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Safety, Tolerability and Pharmacokinetic Study of Multiple Rising Doses of TAK- 063 in Participants With Stable Schizophrenia and Healthy Participants

A Phase 1, Randomized, Double-Blind, Placebo-Controlled, Safety, Tolerability and Pharmacokinetic Study of Multiple Rising Doses of TAK- 063 in Subjects With Stable Schizophrenia and Healthy Japanese Subjects

Status
Completed
Phases
Phase 1
Study type
Interventional
Source
ClinicalTrials.gov
Registry ID
NCT01879722
Enrollment
77
Registered
2013-06-18
Start date
2013-06-01
Completion date
2014-06-01
Last updated
2026-05-08

For informational purposes only — not medical advice. Sourced from public registries and may not reflect the latest updates. Terms

Conditions

Schizophrenia

Keywords

Drug therapy

Brief summary

The purpose of this study is to characterize the safety and tolerability of TAK-063 when administered as multiple oral doses at escalating dose levels in participants with stable schizophrenia and in healthy Japanese participants.

Detailed description

The drug being tested in this study is called TAK-063. TAK-063 is being tested to find a well-tolerated dose and also to treat schizophrenia. This study will look at how well different doses of TAK-063 are tolerated in healthy people of Japanese descent and in people with stable schizophrenia. Five dose levels will be examined, starting at the lowest, in each population with 10 participants in each dose level. These participants will be randomized to receive TAK-063 (8 subjects) and placebo (2 subjects) once daily (QD) for 7 days. In total, approximately 60 participants will be enrolled in the study. This trial will be conducted in single site in the United States. The overall time to participate in this study is up to 42 days. Participants will make 2 visits to the clinic, including 8-10 days confinement to the clinic, and will be contacted by telephone 7 days after last dose of study drug for a follow-up assessment. Dose escalation and the actual choice of the subsequent dose level will only occur following a review of the blinded data from the previous cohorts.

Interventions

DRUGTAK-063

TAK-063 tablets

DRUGTAK-063 Placebo

TAK-063 placebo-matching tablets

Sponsors

Takeda
Lead SponsorINDUSTRY

Study design

Allocation
RANDOMIZED
Intervention model
PARALLEL
Primary purpose
TREATMENT
Masking
QUADRUPLE (Subject, Caregiver, Investigator, Outcomes Assessor)

Eligibility

Sex/Gender
ALL
Age
18 Years to 55 Years
Healthy volunteers
Yes

Inclusion criteria

Healthy Participants: 1. Aged 20-55 years, inclusive, at the time of informed consent and first study medication dose. 2. Is a healthy adult male or female of Japanese descent (born to Japanese parents and grandparents and has lived outside of Japan for less than 5 years). 3. Weighs at least 45 kg and has a body mass index (BMI) between 18.0 and 28.0 kg/m\^2, inclusive, at Screening. Participants with Stable Schizophrenia: 1. Is aged 18 to 55 years, inclusive, at the time of informed consent and first study medication dose. 2. Is an adult male or female with a diagnosis of schizophrenia or schizoaffective disorder. 3. Weighs at least 45 kg and has a BMI between 18.0 and 35.0 kg/m\^2, inclusive at Screening. 4. Has been receiving a stable dose of antipsychotic monotherapy for at least 1 month prior to Screening. 5. Has not had an acute exacerbation of psychosis or been hospitalization for the treatment of schizophrenia or schizoaffective disorder for at least 3 months prior to Screening.

Exclusion criteria

All Participants: 1. Has uncontrolled, clinically significant neurologic, cardiovascular, pulmonary, hepatic, renal, metabolic, gastrointestinal, or endocrine disease or other abnormality (other than the disease being studied), which may impact the ability of the participant to participate or potentially confound the study results. 2. If female, the participant is pregnant or lactating or intending to become pregnant, or intending to donate ova, before, during the course of the study or within 12 weeks after last dose. 3. Intends to donate sperm during the course of this study or for 12 weeks after last dose. 4. 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. Healthy Participants: 1. Has a history or treatment of Axis I/II mental disorders according to Diagnostic and Statistical Manual of Mental Disorders, 4th Edition (DSM-IV) such as depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), autism spectrum disorders, anorexia nervosa, bulimia nervosa or schizophrenia within the past 3 years. 2. 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. Cotinine test is positive at Screening or Check-in (Day -1). Participants with Stable Schizophrenia: 1. Has a history of a primary DSM-IV axis I diagnosis other than schizophrenia or schizoaffective disorder. 2. Has not discontinued antipsychotic or other psychotropic medications or is unable to discontinue antipsychotic or other psychotropic medications at Day -7 (or five half-lives prior to Day -1). 3. Is taking a concomitant medication for a medical condition at a stable dose or regimen for less than two months or is taking a concomitant medication for a medical condition for less than two months and for which the discontinuation for the study period is not medically permissible.

Design outcomes

Primary

MeasureTime frameDescription
Percentage of Participants Who Experience at Least One Treatment-Emergent Adverse Event (TEAE) After 7 Days of DosingDay 1 to Day 14An 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 (TEAE) is defined as an adverse event with an onset that occurs after receiving study drug.
Percentage of Participants With Markedly Abnormal Safety Laboratory TestsDay 1 to Day 8The percentage of participants with any markedly abnormal standard safety laboratory values, including hematology, serum chemistries, and urinalysis, during the treatment period.
Percentage of Participants With Markedly Abnormal Vital Sign MeasurementsDay 1 to Day 8The percentage of participants who meet markedly abnormal criteria for vital signs, including oral body temperature, respiration rate, pulse, and resting blood pressure and after standing
Percentage of Participants With Markedly Abnormal Values of 12-Lead Electrocardiogram (ECG) ParametersDay 1 to Day 8The percentage of participants who meet markedly abnormal criteria specified by the protocol and statistical analysis plan during the treatment period.

Secondary

MeasureTime frameDescription
Cmax: Maximum Observed Plasma Concentration for TAK-063 and TAK-063 Metabolite M-IDays 1 and 7 pre-dose and multiple time-points post-dose (Up to 24 hours)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-IDays 1 and 7 pre-dose and multiple time-points post-dose (Up to 24 hours)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-IDays 1 and 7 pre-dose and multiple time-points post-dose (Up to 24 hours)AUC(0-tlqc) is a measure of total plasma exposure to the drug from time 0 to time of the Last Quantifiable Concentration.
AUC(0-24): Area Under the Plasma Concentration-Time Curve From Time 0 to 24 Hours Postdose for TAK-063 and TAK-063 Metabolite M-IDays 1 and 7 pre-dose and multiple time-points post-dose (Up to 24 hours)AUC(0-24) is a measure of total plasma exposure to the drug from Time 0 to 24 hours post-dose.
CL/F: Oral Clearance of TAK-063Days 1 and 7 pre-dose and multiple time-points post-dose (Up to 24 hours)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).
Average Plasma Concentration on Day 1 (Cav) and Day 7 (Cavss) for TAK-063 and TAK-063 Metabolite M-IDays 1 and 7 pre-dose and multiple time-points post-dose (Up to 24 hours)Cav is the Average plasma concentration on Day 1, calculated as AUC(0-24)/24 on Day 1. Cavss is the average plasma concentration on Day 7, calculated as AUC(0-24)/24 on Day 7.
Cmax Molar Ratio: Ratio of TAK-063 Metabolite Cmax to TAK-063 CmaxDays 1 and 7 pre-dose and multiple time-points post-dose (Up to 24 hours)Cmax Molar Ratio is the ratio of Cmax molar values of the metabolite compared to the parent calculated by dividing Cmax molar values of metabolite M-I with those of TAK-063.
AUC(0-24) Ratio: Ratio of TAK-063 Metabolite AUC(0-24) to TAK-063 AUC(0-24)Days 1 and 7 pre-dose and multiple time-points post-dose (Up to 24 hours)AUC(0-24) Ratio is the ratio of AUC(0-24) values of the metabolite compared to the parent calculated by dividing AUC(0-24) values of metabolite M-I with those of the parent drug TAK-063.
Accumulation Ratios Between Day 7 AUC(0-24) and Day 1 AUC(0-24)Days 1 and 7 pre-dose and multiple time-points post-dose (Up to 24 hours)Accumulation ratios between Day 7 AUC(0-24) and Day 1 AUC(0-24), (Day 7/Day 1). Estimated Ratio (Day 7/Day 1) is the exponentiated results of the difference between Day 7 and Day 1 in log-transformed values which resolves to the ratio of Day 7/Day 1 estimates.
Ae(0-24): Total Amount Excreted in the Urine From Time 0 to 24 Hours Postdose for TAK-063 and TAK-063 Metabolite M-IDays 1 and 7 pre-dose and multiple time-points post-dose (Up to 24 hours)Ae(0-24) is a measure of the total amount of study drug excreted in the urine from time 0 to 24 hours postdose.
Fe: Fraction of Drug Excreted in Urine for TAK-063Days 1 and 7 pre-dose and multiple time-points post-dose (Up to 24 hours)Fe is a measure of the fraction of drug excreted in urine and is calculated as Fe = (total amount excreted in the urine from time 0 to 24 hours post-dose / dose)×100
CLr: Renal Clearance of TAK-063 and TAK-063 Metabolite M-IDays 1 and 7 pre-dose and multiple time-points post-dose (Up to 24 hours)CLr is a measure of apparent clearance of the drug from the urine calculated as total amount excreted in the urine from time 0 to 24 hours postdose / plasma area under the curve from time 0 to 24 hours post-dose.

Countries

United States

Contacts

STUDY_DIRECTORMedical Director

Takeda Global Research & Development Center, Inc. (Note: This product was divested to Axsome in 2026)

Participant flow

Recruitment details

Participants took part in the study at 1 investigative site in the United States from 21 June 2013 (First participant signed consent) to 23 June 2014.

Pre-assignment details

Participants with a diagnosis of Schizophrenia were enrolled into 1 of 6 treatment groups, once a day placebo, 3 mg, 10 mg, 20 mg, 30 mg or 100 mg TAK-063. Healthy Japanese participants were enrolled in 1 of 4 treatment groups, once a day placebo, 3 mg, 10 mg or 20 mg TAK-063.

