Healthy Volunteers
Conditions
Keywords
Drug Therapy
Brief summary
The purpose of this study is to determine: Period 1 (ABA): ABA of mobocertinib following single microdose intravenous administration of 50 microgram (mcg) (approximately 2 microcurie \[mcCi\]) \[14 C\]-\]-mobocertinib and single oral administration of 160 milligram (mg) mobocertinib. Period 2 (absorption, distribution, metabolism, and elimination \[ADME\]): the mass balance and metabolic profile of mobocertinib in plasma, urine, and feces, to characterize the PK of mobocertinib and its metabolites (AP32960 and AP32914) in plasma, whole blood, and urine, and total radioactivity concentration equivalents in plasma and whole blood following a single oral administration of 160 mg (approximately 100 mcCi) \[14C\]-mobocertinib solution.
Detailed description
The drug being tested in this study is called mobocertinib. The study will determine ABA of mobocertinib following single microdose of 50 mcg \[14C\]-mobocertinib and single oral administration of 160 mg mobocertinib and will assess the mass balance and metabolic profile of mobocertinib in plasma, urine, and feces following a single oral administration of 160 mg \[14C\]-mobocertinib solution, and will characterize the PK of mobocertinib and its metabolites in plasma, whole blood, and urine, and total radioactivity concentration equivalents in plasma and whole blood following a single dose of 160 mg \[14C\]-mobocertinib. The study will enroll approximately 6 participants. The study is designed to consist of 2 periods: Period 1 (ABA study period) and Period 2 (ADME study period). In Period 1, all participants will receive single unlabeled oral 160 mg dose of mobocertinib as capsules. At 3.75 hours post oral dosing, participants will receive 15-minute intravenous infusion of a microdose of 50 mcg (approximately 2mcCi) \[14C\]-mobocertinib. In Period 2, participants will receive single dose of 160 mg (approximately 100 mcCi) \[14C\]-mobocertinib as an oral solution. This single center trial will be conducted in the United States. The overall time to participate in this study is approximately 65 days including screening period. Participants will be contacted approximately 30 days after the last dose of study drug for a follow-up assessment.
Interventions
DRUGMobocertinib
Mobocertinib capsule, \[14C\]-Mobocertinib intravenous infusion, \[14C\]-Mobocertinib oral solution.
Sponsors
Millennium Pharmaceuticals, Inc.
Study design
Allocation
NA
Intervention model
SINGLE_GROUP
Primary purpose
OTHER
Masking
NONE
Eligibility
Sex/Gender
MALE
Age
19 Years to 55 Years
Healthy volunteers
Yes
Inclusion criteria
1. Continuous non smoker who has not used nicotine containing products for at least 20 years prior to the first dosing and throughout the study, based on subject self-reporting. 2. Body mass index greater than or equal to (\>=)18 and less than (˂) 30.0 kilogram per square meter (kg/m\^2) at screening.
Exclusion criteria
1. Is mentally or legally incapacitated or has significant emotional problems at the time of the screening visit or expected during the conduct of the study. 2. Has history or presence of alcoholism or drug abuse within the past 2 years prior to the first dosing. 3. Has positive urine drug or alcohol results at screening or first check in. 4. Estimated creatinine clearance \< 80 milliliter per minute (mL/min) at screening. 5. Has tattoo(s) or scarring at or near the site of intravenous (IV) infusion or any other condition which may interfere with infusion site examination, in the opinion of the investigator. 6. Has infrequent bowel movements (less than approximately once per day) within 30 days prior to first dosing. 7. Has recent history of abnormal bowel movements, such as diarrhea, loose stools, or constipation, within 2 weeks of first dosing. 8. Has received radiolabeled substances or has been exposed to radiation sources within 12 months of first dosing or is likely to receive radiation exposure or radioisotopes within 12 months of first dosing such that participation in this study would increase their total exposure beyond the recommended levels considered safe (that is., weighted annual limit recommended by the Commission on Radiological Protection \[ICRP\] of 3000 millirem). 9. Donation of blood or significant blood loss within 56 days prior to the first dosing. 10. Plasma donation within 7 days prior to the first dosing.
