Diastolic Blood Pressure (mmHg) - Overall | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | During tx - Overall | 66.7 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | During tx - Change Relative to BL Lower Criteria | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Temperature (Degree C) - >37.7 C | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | During tx - Change Relative to BL Upper Criteria | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Systolic Blood Pressure - Decrease of >40 mmHg | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Systolic Blood Pressure - Increase of >40 mmHg | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Temperature (Degree C) - Overall | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Systolic Blood Pressure (mmHg) - Overall | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Systolic Blood Pressure (mmHg) - <85 mmHg | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | During tx - Overall | 50.0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | During tx - <Lower Cut-off | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Diastolic Blood Pressure (mmHg) - >110 mmHg | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Systolic Blood Pressure - Decrease of >40 mmHg | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Pulse (bpm) - Overall | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Diastolic Blood Pressure (mmHg) - Overall | 50.0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Temperature (Degree C) - <35.6 C | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Systolic Blood Pressure (mmHg) - >180 mmHg | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Diastolic Blood Pressure (mmHg) - <50 mmHg | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Pulse (bpm) - Decrease of >30 bpm | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | During tx - Change Relative to BL Lower Criteria | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Pulse (bpm) - Increase of >30 bpm | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Systolic Blood Pressure - Increase of >40 mmHg | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Temperature (Degree C) - Overall | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Diastolic BP (mmHg) - Increase of >20 mmHg | 50.0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Systolic Blood Pressure (mmHg) - Overall | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Pulse (bpm) - <50 bpm | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Temperature (Degree C) - >37.7 C | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | During Treatment (tx) - >Upper Cut-off | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | During tx - Change Relative to BL Upper Criteria | 50.0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Diastolic BP (mmHg) - Decrease of >20 mmHg | 0 percentage of participants |
| TAK-063 1000 mg + [^11C]T-773 | Percentage of Participants With Markedly Abnormal Vital Sign Measurements | Pulse (bpm) - >120 bpm | 0 percentage of participants |
Secondary
Phosphodiesterase 10A (PDE10A) Occupancy of Brain Regions With [^11C]T-773 at 23 Hours Following a Single Dose of TAK-063
Volume of tissue distribution (Vt) values will be estimated by several quantitative methods for each positron emission tomography (PET) scan. Based on the change in Vt before and after TAK-063 administration, PDE10A occupancy will be calculated. PET scan #2 in the Pilot Cohort and PET scan #1 in the Main Cohort will be used as a baseline for the occupancy calculation. Data was not available for participants in the pilot cohort. Occupancy is reported for putamen only.
Time frame: 23 hours post-dose
Population: Pharmacodynamic Analysis Set includes all participants with data available for pharmacodynamic analysis.
| Arm | Measure | Value (MEAN) | Dispersion |
|---|---|---|---|
| TAK-063 3 mg + [^11C]T-773 | Phosphodiesterase 10A (PDE10A) Occupancy of Brain Regions With [^11C]T-773 at 23 Hours Following a Single Dose of TAK-063 | -2.250 Percent | Standard Deviation 0.7778 |
| TAK-063 10 mg | Phosphodiesterase 10A (PDE10A) Occupancy of Brain Regions With [^11C]T-773 at 23 Hours Following a Single Dose of TAK-063 | 14.750 Percent | Standard Deviation 1.7678 |
| TAK-063 30 mg + [^11C]T-773 | Phosphodiesterase 10A (PDE10A) Occupancy of Brain Regions With [^11C]T-773 at 23 Hours Following a Single Dose of TAK-063 | 18.800 Percent | — |
| TAK-063 100 mg + [^11C]T-773 | Phosphodiesterase 10A (PDE10A) Occupancy of Brain Regions With [^11C]T-773 at 23 Hours Following a Single Dose of TAK-063 | 24.167 Percent | Standard Deviation 18.6001 |
Secondary
Ratio of TAK-063 Metabolite Cmax to TAK-063 Cmax
Cmax Ratio is the ratio of Cmax values of the metabolite compared to the parent calculated by dividing Cmax values of metabolite M-I with those of the parent drug TAK-063.
Time frame: Pilot Cohort: Day 2 predose and at multiple time points (up to 24 hours) post-dose. Main Cohort: Day 1 predose and at multiple time points (up to 24 hours) post-dose.