Participants by arm

ArmCount
TAK-063 3 mg (Schizophrenia Participants)
TAK-063 3 mg, tablets, orally, once daily for 7 days in participants with Schizophrenia
7
TAK-063 10 mg (Schizophrenia Participants)
TAK-063 10 mg, tablets, orally, once daily for 7 days in participants with Schizophrenia.
8
TAK-063 20 mg (Schizophrenia Participants)
TAK-063 20 mg, tablets, orally, once daily for 7 days in participants with Schizophrenia.
7
TAK-063 30 mg (Schizophrenia Participants)
TAK-063 30 mg, tablets, orally, once daily for 7 days in participants with Schizophrenia.
8
TAK-063 100 mg (Schizophrenia Participants)
TAK-063 100 mg, tablets, orally, once daily for 7 days in participants with Schizophrenia.
8
Placebo (Schizophrenia Participants)
Placebo matching TAK-063, tablets, orally, once daily for 7 days in participants with Schizophrenia.
9
TAK-063 3 mg (Healthy Participants)
TAK-063 3 mg, tablets, orally, once daily for 7 days in healthy Japanese participants.
8
TAK-063 10 mg (Healthy Participants)
TAK-063 10 mg, tablets, orally, once daily for 7 days in healthy Japanese participants.
8
TAK-063 20 mg (Healthy Participants)
TAK-063 20 mg, tablets, orally, once daily for 7 days in healthy Japanese participants.
8
Placebo (Healthy Participants)
Placebo matching TAK-063, tablets, orally, once daily for 7 days in healthy Japanese participants.
6
Total77

Baseline characteristics

CharacteristicTAK-063 10 mg (Schizophrenia Participants)TAK-063 20 mg (Schizophrenia Participants)TAK-063 30 mg (Schizophrenia Participants)TAK-063 100 mg (Schizophrenia Participants)Placebo (Schizophrenia Participants)TAK-063 3 mg (Healthy Participants)TAK-063 10 mg (Healthy Participants)TAK-063 20 mg (Healthy Participants)Placebo (Healthy Participants)TotalTAK-063 3 mg (Schizophrenia Participants)
Age, Continuous39.6 years
STANDARD_DEVIATION 9.9
44.6 years
STANDARD_DEVIATION 9
45.3 years
STANDARD_DEVIATION 8.19
39.4 years
STANDARD_DEVIATION 8.14
43.1 years
STANDARD_DEVIATION 11.34
36.3 years
STANDARD_DEVIATION 9.78
25.9 years
STANDARD_DEVIATION 9.51
34.6 years
STANDARD_DEVIATION 10.61
38.5 years
STANDARD_DEVIATION 11.52
39.0 years
STANDARD_DEVIATION 10.52
43.4 years
STANDARD_DEVIATION 4.2
Body Mass Index (BMI)26.98 kg/m^2
STANDARD_DEVIATION 3.476
27.93 kg/m^2
STANDARD_DEVIATION 5.488
32.16 kg/m^2
STANDARD_DEVIATION 4.243
27.76 kg/m^2
STANDARD_DEVIATION 4.46
28.80 kg/m^2
STANDARD_DEVIATION 5.71
24.75 kg/m^2
STANDARD_DEVIATION 1.962
22.65 kg/m^2
STANDARD_DEVIATION 2.556
24.14 kg/m^2
STANDARD_DEVIATION 1.984
22.23 kg/m^2
STANDARD_DEVIATION 2.778
26.93 kg/m^2
STANDARD_DEVIATION 4.812
31.13 kg/m^2
STANDARD_DEVIATION 3.266
Caffeine Consumption
No
0 participants2 participants3 participants6 participants1 participants5 participants4 participants2 participants3 participants30 participants4 participants
Caffeine Consumption
Yes
8 participants5 participants5 participants2 participants8 participants3 participants4 participants6 participants3 participants47 participants3 participants
Height166.8 cm
STANDARD_DEVIATION 7.89
172.6 cm
STANDARD_DEVIATION 9.61
166.3 cm
STANDARD_DEVIATION 7.7
173.9 cm
STANDARD_DEVIATION 8.82
173.3 cm
STANDARD_DEVIATION 10.95
172.5 cm
STANDARD_DEVIATION 10.35
170.5 cm
STANDARD_DEVIATION 7.21
171.8 cm
STANDARD_DEVIATION 7.46
168.8 cm
STANDARD_DEVIATION 6.49
171.0 cm
STANDARD_DEVIATION 8.44
172.1 cm
STANDARD_DEVIATION 9.19
Race/Ethnicity, Customized
Asian
0 participants1 participants0 participants0 participants0 participants8 participants8 participants8 participants6 participants31 participants0 participants
Race/Ethnicity, Customized
Black or African American
5 participants4 participants7 participants7 participants8 participants0 participants0 participants0 participants0 participants37 participants6 participants
Race/Ethnicity, Customized
Hispanic or Latino
1 participants0 participants0 participants1 participants1 participants0 participants0 participants0 participants0 participants4 participants1 participants
Race/Ethnicity, Customized
Multiracial
0 participants0 participants0 participants1 participants0 participants0 participants0 participants0 participants0 participants1 participants0 participants
Race/Ethnicity, Customized
Non-Hispanic or Latino
7 participants7 participants8 participants7 participants8 participants8 participants8 participants8 participants6 participants73 participants6 participants
Race/Ethnicity, Customized
White
3 participants2 participants1 participants0 participants1 participants0 participants0 participants0 participants0 participants8 participants1 participants
Region of Enrollment
United States
8 participants7 participants8 participants8 participants9 participants8 participants8 participants8 participants6 participants77 participants7 participants
Sex: Female, Male
Female
4 Participants1 Participants3 Participants1 Participants4 Participants2 Participants0 Participants0 Participants1 Participants19 Participants3 Participants
Sex: Female, Male
Male
4 Participants6 Participants5 Participants7 Participants5 Participants6 Participants8 Participants8 Participants5 Participants58 Participants4 Participants
Smoking Classification
Current smoker
7 participants6 participants5 participants7 participants8 participants0 participants0 participants0 participants0 participants38 participants5 participants
Smoking Classification
Ex-smoker
0 participants1 participants1 participants1 participants0 participants1 participants6 participants3 participants4 participants19 participants2 participants
Smoking Classification
Never smoked
1 participants0 participants2 participants0 participants1 participants7 participants2 participants5 participants2 participants20 participants0 participants
Weight74.75 kg
STANDARD_DEVIATION 8.543
83.76 kg
STANDARD_DEVIATION 19.701
88.83 kg
STANDARD_DEVIATION 12.805
83.51 kg
STANDARD_DEVIATION 11.853
86.46 kg
STANDARD_DEVIATION 17.422
73.98 kg
STANDARD_DEVIATION 10.503
67.45 kg
STANDARD_DEVIATION 8.128
70.19 kg
STANDARD_DEVIATION 6.879
63.50 kg
STANDARD_DEVIATION 10.037
78.70 kg
STANDARD_DEVIATION 14.666
92.09 kg
STANDARD_DEVIATION 10.138

Adverse events

Event typeEG000
affected / at risk
EG001
affected / at risk
EG002
affected / at risk
EG003
affected / at risk
EG004
affected / at risk
EG005
affected / at risk
EG006
affected / at risk
EG007
affected / at risk
EG008
affected / at risk
EG009
affected / at risk
other
Total, other adverse events
4 / 77 / 85 / 76 / 88 / 85 / 94 / 85 / 85 / 83 / 6
serious
Total, serious adverse events
0 / 70 / 80 / 70 / 80 / 80 / 90 / 80 / 80 / 80 / 6

Outcome results

Primary

Percentage of Participants Who Experience at Least One Treatment-Emergent Adverse Event (TEAE) After 7 Days of Dosing

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 (TEAE) is defined as an adverse event with an onset that occurs after receiving study drug.

Time frame: Day 1 to Day 14

Population: Safety population included all randomized participants who received at least one dose of study drug.

ArmMeasureValue (NUMBER)
TAK-063 3 mg (Schizophrenia Participants)Percentage of Participants Who Experience at Least One Treatment-Emergent Adverse Event (TEAE) After 7 Days of Dosing57.1 percentage of participants
TAK-063 10 mg (Schizophrenia Participants)Percentage of Participants Who Experience at Least One Treatment-Emergent Adverse Event (TEAE) After 7 Days of Dosing87.5 percentage of participants
TAK-063 20 mg (Schizophrenia Participants)Percentage of Participants Who Experience at Least One Treatment-Emergent Adverse Event (TEAE) After 7 Days of Dosing71.4 percentage of participants
TAK-063 30 mg (Schizophrenia Participants)Percentage of Participants Who Experience at Least One Treatment-Emergent Adverse Event (TEAE) After 7 Days of Dosing75.0 percentage of participants
TAK-063 100 mg (Schizophrenia Participants)Percentage of Participants Who Experience at Least One Treatment-Emergent Adverse Event (TEAE) After 7 Days of Dosing100.0 percentage of participants
Placebo (Schizophrenia Participants)Percentage of Participants Who Experience at Least One Treatment-Emergent Adverse Event (TEAE) After 7 Days of Dosing55.6 percentage of participants
TAK-063 3 mg (Healthy Participants)Percentage of Participants Who Experience at Least One Treatment-Emergent Adverse Event (TEAE) After 7 Days of Dosing50.0 percentage of participants
TAK-063 10 mg (Healthy Participants)Percentage of Participants Who Experience at Least One Treatment-Emergent Adverse Event (TEAE) After 7 Days of Dosing62.5 percentage of participants
TAK-063 20 mg (Healthy Participants)Percentage of Participants Who Experience at Least One Treatment-Emergent Adverse Event (TEAE) After 7 Days of Dosing62.5 percentage of participants
Placebo (Healthy Participants)Percentage of Participants Who Experience at Least One Treatment-Emergent Adverse Event (TEAE) After 7 Days of Dosing50.0 percentage of participants
Primary

Percentage of Participants With Markedly Abnormal Safety Laboratory Tests

The percentage of participants with any markedly abnormal standard safety laboratory values, including hematology, serum chemistries, and urinalysis, during the treatment period.

Time frame: Day 1 to Day 8

Population: Safety population included all randomized participants who received at least one dose of study drug.