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| Period 2, Percentage Change of [14C]-Radioactivity in Whole Blood Relative to Plasma Over the Time for [14C]-Mobocertinib, (Whole Blood : Plasma Partitioning Ratio) | At 0.5 hours (hrs), 1 hr, 2 hrs, 3 hrs, 4 hrs, 5 hrs, 6 hrs, 8 hrs, 12 hrs, 24 hrs, 36 hrs, 48 hrs, 72 hrs, 96 hrs, 120 hrs, 144 hrs, 168 hrs, 192 hrs, 216 hrs and 240 hrs post-dose | — |
| Period 2, AUClast: Area Under the Plasma and Whole Blood Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914) | Day 1 pre-dose at multiple time points (up to 240 hours) post-dose | — |
| Period 2, AUCt: Area Under the Plasma and Whole Blood Concentration-time Curve From Time 0 to Time t for Mobocertinib and Its Metabolites (AP32960 and AP32914) | Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose | — |
| Period 2, Cmax: Maximum Observed Plasma Radioactivity Concentration Equivalents for [14C]-Mobocertinib | Day 1 pre-dose at multiple time points (up to 240 hours) post-dose | — |
| Period 2, Cmax: Maximum Observed Whole Blood Radioactivity Concentration Equivalents for [14C]-Mobocertinib | Day 1 pre-dose at multiple time points (up to 240 hours) post-dose | — |
| Period 2, Tmax: Time to Reach the Maximum Plasma and Whole Blood Radioactivity Concentration (Cmax) Equivalents for [14C]-Mobocertinib | Day 1 pre-dose at multiple time points (up to 240 hours) post-dose | — |
| Period 2, t(1/2z): Terminal Disposition Phase Half-life of Plasma and Whole Blood Radioactivity Concentration Equivalents for [14C]-Mobocertinib | Day 1 pre-dose at multiple time points (up to 240 hours) post-dose | — |
| Period 2, AUC∞: Area Under the Plasma Radioactivity Concentration Equivalents-time Curve From Time 0 to Infinity for [14C]-Mobocertinib | Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose | — |
| Period 2, AUC∞: Area Under the Whole Blood Radioactivity Concentration Equivalents-time Curve From Time 0 to Infinity for [14C]-Mobocertinib | Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose | — |
| Period 2, AUClast: Area Under the Plasma Radioactivity Concentration Equivalents -Time Curve From Time 0 to Last Quantifiable Concentration for [14C]-Mobocertinib | Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose | — |
| Period 2, AUClast: Area Under the Whole Blood Radioactivity Concentration Equivalents -Time Curve From Time 0 to Last Quantifiable Concentration for [14C]- Mobocertinib | Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose | — |
| Period 2, AUCt : Area Under the Plasma Radioactivity Concentration Equivalents-time Curve From Time 0 to Time t for [14C]-Mobocertinib | Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose | — |
| Period 2, AUCt : Area Under the Whole Blood Radioactivity Concentration Equivalents-time Curve From Time 0 to Time t for [14C]-Mobocertinib | Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose | — |
| Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) | Day 1: at Pre-dose, 0-12 hours (hrs), 12-24 hrs, 24-48 hrs, 48-72 hrs, 72-96 hrs, 96-120 hrs, 120-144 hrs, 144-168 hrs, 168-192 hrs, 192-216 hrs and 216-240 hrs post dose | — |
| Period 2, CLR: Renal Clearance for Mobocertinib and Its Metabolites (AP32960 and AP32914) | Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose | — |
| Period 2: t(1/2): Terminal Disposition Phase Half-life of Mobocertinib and Its Metabolites (AP32960 and AP32914) in Plasma and Whole Blood | Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose | — |
| Period 1: Percent Absolute Oral Bioavailability (%F) for Mobocertinib | Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose | Absolute bioavailability (F), defined as the fraction or percentage of the unchanged, orally administered dose that is systemically available, relative to the total dose administered intravenously. Percent Absolute Oral Bioavailability (%F) was calculated as dose of \[14C\]-mobocertinib intravenous in mg\*AUC∞ of mobocertinib (oral)/dose of mobocertinib (oral)\* AUC∞ of \[14C\]-mobocertinib (intravenous)\*100. |
| Period 2: Percentage of Total Radioactivity (Cum%Dose) Recovered in Urine Relative to the Administered Radioactive Dose | Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose | — |
| Period 2: Percentage of Total Radioactivity (Cum%Dose) Recovered in Feces Relative to the Administered Radioactive Dose | Day 1 pre-dose and at multiple time points (up to 432 hours) post-dose | — |
| Period 2: Amount of Total Radioactivity Excreted in Urine (Ae[UR]) | Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose | — |
| Period 2: Amount of Total Radioactivity Excreted in Feces (Ae[Fe]) | Day 1 pre-dose and at multiple time points (up to 432 hours) post-dose | — |
| Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Urine for Mobocertinib | Day 1: Pre-dose, 0-12 hours (hrs), 12-24 hrs, 24-48 hrs, 48-72 hrs, 72-96 hrs, 96-120 hrs, 120-144 hrs, 144-168 hrs, 168-192 hrs, 192-216 hrs, 216-240 hrs post-dose | — |
| Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Feces for Mobocertinib | Day 1: at Pre-dose, 0-24 hours (hrs), 24-48 hrs, 48-72 hrs, 72-96 hrs, 96-120 hrs, 120-144 hrs, 144-168 hrs, 168-192 hrs, 192-216 hrs, 216-240 hrs; 240-264 hrs, 264-288 hrs, 288-312 hrs, 213-408 hrs and 408-432 hrs | — |
| Period 2, Cmax: Maximum Observed Plasma and Whole Blood Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914) | Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose | — |
| Period 2, Tmax: Time to Reach the Maximum Plasma and Whole Blood Concentration (Cmax) for Mobocertinib and Its Metabolites (AP32960 and AP32914) | Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose | — |
| Period 2, AUC∞: Area Under the Plasma and Whole Blood Concentration-time Curve From Time 0 to Infinity for Mobocertinib and Its Metabolites (AP32960 and AP32914) | Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose | — |
Secondary
| Measure | Time frame | Description |
|---|---|---|
| Period 1, Cmax: Maximum Observed Plasma Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914) After Oral Administration | Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose | — |
| Period 1, Cmax: Maximum Observed Plasma Concentration for [14C]-Mobocertinib and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) After Intravenous Administration | Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose | — |
| Period 1, Time to Reach the Maximum Plasma Concentration (Cmax) for Mobocertinib and Its Metabolites (AP32960 and AP32914) After Oral, and [14C]-Mobocertinib and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) After Intravenous Administration | Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose | Data for mobocertinib and its metabolites (AP32960 and AP32914) is reported following the oral administration, and data for \[14C\]-mobocertinib and its metabolites (\[14C\]-AP32960 and \[14C\]-AP32914) is reported following intravenous administration. |
| Period 1, AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for Mobocertinib and Its Metabolites (AP32960 and AP32914) After Oral Administration | Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose | — |
| Period 1, AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for [14C]-Mobocertinib and Its Metabolites ( [14C]-AP32960 and [14C]-AP32914) After Intravenous Administration | Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose | — |
| Period 1, AUClast: Area Under the Plasma Concentration-time Curve From Time 0 to Last Quantifiable Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914) After Oral Administration | Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose | — |
| Period 1, AUClast: Area Under the Plasma Concentration-time Curve From Time 0 to Last Quantifiable Concentration for [14C]-Mobocertinib and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) After Intravenous Administration | Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose | — |
| Period 1, AUCt: Area Under the Plasma Concentration-time Curve From Time 0 to Time t for [14C]-Mobocertinib and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) After Intravenous Administration | Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose | — |
| Period 1, t(1/2):Terminal Disposition Phase Half-Life of Mobocertinib and Its Metabolites (AP32960 and AP32914) in Plasma After Oral, and [14C]-Mobocertinib and Its Metabolites ( [14C]-AP32960 and [14C]-AP32914) in Plasma After Intravenous Administration | Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose | Data for mobocertinib and its metabolites (AP32960 and AP32914) is reported following the oral administration, and data for \[14C\]-mobocertinib and its metabolites (\[14C\]-AP32960 and \[14C\]-AP32914) is reported following intravenous administration. |