Population: Pharmacokinetic Analysis Set
| Arm | Measure | Value (MEAN) | Dispersion |
|---|---|---|---|
| TAK-063 3 mg + [^11C]T-773 | Ratio of TAK-063 Metabolite Cmax to TAK-063 Cmax | 1.30 ratio | Standard Deviation 0.271 |
| TAK-063 10 mg | Ratio of TAK-063 Metabolite Cmax to TAK-063 Cmax | 0.83 ratio | Standard Deviation 0.013 |
| TAK-063 30 mg + [^11C]T-773 | Ratio of TAK-063 Metabolite Cmax to TAK-063 Cmax | 0.65 ratio | Standard Deviation 0.361 |
| TAK-063 100 mg + [^11C]T-773 | Ratio of TAK-063 Metabolite Cmax to TAK-063 Cmax | 0.99 ratio | Standard Deviation 0.145 |
| TAK-063 1000 mg + [^11C]T-773 | Ratio of TAK-063 Metabolite Cmax to TAK-063 Cmax | 0.55 ratio | Standard Deviation 0.001 |
Secondary
Ratio of TAK-063 Metabolite M-I AUC( 0-24) to TAK-063 AUC (0-24)
AUC Ratio is the ratio of AUC values of the metabolite compared to the parent calculated by dividing AUC values of metabolite M-I with those of the parent drug TAK-063.
Time frame: Pilot Cohort: Day 2 predose and at multiple time points (up to 24 hours) post-dose. Main Cohort: Day 1 predose and at multiple time points (up to 24 hours) post-dose.
Population: Pharmacokinetic Analysis Set
| Arm | Measure | Value (MEAN) | Dispersion |
|---|---|---|---|
| TAK-063 3 mg + [^11C]T-773 | Ratio of TAK-063 Metabolite M-I AUC( 0-24) to TAK-063 AUC (0-24) | 0.93 ratio | Standard Deviation 0.193 |
| TAK-063 10 mg | Ratio of TAK-063 Metabolite M-I AUC( 0-24) to TAK-063 AUC (0-24) | 0.75 ratio | Standard Deviation 0.064 |
| TAK-063 30 mg + [^11C]T-773 | Ratio of TAK-063 Metabolite M-I AUC( 0-24) to TAK-063 AUC (0-24) | 0.66 ratio | Standard Deviation 0.357 |
| TAK-063 100 mg + [^11C]T-773 | Ratio of TAK-063 Metabolite M-I AUC( 0-24) to TAK-063 AUC (0-24) | 0.89 ratio | Standard Deviation 0.199 |
| TAK-063 1000 mg + [^11C]T-773 | Ratio of TAK-063 Metabolite M-I AUC( 0-24) to TAK-063 AUC (0-24) | 0.54 ratio | Standard Deviation 0.072 |
Secondary
Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-063 and TAK-063 Metabolite M-I
Time to reach the maximum plasma concentration (Cmax), equal to time (hours) to Cmax.
Time frame: Pilot Cohort: Day 2 predose and at multiple time points (up to 24 hours) post-dose. Main Cohort: Day 1 predose and at multiple time points (up to 24 hours) post-dose.
Population: Pharmacokinetic Analysis Set
| Arm | Measure | Group | Value (MEAN) | Dispersion |
|---|---|---|---|---|
| TAK-063 3 mg + [^11C]T-773 | Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-063 and TAK-063 Metabolite M-I | TAK-063 | 1.25 hour | Standard Deviation 0.354 |
| TAK-063 3 mg + [^11C]T-773 | Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-063 and TAK-063 Metabolite M-I | TAK-063 Metabolite M-I | 1.50 hour | Standard Deviation 0 |
| TAK-063 10 mg | Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-063 and TAK-063 Metabolite M-I | TAK-063 | 2.99 hour | Standard Deviation 0.018 |
| TAK-063 10 mg | Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-063 and TAK-063 Metabolite M-I | TAK-063 Metabolite M-I | 2.99 hour | Standard Deviation 0.018 |
| TAK-063 30 mg + [^11C]T-773 | Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-063 and TAK-063 Metabolite M-I | TAK-063 Metabolite M-I | 1.64 hour | Standard Deviation 1.116 |
| TAK-063 30 mg + [^11C]T-773 | Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-063 and TAK-063 Metabolite M-I | TAK-063 | 1.33 hour | Standard Deviation 0.289 |
| TAK-063 100 mg + [^11C]T-773 | Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-063 and TAK-063 Metabolite M-I | TAK-063 | 2.33 hour | Standard Deviation 0.563 |
| TAK-063 100 mg + [^11C]T-773 | Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-063 and TAK-063 Metabolite M-I | TAK-063 Metabolite M-I | 2.00 hour | Standard Deviation 0 |
| TAK-063 1000 mg + [^11C]T-773 | Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-063 and TAK-063 Metabolite M-I | TAK-063 | 2.25 hour | Standard Deviation 1.137 |
| TAK-063 1000 mg + [^11C]T-773 | Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-063 and TAK-063 Metabolite M-I | TAK-063 Metabolite M-I | 2.79 hour | Standard Deviation 1.12 |