ArmMeasureValue (NUMBER)
TAK-063 3 mg (Schizophrenia Participants)Percentage of Participants With Markedly Abnormal Safety Laboratory Tests0 percentage of participants
TAK-063 10 mg (Schizophrenia Participants)Percentage of Participants With Markedly Abnormal Safety Laboratory Tests0 percentage of participants
TAK-063 20 mg (Schizophrenia Participants)Percentage of Participants With Markedly Abnormal Safety Laboratory Tests0 percentage of participants
TAK-063 30 mg (Schizophrenia Participants)Percentage of Participants With Markedly Abnormal Safety Laboratory Tests0 percentage of participants
TAK-063 100 mg (Schizophrenia Participants)Percentage of Participants With Markedly Abnormal Safety Laboratory Tests0 percentage of participants
Placebo (Schizophrenia Participants)Percentage of Participants With Markedly Abnormal Safety Laboratory Tests0 percentage of participants
TAK-063 3 mg (Healthy Participants)Percentage of Participants With Markedly Abnormal Safety Laboratory Tests25.0 percentage of participants
TAK-063 10 mg (Healthy Participants)Percentage of Participants With Markedly Abnormal Safety Laboratory Tests0 percentage of participants
TAK-063 20 mg (Healthy Participants)Percentage of Participants With Markedly Abnormal Safety Laboratory Tests0 percentage of participants
Placebo (Healthy Participants)Percentage of Participants With Markedly Abnormal Safety Laboratory Tests0 percentage of participants
Primary

Percentage of Participants With Markedly Abnormal Values of 12-Lead Electrocardiogram (ECG) Parameters

The percentage of participants who meet markedly abnormal criteria specified by the protocol and statistical analysis plan during the treatment period.

Time frame: Day 1 to Day 8

Population: Safety population included all randomized participants who received at least one dose of study drug.

ArmMeasureValue (NUMBER)
TAK-063 3 mg (Schizophrenia Participants)Percentage of Participants With Markedly Abnormal Values of 12-Lead Electrocardiogram (ECG) Parameters57.1 percentage of participants
TAK-063 10 mg (Schizophrenia Participants)Percentage of Participants With Markedly Abnormal Values of 12-Lead Electrocardiogram (ECG) Parameters50.0 percentage of participants
TAK-063 20 mg (Schizophrenia Participants)Percentage of Participants With Markedly Abnormal Values of 12-Lead Electrocardiogram (ECG) Parameters57.1 percentage of participants
TAK-063 30 mg (Schizophrenia Participants)Percentage of Participants With Markedly Abnormal Values of 12-Lead Electrocardiogram (ECG) Parameters75.0 percentage of participants
TAK-063 100 mg (Schizophrenia Participants)Percentage of Participants With Markedly Abnormal Values of 12-Lead Electrocardiogram (ECG) Parameters62.5 percentage of participants
Placebo (Schizophrenia Participants)Percentage of Participants With Markedly Abnormal Values of 12-Lead Electrocardiogram (ECG) Parameters44.4 percentage of participants
TAK-063 3 mg (Healthy Participants)Percentage of Participants With Markedly Abnormal Values of 12-Lead Electrocardiogram (ECG) Parameters50.0 percentage of participants
TAK-063 10 mg (Healthy Participants)Percentage of Participants With Markedly Abnormal Values of 12-Lead Electrocardiogram (ECG) Parameters75.0 percentage of participants
TAK-063 20 mg (Healthy Participants)Percentage of Participants With Markedly Abnormal Values of 12-Lead Electrocardiogram (ECG) Parameters50.0 percentage of participants
Placebo (Healthy Participants)Percentage of Participants With Markedly Abnormal Values of 12-Lead Electrocardiogram (ECG) Parameters33.3 percentage of participants
Primary

Percentage of Participants With Markedly Abnormal Vital Sign Measurements

The percentage of participants who meet markedly abnormal criteria for vital signs, including oral body temperature, respiration rate, pulse, and resting blood pressure and after standing

Time frame: Day 1 to Day 8

Population: Safety population included all randomized participants who received at least one dose of study drug.

ArmMeasureValue (NUMBER)
TAK-063 3 mg (Schizophrenia Participants)Percentage of Participants With Markedly Abnormal Vital Sign Measurements71.4 percentage of participants
TAK-063 10 mg (Schizophrenia Participants)Percentage of Participants With Markedly Abnormal Vital Sign Measurements100.0 percentage of participants
TAK-063 20 mg (Schizophrenia Participants)Percentage of Participants With Markedly Abnormal Vital Sign Measurements100.0 percentage of participants
TAK-063 30 mg (Schizophrenia Participants)Percentage of Participants With Markedly Abnormal Vital Sign Measurements100.0 percentage of participants
TAK-063 100 mg (Schizophrenia Participants)Percentage of Participants With Markedly Abnormal Vital Sign Measurements100.0 percentage of participants
Placebo (Schizophrenia Participants)Percentage of Participants With Markedly Abnormal Vital Sign Measurements100.0 percentage of participants
TAK-063 3 mg (Healthy Participants)Percentage of Participants With Markedly Abnormal Vital Sign Measurements100.0 percentage of participants
TAK-063 10 mg (Healthy Participants)Percentage of Participants With Markedly Abnormal Vital Sign Measurements100.0 percentage of participants
TAK-063 20 mg (Healthy Participants)Percentage of Participants With Markedly Abnormal Vital Sign Measurements100.0 percentage of participants
Placebo (Healthy Participants)Percentage of Participants With Markedly Abnormal Vital Sign Measurements100.0 percentage of participants
Secondary

Accumulation Ratios Between Day 7 AUC(0-24) and Day 1 AUC(0-24)

Accumulation ratios between Day 7 AUC(0-24) and Day 1 AUC(0-24), (Day 7/Day 1). Estimated Ratio (Day 7/Day 1) is the exponentiated results of the difference between Day 7 and Day 1 in log-transformed values which resolves to the ratio of Day 7/Day 1 estimates.

Time frame: Days 1 and 7 pre-dose and multiple time-points post-dose (Up to 24 hours)

Population: PK Set included all randomized participants who received study drug for whom PK data was available for analysis.

ArmMeasureGroupValue (MEAN)Dispersion
TAK-063 3 mg (Schizophrenia Participants)Accumulation Ratios Between Day 7 AUC(0-24) and Day 1 AUC(0-24)TAK-0631.8 ratio90% Confidence Interval 0.55
TAK-063 3 mg (Schizophrenia Participants)Accumulation Ratios Between Day 7 AUC(0-24) and Day 1 AUC(0-24)TAK-063 M-I2.0 ratio90% Confidence Interval 0.619
TAK-063 10 mg (Schizophrenia Participants)Accumulation Ratios Between Day 7 AUC(0-24) and Day 1 AUC(0-24)TAK-0631.1 ratio90% Confidence Interval 0.21
TAK-063 10 mg (Schizophrenia Participants)Accumulation Ratios Between Day 7 AUC(0-24) and Day 1 AUC(0-24)TAK-063 M-I1.2 ratio90% Confidence Interval 0.308
TAK-063 20 mg (Schizophrenia Participants)Accumulation Ratios Between Day 7 AUC(0-24) and Day 1 AUC(0-24)TAK-0631.4 ratio90% Confidence Interval 0.325
TAK-063 20 mg (Schizophrenia Participants)Accumulation Ratios Between Day 7 AUC(0-24) and Day 1 AUC(0-24)TAK-063 M-I1.4 ratio90% Confidence Interval 0.371
TAK-063 30 mg (Schizophrenia Participants)Accumulation Ratios Between Day 7 AUC(0-24) and Day 1 AUC(0-24)TAK-0631.3 ratio90% Confidence Interval 0.126
TAK-063 30 mg (Schizophrenia Participants)Accumulation Ratios Between Day 7 AUC(0-24) and Day 1 AUC(0-24)TAK-063 M-I1.3 ratio90% Confidence Interval 0.183
TAK-063 100 mg (Schizophrenia Participants)Accumulation Ratios Between Day 7 AUC(0-24) and Day 1 AUC(0-24)TAK-0631.2 ratio90% Confidence Interval 0.324
TAK-063 100 mg (Schizophrenia Participants)Accumulation Ratios Between Day 7 AUC(0-24) and Day 1 AUC(0-24)TAK-063 M-I1.1 ratio90% Confidence Interval 0.243
Placebo (Schizophrenia Participants)Accumulation Ratios Between Day 7 AUC(0-24) and Day 1 AUC(0-24)TAK-0632.0 ratio90% Confidence Interval 0.472
Placebo (Schizophrenia Participants)Accumulation Ratios Between Day 7 AUC(0-24) and Day 1 AUC(0-24)TAK-063 M-I2.1 ratio90% Confidence Interval 0.408
TAK-063 3 mg (Healthy Participants)Accumulation Ratios Between Day 7 AUC(0-24) and Day 1 AUC(0-24)TAK-063 M-I1.1 ratio90% Confidence Interval 0.158
TAK-063 3 mg (Healthy Participants)Accumulation Ratios Between Day 7 AUC(0-24) and Day 1 AUC(0-24)TAK-0631.1 ratio90% Confidence Interval 0.169
TAK-063 10 mg (Healthy Participants)Accumulation Ratios Between Day 7 AUC(0-24) and Day 1 AUC(0-24)TAK-0631.2 ratio90% Confidence Interval 0.18
TAK-063 10 mg (Healthy Participants)Accumulation Ratios Between Day 7 AUC(0-24) and Day 1 AUC(0-24)TAK-063 M-I1.1 ratio90% Confidence Interval 0.226
Secondary

Ae(0-24): Total Amount Excreted in the Urine From Time 0 to 24 Hours Postdose for TAK-063 and TAK-063 Metabolite M-I

Ae(0-24) is a measure of the total amount of study drug excreted in the urine from time 0 to 24 hours postdose.

Time frame: Days 1 and 7 pre-dose and multiple time-points post-dose (Up to 24 hours)

Population: PK Set included all randomized participants who received study drug for whom PK data was available for analysis.