| Number of Participants Reporting One or More Treatment-emergent Adverse Events (TEAEs) | Baseline up to 30 days after last dose of study drug in Period 2 (Day 41) | — |
| Number of Participants With Clinically Significant Change From Baseline in 12-lead Electrocardiogram (ECG) Findings | Baseline up to 30 days after last dose of study drug in Period 2 (Day 41) | — |
| Number of Participants With Clinically Significant Change From Baseline in Vital Signs | Baseline up to 30 days after last dose of study drug in Period 2 (Day 41) | — |
| Number of Participants With Clinically Significant Change From Baseline in Laboratory Values | Baseline up to 30 days after last dose of study drug in Period 2 (Day 41) | — |
| Period 1, Ceoi: Plasma Concentration at the End of Infusion for [14C]-Mobocertinib, and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) | Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose | — |
Countries
United States
Participant flow
Recruitment details
Participants took part in the study at 1 investigative site in the United States from 22 January 2019 to 11 March 2019.
Pre-assignment details
Healthy male participants were enrolled in this 2-period study to receive mobocertinib 160 milligram (mg), capsules followed by carbon-14 \[14C\]-mobocertinib 50 microgram (mcg), infusion in Period 1 (Absolute Bioavailability \[ABA\]) and \[14C\]-mobocertinib 160 mg, solution in Period 2 (Absorption, Distribution, Metabolism, and Elimination \[ADME\]).
Participants by arm
| Arm | Count |
|---|---|
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg +[14C]-Mobocertinib 160 mg Mobocertinib 160 mg, capsule, orally, once under fasted state, followed by \[14C\]-mobocertinib 50 mcg (approximately 2 mcCi), infusion, intravenously, once on Day 1 of Period 1, further followed by a washout period of 9 days, followed by \[14C\]-mobocertinib 160 mg (approximately 100 mcCi), solution, orally, once under fasted state on Day 1 of Period 2. | 7 |
| Total | 7 |
Withdrawals & dropouts
| Period | Reason | FG000 |
|---|---|---|
| Period 1 ( 7 Days) | Adverse Event | 1 |
Baseline characteristics
| Characteristic | Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg +[14C]-Mobocertinib 160 mg |
|---|---|
| Age, Continuous | 38.6 years STANDARD_DEVIATION 12.75 |
| Body mass index (BMI) | 27.079 kilogram per square meter (kg/m^2) STANDARD_DEVIATION 1.652 |
| Ethnicity (NIH/OMB) Hispanic or Latino | 2 Participants |
| Ethnicity (NIH/OMB) Not Hispanic or Latino | 5 Participants |
| Ethnicity (NIH/OMB) Unknown or Not Reported | 0 Participants |
| Height | 175.9 centimeter (cm) STANDARD_DEVIATION 4.14 |
| Race (NIH/OMB) American Indian or Alaska Native | 0 Participants |
| Race (NIH/OMB) Asian | 0 Participants |
| Race (NIH/OMB) Black or African American | 1 Participants |
| Race (NIH/OMB) More than one race | 0 Participants |
| Race (NIH/OMB) Native Hawaiian or Other Pacific Islander | 1 Participants |
| Race (NIH/OMB) Unknown or Not Reported | 0 Participants |
| Race (NIH/OMB) White | 5 Participants |
| Region of Enrollment United States | 7 Participants |
| Sex: Female, Male Female | 0 Participants |
| Sex: Female, Male Male | 7 Participants |
| Weight | 83.74 kilogram (Kg) STANDARD_DEVIATION 6.141 |
Adverse events
| Event type | EG000 affected / at risk | EG001 affected / at risk |
|---|---|---|
| deaths Total, all-cause mortality | 0 / 7 | 0 / 6 |
| other Total, other adverse events | 6 / 7 | 4 / 6 |
| serious Total, serious adverse events | 0 / 7 | 0 / 6 |
Outcome results
Primary
Period 1: Percent Absolute Oral Bioavailability (%F) for Mobocertinib
Absolute bioavailability (F), defined as the fraction or percentage of the unchanged, orally administered dose that is systemically available, relative to the total dose administered intravenously. Percent Absolute Oral Bioavailability (%F) was calculated as dose of \[14C\]-mobocertinib intravenous in mg\*AUC∞ of mobocertinib (oral)/dose of mobocertinib (oral)\* AUC∞ of \[14C\]-mobocertinib (intravenous)\*100.