ArmMeasureGroupValue (MEAN)Dispersion
TAK-063 3 mg (Schizophrenia Participants)Ae(0-24): Total Amount Excreted in the Urine From Time 0 to 24 Hours Postdose for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 10.0 ngStandard Deviation 0
TAK-063 3 mg (Schizophrenia Participants)Ae(0-24): Total Amount Excreted in the Urine From Time 0 to 24 Hours Postdose for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 10.0 ngStandard Deviation 0
TAK-063 3 mg (Schizophrenia Participants)Ae(0-24): Total Amount Excreted in the Urine From Time 0 to 24 Hours Postdose for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)0.0 ngStandard Deviation 0
TAK-063 3 mg (Schizophrenia Participants)Ae(0-24): Total Amount Excreted in the Urine From Time 0 to 24 Hours Postdose for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)630.2 ngStandard Deviation 1129.4
TAK-063 10 mg (Schizophrenia Participants)Ae(0-24): Total Amount Excreted in the Urine From Time 0 to 24 Hours Postdose for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)11708.6 ngStandard Deviation 7047.1
TAK-063 10 mg (Schizophrenia Participants)Ae(0-24): Total Amount Excreted in the Urine From Time 0 to 24 Hours Postdose for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 19099.4 ngStandard Deviation 3451
TAK-063 10 mg (Schizophrenia Participants)Ae(0-24): Total Amount Excreted in the Urine From Time 0 to 24 Hours Postdose for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 13642.3 ngStandard Deviation 2611.9
TAK-063 10 mg (Schizophrenia Participants)Ae(0-24): Total Amount Excreted in the Urine From Time 0 to 24 Hours Postdose for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)4430.9 ngStandard Deviation 2831.5
TAK-063 20 mg (Schizophrenia Participants)Ae(0-24): Total Amount Excreted in the Urine From Time 0 to 24 Hours Postdose for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 14432.8 ngStandard Deviation 3418.6
TAK-063 20 mg (Schizophrenia Participants)Ae(0-24): Total Amount Excreted in the Urine From Time 0 to 24 Hours Postdose for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)25327.7 ngStandard Deviation 12723.6
TAK-063 20 mg (Schizophrenia Participants)Ae(0-24): Total Amount Excreted in the Urine From Time 0 to 24 Hours Postdose for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 116879.5 ngStandard Deviation 8061.5
TAK-063 20 mg (Schizophrenia Participants)Ae(0-24): Total Amount Excreted in the Urine From Time 0 to 24 Hours Postdose for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)7979.2 ngStandard Deviation 4739
TAK-063 30 mg (Schizophrenia Participants)Ae(0-24): Total Amount Excreted in the Urine From Time 0 to 24 Hours Postdose for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 19952.1 ngStandard Deviation 6025.2
TAK-063 30 mg (Schizophrenia Participants)Ae(0-24): Total Amount Excreted in the Urine From Time 0 to 24 Hours Postdose for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 124302.0 ngStandard Deviation 12756.6
TAK-063 30 mg (Schizophrenia Participants)Ae(0-24): Total Amount Excreted in the Urine From Time 0 to 24 Hours Postdose for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)15066.0 ngStandard Deviation 9996.7
TAK-063 30 mg (Schizophrenia Participants)Ae(0-24): Total Amount Excreted in the Urine From Time 0 to 24 Hours Postdose for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)35462.0 ngStandard Deviation 11737.9
TAK-063 100 mg (Schizophrenia Participants)Ae(0-24): Total Amount Excreted in the Urine From Time 0 to 24 Hours Postdose for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)67767.6 ngStandard Deviation 36686.1
TAK-063 100 mg (Schizophrenia Participants)Ae(0-24): Total Amount Excreted in the Urine From Time 0 to 24 Hours Postdose for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)35527.5 ngStandard Deviation 20919.1
TAK-063 100 mg (Schizophrenia Participants)Ae(0-24): Total Amount Excreted in the Urine From Time 0 to 24 Hours Postdose for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 152682.9 ngStandard Deviation 14870.1
TAK-063 100 mg (Schizophrenia Participants)Ae(0-24): Total Amount Excreted in the Urine From Time 0 to 24 Hours Postdose for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 134893.4 ngStandard Deviation 27402.5
Placebo (Schizophrenia Participants)Ae(0-24): Total Amount Excreted in the Urine From Time 0 to 24 Hours Postdose for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)1024.2 ngStandard Deviation 1665.5
Placebo (Schizophrenia Participants)Ae(0-24): Total Amount Excreted in the Urine From Time 0 to 24 Hours Postdose for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)0.0 ngStandard Deviation 0
Placebo (Schizophrenia Participants)Ae(0-24): Total Amount Excreted in the Urine From Time 0 to 24 Hours Postdose for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 10.0 ngStandard Deviation 0
Placebo (Schizophrenia Participants)Ae(0-24): Total Amount Excreted in the Urine From Time 0 to 24 Hours Postdose for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 10.0 ngStandard Deviation 0
TAK-063 3 mg (Healthy Participants)Ae(0-24): Total Amount Excreted in the Urine From Time 0 to 24 Hours Postdose for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)14139.9 ngStandard Deviation 8205.9
TAK-063 3 mg (Healthy Participants)Ae(0-24): Total Amount Excreted in the Urine From Time 0 to 24 Hours Postdose for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 13592.0 ngStandard Deviation 4936.1
TAK-063 3 mg (Healthy Participants)Ae(0-24): Total Amount Excreted in the Urine From Time 0 to 24 Hours Postdose for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)4765.2 ngStandard Deviation 3491
TAK-063 3 mg (Healthy Participants)Ae(0-24): Total Amount Excreted in the Urine From Time 0 to 24 Hours Postdose for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 110487.8 ngStandard Deviation 5847.3
TAK-063 10 mg (Healthy Participants)Ae(0-24): Total Amount Excreted in the Urine From Time 0 to 24 Hours Postdose for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 126557.0 ngStandard Deviation 11839.7
TAK-063 10 mg (Healthy Participants)Ae(0-24): Total Amount Excreted in the Urine From Time 0 to 24 Hours Postdose for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)15913.7 ngStandard Deviation 9619.6
TAK-063 10 mg (Healthy Participants)Ae(0-24): Total Amount Excreted in the Urine From Time 0 to 24 Hours Postdose for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)35341.3 ngStandard Deviation 12664.4
TAK-063 10 mg (Healthy Participants)Ae(0-24): Total Amount Excreted in the Urine From Time 0 to 24 Hours Postdose for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 114145.4 ngStandard Deviation 9576.1
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: Days 1 and 7 pre-dose and multiple time-points post-dose (Up to 24 hours)

Population: PK Set included all randomized participants who received study drug for whom PK data was available for analysis.

ArmMeasureGroupValue (MEAN)Dispersion
TAK-063 3 mg (Schizophrenia Participants)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-ITAK-063 Day 1159.0 ng*hr/mLStandard Deviation 60
TAK-063 3 mg (Schizophrenia Participants)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-ITAK-063 M-I Day 1114.0 ng*hr/mLStandard Deviation 49.1
TAK-063 3 mg (Schizophrenia Participants)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-ITAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)280.6 ng*hr/mLStandard Deviation 60.5
TAK-063 3 mg (Schizophrenia Participants)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-ITAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)218.7 ng*hr/mLStandard Deviation 57
TAK-063 10 mg (Schizophrenia Participants)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-ITAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)786.0 ng*hr/mLStandard Deviation 296.4
TAK-063 10 mg (Schizophrenia Participants)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-ITAK-063 M-I Day 1682.5 ng*hr/mLStandard Deviation 269
TAK-063 10 mg (Schizophrenia Participants)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-ITAK-063 Day 1623.2 ng*hr/mLStandard Deviation 141
TAK-063 10 mg (Schizophrenia Participants)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-ITAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)680.1 ng*hr/mLStandard Deviation 153.3
TAK-063 20 mg (Schizophrenia Participants)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-ITAK-063 Day 1939.3 ng*hr/mLStandard Deviation 402
TAK-063 20 mg (Schizophrenia Participants)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-ITAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)1387.2 ng*hr/mLStandard Deviation 681
TAK-063 20 mg (Schizophrenia Participants)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-ITAK-063 M-I Day 11011.0 ng*hr/mLStandard Deviation 517.9
TAK-063 20 mg (Schizophrenia Participants)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-ITAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)1240.9 ng*hr/mLStandard Deviation 385.4
TAK-063 30 mg (Schizophrenia Participants)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-ITAK-063 Day 11619.0 ng*hr/mLStandard Deviation 393.3
TAK-063 30 mg (Schizophrenia Participants)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-ITAK-063 M-I Day 11070.8 ng*hr/mLStandard Deviation 120.7
TAK-063 30 mg (Schizophrenia Participants)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-ITAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)2030.9 ng*hr/mLStandard Deviation 479.2
TAK-063 30 mg (Schizophrenia Participants)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-ITAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)1371.2 ng*hr/mLStandard Deviation 291.8
TAK-063 100 mg (Schizophrenia Participants)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-ITAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)1598.4 ng*hr/mLStandard Deviation 289.1
TAK-063 100 mg (Schizophrenia Participants)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-ITAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)2764.0 ng*hr/mLStandard Deviation 712.1
TAK-063 100 mg (Schizophrenia Participants)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-ITAK-063 M-I Day 11483.6 ng*hr/mLStandard Deviation 405.8
TAK-063 100 mg (Schizophrenia Participants)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-ITAK-063 Day 12503.2 ng*hr/mLStandard Deviation 1146.4
Placebo (Schizophrenia Participants)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-ITAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)156.7 ng*hr/mLStandard Deviation 37.3
Placebo (Schizophrenia Participants)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-ITAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)295.6 ng*hr/mLStandard Deviation 83.5
Placebo (Schizophrenia Participants)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-ITAK-063 M-I Day 174.8 ng*hr/mLStandard Deviation 19.2
Placebo (Schizophrenia Participants)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-ITAK-063 Day 1148.6 ng*hr/mLStandard Deviation 54.9
TAK-063 3 mg (Healthy Participants)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-ITAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)378.5 ng*hr/mLStandard Deviation 51.6
TAK-063 3 mg (Healthy Participants)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-ITAK-063 Day 1651.9 ng*hr/mLStandard Deviation 73.3
TAK-063 3 mg (Healthy Participants)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-ITAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)736.1 ng*hr/mLStandard Deviation 90.6
TAK-063 3 mg (Healthy Participants)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-ITAK-063 M-I Day 1327.9 ng*hr/mLStandard Deviation 37.5
TAK-063 10 mg (Healthy Participants)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-ITAK-063 M-I Day 1667.3 ng*hr/mLStandard Deviation 149.1
TAK-063 10 mg (Healthy Participants)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-ITAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)1536.4 ng*hr/mLStandard Deviation 236.2
TAK-063 10 mg (Healthy Participants)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-ITAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)806.3 ng*hr/mLStandard Deviation 174.1
TAK-063 10 mg (Healthy Participants)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-ITAK-063 Day 11243.9 ng*hr/mLStandard Deviation 276
Secondary

AUC(0-24) Ratio: Ratio of TAK-063 Metabolite AUC(0-24) to TAK-063 AUC(0-24)

AUC(0-24) Ratio is the ratio of AUC(0-24) values of the metabolite compared to the parent calculated by dividing AUC(0-24) values of metabolite M-I with those of the parent drug TAK-063.

Time frame: Days 1 and 7 pre-dose and multiple time-points post-dose (Up to 24 hours)

Population: PK Set included all randomized participants who received study drug for whom PK data was available for analysis.

ArmMeasureGroupValue (MEAN)Dispersion
TAK-063 3 mg (Schizophrenia Participants)AUC(0-24) Ratio: Ratio of TAK-063 Metabolite AUC(0-24) to TAK-063 AUC(0-24)TAK-063 M-I Day 10.7 ratioStandard Deviation 0.1
TAK-063 3 mg (Schizophrenia Participants)AUC(0-24) Ratio: Ratio of TAK-063 Metabolite AUC(0-24) to TAK-063 AUC(0-24)TAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)0.8 ratioStandard Deviation 0.2
TAK-063 10 mg (Schizophrenia Participants)AUC(0-24) Ratio: Ratio of TAK-063 Metabolite AUC(0-24) to TAK-063 AUC(0-24)TAK-063 M-I Day 11.0 ratioStandard Deviation 0.3
TAK-063 10 mg (Schizophrenia Participants)AUC(0-24) Ratio: Ratio of TAK-063 Metabolite AUC(0-24) to TAK-063 AUC(0-24)TAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)1.1 ratioStandard Deviation 0.3
TAK-063 20 mg (Schizophrenia Participants)AUC(0-24) Ratio: Ratio of TAK-063 Metabolite AUC(0-24) to TAK-063 AUC(0-24)TAK-063 M-I Day 11.0 ratioStandard Deviation 0.2
TAK-063 20 mg (Schizophrenia Participants)AUC(0-24) Ratio: Ratio of TAK-063 Metabolite AUC(0-24) to TAK-063 AUC(0-24)TAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)1.1 ratioStandard Deviation 0.2
TAK-063 30 mg (Schizophrenia Participants)AUC(0-24) Ratio: Ratio of TAK-063 Metabolite AUC(0-24) to TAK-063 AUC(0-24)TAK-063 M-I Day 10.7 ratioStandard Deviation 0.1
TAK-063 30 mg (Schizophrenia Participants)AUC(0-24) Ratio: Ratio of TAK-063 Metabolite AUC(0-24) to TAK-063 AUC(0-24)TAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)0.7 ratioStandard Deviation 0.1
TAK-063 100 mg (Schizophrenia Participants)AUC(0-24) Ratio: Ratio of TAK-063 Metabolite AUC(0-24) to TAK-063 AUC(0-24)TAK-063 M-I Day 10.6 ratioStandard Deviation 0.2
TAK-063 100 mg (Schizophrenia Participants)AUC(0-24) Ratio: Ratio of TAK-063 Metabolite AUC(0-24) to TAK-063 AUC(0-24)TAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)0.6 ratioStandard Deviation 0.1
Placebo (Schizophrenia Participants)AUC(0-24) Ratio: Ratio of TAK-063 Metabolite AUC(0-24) to TAK-063 AUC(0-24)TAK-063 M-I Day 10.5 ratioStandard Deviation 0.1
Placebo (Schizophrenia Participants)AUC(0-24) Ratio: Ratio of TAK-063 Metabolite AUC(0-24) to TAK-063 AUC(0-24)TAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)0.5 ratioStandard Deviation 0.04
TAK-063 3 mg (Healthy Participants)AUC(0-24) Ratio: Ratio of TAK-063 Metabolite AUC(0-24) to TAK-063 AUC(0-24)TAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)0.5 ratioStandard Deviation 0.1
TAK-063 3 mg (Healthy Participants)AUC(0-24) Ratio: Ratio of TAK-063 Metabolite AUC(0-24) to TAK-063 AUC(0-24)TAK-063 M-I Day 10.5 ratioStandard Deviation 0.1
TAK-063 10 mg (Healthy Participants)AUC(0-24) Ratio: Ratio of TAK-063 Metabolite AUC(0-24) to TAK-063 AUC(0-24)TAK-063 M-I Day 10.5 ratioStandard Deviation 0.1
TAK-063 10 mg (Healthy Participants)AUC(0-24) Ratio: Ratio of TAK-063 Metabolite AUC(0-24) to TAK-063 AUC(0-24)TAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)0.5 ratioStandard Deviation 0.1
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.

Time frame: Days 1 and 7 pre-dose and multiple time-points post-dose (Up to 24 hours)

Population: PK Set included all randomized participants who received study drug for whom PK data was available for analysis.

ArmMeasureGroupValue (MEAN)Dispersion
TAK-063 3 mg (Schizophrenia Participants)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-ITAK-063 Day 1158.8 ng*hr/mLStandard Deviation 59.8
TAK-063 3 mg (Schizophrenia Participants)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-ITAK-063 M-I Day 1113.9 ng*hr/mLStandard Deviation 48.9
TAK-063 3 mg (Schizophrenia Participants)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-ITAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)280.8 ng*hr/mLStandard Deviation 60.4
TAK-063 3 mg (Schizophrenia Participants)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-ITAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)218.9 ng*hr/mLStandard Deviation 56.9
TAK-063 10 mg (Schizophrenia Participants)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-ITAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)786.3 ng*hr/mLStandard Deviation 296.6
TAK-063 10 mg (Schizophrenia Participants)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-ITAK-063 M-I Day 1681.8 ng*hr/mLStandard Deviation 268.9
TAK-063 10 mg (Schizophrenia Participants)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-ITAK-063 Day 1622.7 ng*hr/mLStandard Deviation 140.9
TAK-063 10 mg (Schizophrenia Participants)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-ITAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)680.3 ng*hr/mLStandard Deviation 153.4
TAK-063 20 mg (Schizophrenia Participants)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-ITAK-063 Day 1938.3 ng*hr/mLStandard Deviation 401
TAK-063 20 mg (Schizophrenia Participants)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-ITAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)1387.2 ng*hr/mLStandard Deviation 681
TAK-063 20 mg (Schizophrenia Participants)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-ITAK-063 M-I Day 11009.6 ng*hr/mLStandard Deviation 516.5
TAK-063 20 mg (Schizophrenia Participants)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-ITAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)1240.9 ng*hr/mLStandard Deviation 385.4
TAK-063 30 mg (Schizophrenia Participants)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-ITAK-063 Day 11616.6 ng*hr/mLStandard Deviation 392.1
TAK-063 30 mg (Schizophrenia Participants)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-ITAK-063 M-I Day 11069.1 ng*hr/mLStandard Deviation 120.2
TAK-063 30 mg (Schizophrenia Participants)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-ITAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)2030.9 ng*hr/mLStandard Deviation 479.2
TAK-063 30 mg (Schizophrenia Participants)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-ITAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)1371.2 ng*hr/mLStandard Deviation 291.8
TAK-063 100 mg (Schizophrenia Participants)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-ITAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)1598.8 ng*hr/mLStandard Deviation 288.7
TAK-063 100 mg (Schizophrenia Participants)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-ITAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)2764.5 ng*hr/mLStandard Deviation 711.4
TAK-063 100 mg (Schizophrenia Participants)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-ITAK-063 M-I Day 11481.1 ng*hr/mLStandard Deviation 404.5
TAK-063 100 mg (Schizophrenia Participants)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-ITAK-063 Day 12499.3 ng*hr/mLStandard Deviation 1143.3
Placebo (Schizophrenia Participants)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-ITAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)156.7 ng*hr/mLStandard Deviation 37.3
Placebo (Schizophrenia Participants)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-ITAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)295.6 ng*hr/mLStandard Deviation 83.5
Placebo (Schizophrenia Participants)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-ITAK-063 M-I Day 174.7 ng*hr/mLStandard Deviation 19.1
Placebo (Schizophrenia Participants)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-ITAK-063 Day 1148.3 ng*hr/mLStandard Deviation 54.8
TAK-063 3 mg (Healthy Participants)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-ITAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)378.5 ng*hr/mLStandard Deviation 51.6
TAK-063 3 mg (Healthy Participants)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-ITAK-063 Day 1651.3 ng*hr/mLStandard Deviation 73.2
TAK-063 3 mg (Healthy Participants)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-ITAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)736.1 ng*hr/mLStandard Deviation 90.7
TAK-063 3 mg (Healthy Participants)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-ITAK-063 M-I Day 1327.6 ng*hr/mLStandard Deviation 37.4
TAK-063 10 mg (Healthy Participants)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-ITAK-063 M-I Day 1666.3 ng*hr/mLStandard Deviation 148.8
TAK-063 10 mg (Healthy Participants)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-ITAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)1536.7 ng*hr/mLStandard Deviation 236.7
TAK-063 10 mg (Healthy Participants)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-ITAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)806.5 ng*hr/mLStandard Deviation 174.3
TAK-063 10 mg (Healthy Participants)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-ITAK-063 Day 11242.3 ng*hr/mLStandard Deviation 275.4
Secondary

Average Plasma Concentration on Day 1 (Cav) and Day 7 (Cavss) for TAK-063 and TAK-063 Metabolite M-I

Cav is the Average plasma concentration on Day 1, calculated as AUC(0-24)/24 on Day 1. Cavss is the average plasma concentration on Day 7, calculated as AUC(0-24)/24 on Day 7.

Time frame: Days 1 and 7 pre-dose and multiple time-points post-dose (Up to 24 hours)

Population: PK Set included all randomized participants for whom PK data was available for analysis.