Time frame: Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose
Population: The pharmacokinetic (PK) set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This outcome measure (OM) was planned to be assessed only in Period 1.
| Arm | Measure | Value (GEOMETRIC_MEAN) |
|---|---|---|
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 1: Percent Absolute Oral Bioavailability (%F) for Mobocertinib | 36.7 percentage bioavailability |
Primary
Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914)
Time frame: Day 1: at Pre-dose, 0-12 hours (hrs), 12-24 hrs, 24-48 hrs, 48-72 hrs, 72-96 hrs, 96-120 hrs, 120-144 hrs, 144-168 hrs, 168-192 hrs, 192-216 hrs and 216-240 hrs post dose
Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. Here number analyzed n are the participants who were evaluable for the outcome measure at given timepoints. This OM was planned to be assessed only in Period 2.
| Arm | Measure | Group | Value (MEAN) | Dispersion |
|---|---|---|---|---|
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) | Mobocertinib: Pre-dose | 0.001072 mg | Standard Deviation 0.0010474 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) | Mobocertinib: 0 to 12 hours | 0.1917 mg | Standard Deviation 0.10878 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) | AP32960: 96-120 hours | 0.03017 mg | Standard Deviation 0.0070669 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) | Mobocertinib: 12 to 24 hours | 0.2047 mg | Standard Deviation 0.084347 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) | Mobocertinib: 24 to 48 hours | 0.1628 mg | Standard Deviation 0.050589 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) | Mobocertinib: 48 to 72 hours | 0.05069 mg | Standard Deviation 0.029114 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) | Mobocertinib: 72 to 96 hours | 0.02087 mg | Standard Deviation 0.013052 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) | Mobocertinib: 96 to 120 hours | 0.01028 mg | Standard Deviation 0.0052244 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) | Mobocertinib: 120 to 144 hours | 0.005860 mg | Standard Deviation 0.0055472 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) | Mobocertinib: 144 to 168 hours | 0.002438 mg | Standard Deviation 0.0014131 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) | Mobocertinib: 168 to 192 hours | 0.0009682 mg | Standard Deviation 0.0011637 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) | Mobocertinib: 192 to 216 hours | 0.0009890 mg | Standard Deviation 0.00090295 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) | Mobocertinib: 216 to 240 hours | 0.0002824 mg | Standard Deviation 0.00063158 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) | AP32960: Pre-dose | 0.005308 mg | Standard Deviation 0.0045461 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) | AP32960: 0-12 hours | 0.2948 mg | Standard Deviation 0.078117 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) | AP32960: 12-24 hours | 0.2199 mg | Standard Deviation 0.056834 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) | AP32960: 24-48 hours | 0.2166 mg | Standard Deviation 0.04903 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) | AP32960: 48-72 hours | 0.09444 mg | Standard Deviation 0.020647 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) | AP32960: 72-96 hours | 0.05401 mg | Standard Deviation 0.014311 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) | AP32960: 120-144 hours | 0.01764 mg | Standard Deviation 0.006867 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) | AP32960: 144-168 hours | 0.01082 mg | Standard Deviation 0.0028229 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) | AP32960: 168-192 hours | 0.007272 mg | Standard Deviation 0.0023649 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) | AP32960: 192-216 hours | 0.005427 mg | Standard Deviation 0.0021935 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) | AP32960: 216-240 hours | 0.004235 mg | Standard Deviation 0.0016891 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) | AP32914: Pre-dose | 0.00 mg | Standard Deviation 0 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) | AP32914: 0-12 hours | 0.08336 mg | Standard Deviation 0.022896 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) | AP32914: 12-24 hours | 0.06029 mg | Standard Deviation 0.015305 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) | AP32914: 24-48 hours | 0.04953 mg | Standard Deviation 0.021338 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) | AP32914: 48-72 hours | 0.01543 mg | Standard Deviation 0.0068257 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) | AP32914: 72-96 hours | 0.005859 mg | Standard Deviation 0.0040117 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) | AP32914: 96-120 hours | 0.002477 mg | Standard Deviation 0.0016606 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) | AP32914: 120-144 hours | 0.0008353 mg | Standard Deviation 0.0010134 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) | AP32914: 144-168 hours | 0.0001780 mg | Standard Deviation 0.00043613 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) | AP32914: 168-192 hours | 0.00 mg | Standard Deviation 0 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) | AP32914: 192-216 hours | 0.00 mg | Standard Deviation 0 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914) | AP32914: 216-240 hours | 0.00 mg | Standard Deviation 0 |
Primary
Period 2: Amount of Total Radioactivity Excreted in Feces (Ae[Fe])
Time frame: Day 1 pre-dose and at multiple time points (up to 432 hours) post-dose
Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 2.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2: Amount of Total Radioactivity Excreted in Feces (Ae[Fe]) | 123.1 mg eq | Geometric Coefficient of Variation 6.1 |
Primary
Period 2: Amount of Total Radioactivity Excreted in Urine (Ae[UR])
Time frame: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 2.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2: Amount of Total Radioactivity Excreted in Urine (Ae[UR]) | 5.777 milligram equivalent (mg eq) | Geometric Coefficient of Variation 12.6 |
Primary
Period 2, AUC∞: Area Under the Plasma and Whole Blood Concentration-time Curve From Time 0 to Infinity for Mobocertinib and Its Metabolites (AP32960 and AP32914)
Time frame: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 2.
| Arm | Measure | Group | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|---|
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, AUC∞: Area Under the Plasma and Whole Blood Concentration-time Curve From Time 0 to Infinity for Mobocertinib and Its Metabolites (AP32960 and AP32914) | Plasma: Mobocertinib | 956 nanogram*hour per milliliter (ng*hr/mL) | Geometric Coefficient of Variation 38.6 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, AUC∞: Area Under the Plasma and Whole Blood Concentration-time Curve From Time 0 to Infinity for Mobocertinib and Its Metabolites (AP32960 and AP32914) | Plasma: AP32960 | 486 nanogram*hour per milliliter (ng*hr/mL) | Geometric Coefficient of Variation 26.7 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, AUC∞: Area Under the Plasma and Whole Blood Concentration-time Curve From Time 0 to Infinity for Mobocertinib and Its Metabolites (AP32960 and AP32914) | Plasma: AP32914 | 73.4 nanogram*hour per milliliter (ng*hr/mL) | Geometric Coefficient of Variation 39.9 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, AUC∞: Area Under the Plasma and Whole Blood Concentration-time Curve From Time 0 to Infinity for Mobocertinib and Its Metabolites (AP32960 and AP32914) | Whole Blood: Mobocertinib | 729 nanogram*hour per milliliter (ng*hr/mL) | Geometric Coefficient of Variation 32.8 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, AUC∞: Area Under the Plasma and Whole Blood Concentration-time Curve From Time 0 to Infinity for Mobocertinib and Its Metabolites (AP32960 and AP32914) | Whole Blood: AP32960 | 556 nanogram*hour per milliliter (ng*hr/mL) | Geometric Coefficient of Variation 20.2 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, AUC∞: Area Under the Plasma and Whole Blood Concentration-time Curve From Time 0 to Infinity for Mobocertinib and Its Metabolites (AP32960 and AP32914) | Whole Blood: AP32914 | 52.4 nanogram*hour per milliliter (ng*hr/mL) | Geometric Coefficient of Variation 37.3 |
Primary
Period 2, AUC∞: Area Under the Plasma Radioactivity Concentration Equivalents-time Curve From Time 0 to Infinity for [14C]-Mobocertinib
Time frame: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 2.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, AUC∞: Area Under the Plasma Radioactivity Concentration Equivalents-time Curve From Time 0 to Infinity for [14C]-Mobocertinib | 556000 nanogram equivalent*hour per milliliter | Geometric Coefficient of Variation 14.9 |
Primary
Period 2, AUC∞: Area Under the Whole Blood Radioactivity Concentration Equivalents-time Curve From Time 0 to Infinity for [14C]-Mobocertinib
Time frame: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 2.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, AUC∞: Area Under the Whole Blood Radioactivity Concentration Equivalents-time Curve From Time 0 to Infinity for [14C]-Mobocertinib | 325000 nanogram equivalent*hour per gram | Geometric Coefficient of Variation 21.2 |
Primary
Period 2, AUClast: Area Under the Plasma and Whole Blood Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914)
Time frame: Day 1 pre-dose at multiple time points (up to 240 hours) post-dose
Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 2.