ArmMeasureGroupValue (MEAN)Dispersion
TAK-063 3 mg (Schizophrenia Participants)Average Plasma Concentration on Day 1 (Cav) and Day 7 (Cavss) for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 16.6 ng/mLStandard Deviation 2.5
TAK-063 3 mg (Schizophrenia Participants)Average Plasma Concentration on Day 1 (Cav) and Day 7 (Cavss) for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 14.8 ng/mLStandard Deviation 2
TAK-063 3 mg (Schizophrenia Participants)Average Plasma Concentration on Day 1 (Cav) and Day 7 (Cavss) for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)11.7 ng/mLStandard Deviation 2.5
TAK-063 3 mg (Schizophrenia Participants)Average Plasma Concentration on Day 1 (Cav) and Day 7 (Cavss) for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)9.1 ng/mLStandard Deviation 2.4
TAK-063 10 mg (Schizophrenia Participants)Average Plasma Concentration on Day 1 (Cav) and Day 7 (Cavss) for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)32.8 ng/mLStandard Deviation 12.4
TAK-063 10 mg (Schizophrenia Participants)Average Plasma Concentration on Day 1 (Cav) and Day 7 (Cavss) for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 128.4 ng/mLStandard Deviation 11.2
TAK-063 10 mg (Schizophrenia Participants)Average Plasma Concentration on Day 1 (Cav) and Day 7 (Cavss) for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 126.0 ng/mLStandard Deviation 5.9
TAK-063 10 mg (Schizophrenia Participants)Average Plasma Concentration on Day 1 (Cav) and Day 7 (Cavss) for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)28.3 ng/mLStandard Deviation 6.4
TAK-063 20 mg (Schizophrenia Participants)Average Plasma Concentration on Day 1 (Cav) and Day 7 (Cavss) for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 139.1 ng/mLStandard Deviation 16.8
TAK-063 20 mg (Schizophrenia Participants)Average Plasma Concentration on Day 1 (Cav) and Day 7 (Cavss) for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)57.8 ng/mLStandard Deviation 28.4
TAK-063 20 mg (Schizophrenia Participants)Average Plasma Concentration on Day 1 (Cav) and Day 7 (Cavss) for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 142.1 ng/mLStandard Deviation 21.6
TAK-063 20 mg (Schizophrenia Participants)Average Plasma Concentration on Day 1 (Cav) and Day 7 (Cavss) for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)51.7 ng/mLStandard Deviation 16.1
TAK-063 30 mg (Schizophrenia Participants)Average Plasma Concentration on Day 1 (Cav) and Day 7 (Cavss) for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 167.5 ng/mLStandard Deviation 16.4
TAK-063 30 mg (Schizophrenia Participants)Average Plasma Concentration on Day 1 (Cav) and Day 7 (Cavss) for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 144.6 ng/mLStandard Deviation 5
TAK-063 30 mg (Schizophrenia Participants)Average Plasma Concentration on Day 1 (Cav) and Day 7 (Cavss) for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)84.6 ng/mLStandard Deviation 20
TAK-063 30 mg (Schizophrenia Participants)Average Plasma Concentration on Day 1 (Cav) and Day 7 (Cavss) for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)57.1 ng/mLStandard Deviation 12.2
TAK-063 100 mg (Schizophrenia Participants)Average Plasma Concentration on Day 1 (Cav) and Day 7 (Cavss) for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)66.6 ng/mLStandard Deviation 12
TAK-063 100 mg (Schizophrenia Participants)Average Plasma Concentration on Day 1 (Cav) and Day 7 (Cavss) for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)115.2 ng/mLStandard Deviation 29.7
TAK-063 100 mg (Schizophrenia Participants)Average Plasma Concentration on Day 1 (Cav) and Day 7 (Cavss) for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 161.8 ng/mLStandard Deviation 16.9
TAK-063 100 mg (Schizophrenia Participants)Average Plasma Concentration on Day 1 (Cav) and Day 7 (Cavss) for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 1104.3 ng/mLStandard Deviation 47.8
Placebo (Schizophrenia Participants)Average Plasma Concentration on Day 1 (Cav) and Day 7 (Cavss) for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)6.5 ng/mLStandard Deviation 1.6
Placebo (Schizophrenia Participants)Average Plasma Concentration on Day 1 (Cav) and Day 7 (Cavss) for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)12.3 ng/mLStandard Deviation 3.5
Placebo (Schizophrenia Participants)Average Plasma Concentration on Day 1 (Cav) and Day 7 (Cavss) for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 13.1 ng/mLStandard Deviation 0.8
Placebo (Schizophrenia Participants)Average Plasma Concentration on Day 1 (Cav) and Day 7 (Cavss) for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 16.2 ng/mLStandard Deviation 2.3
TAK-063 3 mg (Healthy Participants)Average Plasma Concentration on Day 1 (Cav) and Day 7 (Cavss) for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)15.8 ng/mLStandard Deviation 2.2
TAK-063 3 mg (Healthy Participants)Average Plasma Concentration on Day 1 (Cav) and Day 7 (Cavss) for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 127.2 ng/mLStandard Deviation 3.1
TAK-063 3 mg (Healthy Participants)Average Plasma Concentration on Day 1 (Cav) and Day 7 (Cavss) for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)30.7 ng/mLStandard Deviation 3.8
TAK-063 3 mg (Healthy Participants)Average Plasma Concentration on Day 1 (Cav) and Day 7 (Cavss) for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 113.7 ng/mLStandard Deviation 1.6
TAK-063 10 mg (Healthy Participants)Average Plasma Concentration on Day 1 (Cav) and Day 7 (Cavss) for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 127.8 ng/mLStandard Deviation 6.2
TAK-063 10 mg (Healthy Participants)Average Plasma Concentration on Day 1 (Cav) and Day 7 (Cavss) for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)64.0 ng/mLStandard Deviation 9.8
TAK-063 10 mg (Healthy Participants)Average Plasma Concentration on Day 1 (Cav) and Day 7 (Cavss) for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)33.6 ng/mLStandard Deviation 7.3
TAK-063 10 mg (Healthy Participants)Average Plasma Concentration on Day 1 (Cav) and Day 7 (Cavss) for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 151.8 ng/mLStandard Deviation 11.5
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: Days 1 and 7 pre-dose and multiple time-points post-dose (Up to 24 hours)

Population: PK Set included all randomized participants who received study drug for whom PK data was available for analysis.

ArmMeasureGroupValue (MEAN)Dispersion
TAK-063 3 mg (Schizophrenia Participants)CL/F: Oral Clearance of TAK-063TAK-063 Day 116.1 liter/hourStandard Deviation 7.3
TAK-063 3 mg (Schizophrenia Participants)CL/F: Oral Clearance of TAK-063TAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)11.2 liter/hourStandard Deviation 2.7
TAK-063 10 mg (Schizophrenia Participants)CL/F: Oral Clearance of TAK-063TAK-063 Day 114.0 liter/hourStandard Deviation 4.3
TAK-063 10 mg (Schizophrenia Participants)CL/F: Oral Clearance of TAK-063TAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)15.4 liter/hourStandard Deviation 3.9
TAK-063 20 mg (Schizophrenia Participants)CL/F: Oral Clearance of TAK-063TAK-063 Day 121.3 liter/hourStandard Deviation 8
TAK-063 20 mg (Schizophrenia Participants)CL/F: Oral Clearance of TAK-063TAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)17.1 liter/hourStandard Deviation 4
TAK-063 30 mg (Schizophrenia Participants)CL/F: Oral Clearance of TAK-063TAK-063 Day 114.4 liter/hourStandard Deviation 5.4
TAK-063 30 mg (Schizophrenia Participants)CL/F: Oral Clearance of TAK-063TAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)15.5 liter/hourStandard Deviation 3.5
TAK-063 100 mg (Schizophrenia Participants)CL/F: Oral Clearance of TAK-063TAK-063 Day 138.1 liter/hourStandard Deviation 25
TAK-063 100 mg (Schizophrenia Participants)CL/F: Oral Clearance of TAK-063TAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)38.5 liter/hourStandard Deviation 10.8
Placebo (Schizophrenia Participants)CL/F: Oral Clearance of TAK-063TAK-063 Day 116.9 liter/hourStandard Deviation 5.2
Placebo (Schizophrenia Participants)CL/F: Oral Clearance of TAK-063TAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)10.8 liter/hourStandard Deviation 2.8
TAK-063 3 mg (Healthy Participants)CL/F: Oral Clearance of TAK-063TAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)13.8 liter/hourStandard Deviation 1.6
TAK-063 3 mg (Healthy Participants)CL/F: Oral Clearance of TAK-063TAK-063 Day 113.9 liter/hourStandard Deviation 2
TAK-063 10 mg (Healthy Participants)CL/F: Oral Clearance of TAK-063TAK-063 Day 113.9 liter/hourStandard Deviation 4.6
TAK-063 10 mg (Healthy Participants)CL/F: Oral Clearance of TAK-063TAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)13.3 liter/hourStandard Deviation 1.9
Secondary

CLr: Renal Clearance of TAK-063 and TAK-063 Metabolite M-I

CLr is a measure of apparent clearance of the drug from the urine calculated as total amount excreted in the urine from time 0 to 24 hours postdose / plasma area under the curve from time 0 to 24 hours post-dose.

Time frame: Days 1 and 7 pre-dose and multiple time-points post-dose (Up to 24 hours)

Population: PK Set included all randomized participants who received study drug for whom PK data was available for analysis.

ArmMeasureGroupValue (MEAN)Dispersion
TAK-063 3 mg (Schizophrenia Participants)CLr: Renal Clearance of TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 7 (n=2, 7, 6, 7, 7, 3, 6, 6)11.3 mL/hourStandard Deviation 6.7
TAK-063 3 mg (Schizophrenia Participants)CLr: Renal Clearance of TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 1 (n=0, 8, 6, 7, 7, 0, 7, 8)NA mL/hour—
TAK-063 3 mg (Schizophrenia Participants)CLr: Renal Clearance of TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 7 (n=0, 7, 6, 7, 7, 0, 6, 6)NA mL/hour—
TAK-063 3 mg (Schizophrenia Participants)CLr: Renal Clearance of TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 1 (n=0, 6, 6, 7, 7, 0, 6, 7)NA mL/hour—
TAK-063 10 mg (Schizophrenia Participants)CLr: Renal Clearance of TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 7 (n=2, 7, 6, 7, 7, 3, 6, 6)16.9 mL/hourStandard Deviation 15.5
TAK-063 10 mg (Schizophrenia Participants)CLr: Renal Clearance of TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 1 (n=0, 6, 6, 7, 7, 0, 6, 7)8.4 mL/hourStandard Deviation 3.9
TAK-063 10 mg (Schizophrenia Participants)CLr: Renal Clearance of TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 1 (n=0, 8, 6, 7, 7, 0, 7, 8)15.9 mL/hourStandard Deviation 10.7
TAK-063 10 mg (Schizophrenia Participants)CLr: Renal Clearance of TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 7 (n=0, 7, 6, 7, 7, 0, 6, 6)6.8 mL/hourStandard Deviation 4.4
TAK-063 20 mg (Schizophrenia Participants)CLr: Renal Clearance of TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 1 (n=0, 8, 6, 7, 7, 0, 7, 8)20.4 mL/hourStandard Deviation 8
TAK-063 20 mg (Schizophrenia Participants)CLr: Renal Clearance of TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 1 (n=0, 6, 6, 7, 7, 0, 6, 7)5.2 mL/hourStandard Deviation 2.5
TAK-063 20 mg (Schizophrenia Participants)CLr: Renal Clearance of TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 7 (n=2, 7, 6, 7, 7, 3, 6, 6)21.7 mL/hourStandard Deviation 8.8
TAK-063 20 mg (Schizophrenia Participants)CLr: Renal Clearance of TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 7 (n=0, 7, 6, 7, 7, 0, 6, 6)7.2 mL/hourStandard Deviation 1.1
TAK-063 30 mg (Schizophrenia Participants)CLr: Renal Clearance of TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 1 (n=0, 8, 6, 7, 7, 0, 7, 8)25.6 mL/hourStandard Deviation 9.3
TAK-063 30 mg (Schizophrenia Participants)CLr: Renal Clearance of TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 7 (n=2, 7, 6, 7, 7, 3, 6, 6)26.4 mL/hourStandard Deviation 8.7
TAK-063 30 mg (Schizophrenia Participants)CLr: Renal Clearance of TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 7 (n=0, 7, 6, 7, 7, 0, 6, 6)7.3 mL/hourStandard Deviation 3.4
TAK-063 30 mg (Schizophrenia Participants)CLr: Renal Clearance of TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 1 (n=0, 6, 6, 7, 7, 0, 6, 7)6.7 mL/hourStandard Deviation 1.6
TAK-063 100 mg (Schizophrenia Participants)CLr: Renal Clearance of TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 1 (n=0, 6, 6, 7, 7, 0, 6, 7)16.2 mL/hourStandard Deviation 13.1
TAK-063 100 mg (Schizophrenia Participants)CLr: Renal Clearance of TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 1 (n=0, 8, 6, 7, 7, 0, 7, 8)36.8 mL/hourStandard Deviation 11.9
TAK-063 100 mg (Schizophrenia Participants)CLr: Renal Clearance of TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 7 (n=0, 7, 6, 7, 7, 0, 6, 6)13.3 mL/hourStandard Deviation 7.3
TAK-063 100 mg (Schizophrenia Participants)CLr: Renal Clearance of TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 7 (n=2, 7, 6, 7, 7, 3, 6, 6)41.4 mL/hourStandard Deviation 17
Placebo (Schizophrenia Participants)CLr: Renal Clearance of TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 7 (n=0, 7, 6, 7, 7, 0, 6, 6)NA mL/hour—
Placebo (Schizophrenia Participants)CLr: Renal Clearance of TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 1 (n=0, 6, 6, 7, 7, 0, 6, 7)NA mL/hour—
Placebo (Schizophrenia Participants)CLr: Renal Clearance of TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 7 (n=2, 7, 6, 7, 7, 3, 6, 6)14.2 mL/hourStandard Deviation 6.8
Placebo (Schizophrenia Participants)CLr: Renal Clearance of TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 1 (n=0, 8, 6, 7, 7, 0, 7, 8)NA mL/hour—
TAK-063 3 mg (Healthy Participants)CLr: Renal Clearance of TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 1 (n=0, 8, 6, 7, 7, 0, 7, 8)38.0 mL/hourStandard Deviation 16.4
TAK-063 3 mg (Healthy Participants)CLr: Renal Clearance of TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 1 (n=0, 6, 6, 7, 7, 0, 6, 7)7.0 mL/hourStandard Deviation 7
TAK-063 3 mg (Healthy Participants)CLr: Renal Clearance of TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 7 (n=0, 7, 6, 7, 7, 0, 6, 6)7.3 mL/hourStandard Deviation 3.2
TAK-063 3 mg (Healthy Participants)CLr: Renal Clearance of TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 7 (n=2, 7, 6, 7, 7, 3, 6, 6)42.8 mL/hourStandard Deviation 14
TAK-063 10 mg (Healthy Participants)CLr: Renal Clearance of TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 1 (n=0, 8, 6, 7, 7, 0, 7, 8)39.9 mL/hourStandard Deviation 16.1
TAK-063 10 mg (Healthy Participants)CLr: Renal Clearance of TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 1 (n=0, 6, 6, 7, 7, 0, 6, 7)12.9 mL/hourStandard Deviation 7.5
TAK-063 10 mg (Healthy Participants)CLr: Renal Clearance of TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 7 (n=2, 7, 6, 7, 7, 3, 6, 6)45.5 mL/hourStandard Deviation 17.5
TAK-063 10 mg (Healthy Participants)CLr: Renal Clearance of TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 7 (n=0, 7, 6, 7, 7, 0, 6, 6)10.5 mL/hourStandard Deviation 6.3
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: Days 1 and 7 pre-dose and multiple time-points post-dose (Up to 24 hours)

Population: PK Set included all randomized participants who received study drug for whom PK data was available for analysis.

ArmMeasureGroupValue (MEAN)Dispersion
TAK-063 3 mg (Schizophrenia Participants)Cmax: Maximum Observed Plasma Concentration for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 117.0 ng/mLStandard Deviation 7.2
TAK-063 3 mg (Schizophrenia Participants)Cmax: Maximum Observed Plasma Concentration for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 111.3 ng/mLStandard Deviation 4.2
TAK-063 3 mg (Schizophrenia Participants)Cmax: Maximum Observed Plasma Concentration for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)25.6 ng/mLStandard Deviation 4.6
TAK-063 3 mg (Schizophrenia Participants)Cmax: Maximum Observed Plasma Concentration for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)19.2 ng/mLStandard Deviation 4.2
TAK-063 10 mg (Schizophrenia Participants)Cmax: Maximum Observed Plasma Concentration for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)74.8 ng/mLStandard Deviation 20.3
TAK-063 10 mg (Schizophrenia Participants)Cmax: Maximum Observed Plasma Concentration for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 164.8 ng/mLStandard Deviation 21.5
TAK-063 10 mg (Schizophrenia Participants)Cmax: Maximum Observed Plasma Concentration for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 162.8 ng/mLStandard Deviation 16.6
TAK-063 10 mg (Schizophrenia Participants)Cmax: Maximum Observed Plasma Concentration for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)70.3 ng/mLStandard Deviation 11.5
TAK-063 20 mg (Schizophrenia Participants)Cmax: Maximum Observed Plasma Concentration for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 195.1 ng/mLStandard Deviation 30.8
TAK-063 20 mg (Schizophrenia Participants)Cmax: Maximum Observed Plasma Concentration for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)123.6 ng/mLStandard Deviation 48.2
TAK-063 20 mg (Schizophrenia Participants)Cmax: Maximum Observed Plasma Concentration for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 198.5 ng/mLStandard Deviation 29.1
TAK-063 20 mg (Schizophrenia Participants)Cmax: Maximum Observed Plasma Concentration for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)120.0 ng/mLStandard Deviation 39.3
TAK-063 30 mg (Schizophrenia Participants)Cmax: Maximum Observed Plasma Concentration for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 1151.4 ng/mLStandard Deviation 31.9
TAK-063 30 mg (Schizophrenia Participants)Cmax: Maximum Observed Plasma Concentration for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 193.2 ng/mLStandard Deviation 4.8
TAK-063 30 mg (Schizophrenia Participants)Cmax: Maximum Observed Plasma Concentration for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)179.4 ng/mLStandard Deviation 34.9
TAK-063 30 mg (Schizophrenia Participants)Cmax: Maximum Observed Plasma Concentration for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)108.5 ng/mLStandard Deviation 15.8
TAK-063 100 mg (Schizophrenia Participants)Cmax: Maximum Observed Plasma Concentration for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)127.7 ng/mLStandard Deviation 22.6
TAK-063 100 mg (Schizophrenia Participants)Cmax: Maximum Observed Plasma Concentration for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)228.3 ng/mLStandard Deviation 55.1
TAK-063 100 mg (Schizophrenia Participants)Cmax: Maximum Observed Plasma Concentration for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 1126.7 ng/mLStandard Deviation 29.9
TAK-063 100 mg (Schizophrenia Participants)Cmax: Maximum Observed Plasma Concentration for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 1211.3 ng/mLStandard Deviation 84.8
Placebo (Schizophrenia Participants)Cmax: Maximum Observed Plasma Concentration for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)15.1 ng/mLStandard Deviation 2.4
Placebo (Schizophrenia Participants)Cmax: Maximum Observed Plasma Concentration for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)29.1 ng/mLStandard Deviation 8
Placebo (Schizophrenia Participants)Cmax: Maximum Observed Plasma Concentration for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 18.8 ng/mLStandard Deviation 1.7
Placebo (Schizophrenia Participants)Cmax: Maximum Observed Plasma Concentration for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 114.9 ng/mLStandard Deviation 5.3
TAK-063 3 mg (Healthy Participants)Cmax: Maximum Observed Plasma Concentration for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)38.2 ng/mLStandard Deviation 4.4
TAK-063 3 mg (Healthy Participants)Cmax: Maximum Observed Plasma Concentration for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 169.4 ng/mLStandard Deviation 13.2
TAK-063 3 mg (Healthy Participants)Cmax: Maximum Observed Plasma Concentration for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)74.6 ng/mLStandard Deviation 12.5
TAK-063 3 mg (Healthy Participants)Cmax: Maximum Observed Plasma Concentration for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 136.0 ng/mLStandard Deviation 5
TAK-063 10 mg (Healthy Participants)Cmax: Maximum Observed Plasma Concentration for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 161.8 ng/mLStandard Deviation 11.2
TAK-063 10 mg (Healthy Participants)Cmax: Maximum Observed Plasma Concentration for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)139.8 ng/mLStandard Deviation 25.4
TAK-063 10 mg (Healthy Participants)Cmax: Maximum Observed Plasma Concentration for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)70.9 ng/mLStandard Deviation 17.8
TAK-063 10 mg (Healthy Participants)Cmax: Maximum Observed Plasma Concentration for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 1116.2 ng/mLStandard Deviation 17.9
Secondary

Cmax Molar Ratio: Ratio of TAK-063 Metabolite Cmax to TAK-063 Cmax

Cmax Molar Ratio is the ratio of Cmax molar values of the metabolite compared to the parent calculated by dividing Cmax molar values of metabolite M-I with those of TAK-063.

Time frame: Days 1 and 7 pre-dose and multiple time-points post-dose (Up to 24 hours)

Population: PK Set included all randomized participants who received study drug for whom PK data was available for analysis.

ArmMeasureGroupValue (MEAN)Dispersion
TAK-063 3 mg (Schizophrenia Participants)Cmax Molar Ratio: Ratio of TAK-063 Metabolite Cmax to TAK-063 CmaxTAK-063 M-I Day 10.7 ratioStandard Deviation 0.1
TAK-063 3 mg (Schizophrenia Participants)Cmax Molar Ratio: Ratio of TAK-063 Metabolite Cmax to TAK-063 CmaxTAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)0.7 ratioStandard Deviation 0.2
TAK-063 10 mg (Schizophrenia Participants)Cmax Molar Ratio: Ratio of TAK-063 Metabolite Cmax to TAK-063 CmaxTAK-063 M-I Day 11.0 ratioStandard Deviation 0.2
TAK-063 10 mg (Schizophrenia Participants)Cmax Molar Ratio: Ratio of TAK-063 Metabolite Cmax to TAK-063 CmaxTAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)1.0 ratioStandard Deviation 0.2
TAK-063 20 mg (Schizophrenia Participants)Cmax Molar Ratio: Ratio of TAK-063 Metabolite Cmax to TAK-063 CmaxTAK-063 M-I Day 11.0 ratioStandard Deviation 0.2
TAK-063 20 mg (Schizophrenia Participants)Cmax Molar Ratio: Ratio of TAK-063 Metabolite Cmax to TAK-063 CmaxTAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)1.0 ratioStandard Deviation 0.2
TAK-063 30 mg (Schizophrenia Participants)Cmax Molar Ratio: Ratio of TAK-063 Metabolite Cmax to TAK-063 CmaxTAK-063 M-I Day 10.6 ratioStandard Deviation 0.1
TAK-063 30 mg (Schizophrenia Participants)Cmax Molar Ratio: Ratio of TAK-063 Metabolite Cmax to TAK-063 CmaxTAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)0.6 ratioStandard Deviation 0.1
TAK-063 100 mg (Schizophrenia Participants)Cmax Molar Ratio: Ratio of TAK-063 Metabolite Cmax to TAK-063 CmaxTAK-063 M-I Day 10.6 ratioStandard Deviation 0.2
TAK-063 100 mg (Schizophrenia Participants)Cmax Molar Ratio: Ratio of TAK-063 Metabolite Cmax to TAK-063 CmaxTAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)0.6 ratioStandard Deviation 0.1
Placebo (Schizophrenia Participants)Cmax Molar Ratio: Ratio of TAK-063 Metabolite Cmax to TAK-063 CmaxTAK-063 M-I Day 10.6 ratioStandard Deviation 0.2
Placebo (Schizophrenia Participants)Cmax Molar Ratio: Ratio of TAK-063 Metabolite Cmax to TAK-063 CmaxTAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)0.5 ratioStandard Deviation 0.1
TAK-063 3 mg (Healthy Participants)Cmax Molar Ratio: Ratio of TAK-063 Metabolite Cmax to TAK-063 CmaxTAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)0.5 ratioStandard Deviation 0.1
TAK-063 3 mg (Healthy Participants)Cmax Molar Ratio: Ratio of TAK-063 Metabolite Cmax to TAK-063 CmaxTAK-063 M-I Day 10.5 ratioStandard Deviation 0.1
TAK-063 10 mg (Healthy Participants)Cmax Molar Ratio: Ratio of TAK-063 Metabolite Cmax to TAK-063 CmaxTAK-063 M-I Day 10.5 ratioStandard Deviation 0.1
TAK-063 10 mg (Healthy Participants)Cmax Molar Ratio: Ratio of TAK-063 Metabolite Cmax to TAK-063 CmaxTAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)0.5 ratioStandard Deviation 0.1
Secondary

Fe: Fraction of Drug Excreted in Urine for TAK-063

Fe is a measure of the fraction of drug excreted in urine and is calculated as Fe = (total amount excreted in the urine from time 0 to 24 hours post-dose / dose)×100

Time frame: Days 1 and 7 pre-dose and multiple time-points post-dose (Up to 24 hours)

Population: PK Set included all randomized participants who received study drug for whom PK data was available for analysis.

ArmMeasureGroupValue (MEAN)Dispersion
TAK-063 3 mg (Schizophrenia Participants)Fe: Fraction of Drug Excreted in Urine for TAK-063Day 10.00 percentStandard Deviation 0
TAK-063 3 mg (Schizophrenia Participants)Fe: Fraction of Drug Excreted in Urine for TAK-063Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)0.00 percentStandard Deviation 0
TAK-063 10 mg (Schizophrenia Participants)Fe: Fraction of Drug Excreted in Urine for TAK-063Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)0.04 percentStandard Deviation 0.03
TAK-063 10 mg (Schizophrenia Participants)Fe: Fraction of Drug Excreted in Urine for TAK-063Day 10.04 percentStandard Deviation 0.03
TAK-063 20 mg (Schizophrenia Participants)Fe: Fraction of Drug Excreted in Urine for TAK-063Day 10.02 percentStandard Deviation 0.02
TAK-063 20 mg (Schizophrenia Participants)Fe: Fraction of Drug Excreted in Urine for TAK-063Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)0.04 percentStandard Deviation 0.02
TAK-063 30 mg (Schizophrenia Participants)Fe: Fraction of Drug Excreted in Urine for TAK-063Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)0.05 percentStandard Deviation 0.03
TAK-063 30 mg (Schizophrenia Participants)Fe: Fraction of Drug Excreted in Urine for TAK-063Day 10.03 percentStandard Deviation 0.02
TAK-063 100 mg (Schizophrenia Participants)Fe: Fraction of Drug Excreted in Urine for TAK-063Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)0.04 percentStandard Deviation 0.02
TAK-063 100 mg (Schizophrenia Participants)Fe: Fraction of Drug Excreted in Urine for TAK-063Day 10.03 percentStandard Deviation 0.03
Placebo (Schizophrenia Participants)Fe: Fraction of Drug Excreted in Urine for TAK-063Day 10.00 percentStandard Deviation 0
Placebo (Schizophrenia Participants)Fe: Fraction of Drug Excreted in Urine for TAK-063Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)0.00 percentStandard Deviation 0
TAK-063 3 mg (Healthy Participants)Fe: Fraction of Drug Excreted in Urine for TAK-063Day 10.04 percentStandard Deviation 0.05
TAK-063 3 mg (Healthy Participants)Fe: Fraction of Drug Excreted in Urine for TAK-063Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)0.05 percentStandard Deviation 0.03
TAK-063 10 mg (Healthy Participants)Fe: Fraction of Drug Excreted in Urine for TAK-063Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)0.08 percentStandard Deviation 0.05
TAK-063 10 mg (Healthy Participants)Fe: Fraction of Drug Excreted in Urine for TAK-063Day 10.07 percentStandard Deviation 0.05
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: Days 1 and 7 pre-dose and multiple time-points post-dose (Up to 24 hours)

Population: PK Set included all randomized participants who received study drug for whom PK data was available for analysis.

ArmMeasureGroupValue (MEDIAN)
TAK-063 3 mg (Schizophrenia Participants)Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 13.0 hour
TAK-063 3 mg (Schizophrenia Participants)Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 13.0 hour
TAK-063 3 mg (Schizophrenia Participants)Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)3.0 hour
TAK-063 3 mg (Schizophrenia Participants)Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)4.0 hour
TAK-063 10 mg (Schizophrenia Participants)Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)3.0 hour
TAK-063 10 mg (Schizophrenia Participants)Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 12.0 hour
TAK-063 10 mg (Schizophrenia Participants)Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 12.0 hour
TAK-063 10 mg (Schizophrenia Participants)Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)3.0 hour
TAK-063 20 mg (Schizophrenia Participants)Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 13.0 hour
TAK-063 20 mg (Schizophrenia Participants)Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)3.0 hour
TAK-063 20 mg (Schizophrenia Participants)Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 13.0 hour
TAK-063 20 mg (Schizophrenia Participants)Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)3.0 hour
TAK-063 30 mg (Schizophrenia Participants)Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 13.0 hour
TAK-063 30 mg (Schizophrenia Participants)Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 13.1 hour
TAK-063 30 mg (Schizophrenia Participants)Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)3.0 hour
TAK-063 30 mg (Schizophrenia Participants)Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)3.0 hour
TAK-063 100 mg (Schizophrenia Participants)Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)3.0 hour
TAK-063 100 mg (Schizophrenia Participants)Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)3.0 hour
TAK-063 100 mg (Schizophrenia Participants)Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 13.0 hour
TAK-063 100 mg (Schizophrenia Participants)Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 14.0 hour
Placebo (Schizophrenia Participants)Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)3.0 hour
Placebo (Schizophrenia Participants)Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)3.0 hour
Placebo (Schizophrenia Participants)Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 12.5 hour
Placebo (Schizophrenia Participants)Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 13.0 hour
TAK-063 3 mg (Healthy Participants)Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)3.0 hour
TAK-063 3 mg (Healthy Participants)Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 13.0 hour
TAK-063 3 mg (Healthy Participants)Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)1.5 hour
TAK-063 3 mg (Healthy Participants)Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 13.0 hour
TAK-063 10 mg (Healthy Participants)Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 13.0 hour
TAK-063 10 mg (Healthy Participants)Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)2.5 hour
TAK-063 10 mg (Healthy Participants)Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-063 and TAK-063 Metabolite M-ITAK-063 M-I Day 7 (n=7, 7, 7, 7, 7, 8, 7, 6)3.0 hour
TAK-063 10 mg (Healthy Participants)Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-063 and TAK-063 Metabolite M-ITAK-063 Day 12.5 hour

Source: ClinicalTrials.gov · Data processed: May 9, 2026