| Arm | Measure | Group | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|---|
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, AUClast: Area Under the Plasma and Whole Blood Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914) | Plasma: Mobocertinib | 945 ng*hr/mL | Geometric Coefficient of Variation 39.2 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, AUClast: Area Under the Plasma and Whole Blood Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914) | Plasma: AP32960 | 471 ng*hr/mL | Geometric Coefficient of Variation 27.5 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, AUClast: Area Under the Plasma and Whole Blood Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914) | Plasma: AP32914 | 63.6 ng*hr/mL | Geometric Coefficient of Variation 45.7 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, AUClast: Area Under the Plasma and Whole Blood Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914) | Whole Blood: Mobocertinib | 718 ng*hr/mL | Geometric Coefficient of Variation 33.2 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, AUClast: Area Under the Plasma and Whole Blood Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914) | Whole Blood: AP32960 | 543 ng*hr/mL | Geometric Coefficient of Variation 20.5 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, AUClast: Area Under the Plasma and Whole Blood Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914) | Whole Blood: AP32914 | 45.7 ng*hr/mL | Geometric Coefficient of Variation 40.4 |
Primary
Period 2, AUClast: Area Under the Plasma Radioactivity Concentration Equivalents -Time Curve From Time 0 to Last Quantifiable Concentration for [14C]-Mobocertinib
Time frame: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 2.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, AUClast: Area Under the Plasma Radioactivity Concentration Equivalents -Time Curve From Time 0 to Last Quantifiable Concentration for [14C]-Mobocertinib | 230300 nanogram equivalent*hour per milliliter | Geometric Coefficient of Variation 15.5 |
Primary
Period 2, AUClast: Area Under the Whole Blood Radioactivity Concentration Equivalents -Time Curve From Time 0 to Last Quantifiable Concentration for [14C]- Mobocertinib
Time frame: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 2.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, AUClast: Area Under the Whole Blood Radioactivity Concentration Equivalents -Time Curve From Time 0 to Last Quantifiable Concentration for [14C]- Mobocertinib | 131000 nanogram equivalent*hour per gram | Geometric Coefficient of Variation 18.5 |
Primary
Period 2, AUCt: Area Under the Plasma and Whole Blood Concentration-time Curve From Time 0 to Time t for Mobocertinib and Its Metabolites (AP32960 and AP32914)
Time frame: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 2.
| Arm | Measure | Group | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|---|
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, AUCt: Area Under the Plasma and Whole Blood Concentration-time Curve From Time 0 to Time t for Mobocertinib and Its Metabolites (AP32960 and AP32914) | Plasma: Mobocertinib | 944.9 ng*hr/mL | Geometric Coefficient of Variation 39.2 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, AUCt: Area Under the Plasma and Whole Blood Concentration-time Curve From Time 0 to Time t for Mobocertinib and Its Metabolites (AP32960 and AP32914) | Plasma: AP32960 | 471.1 ng*hr/mL | Geometric Coefficient of Variation 27.5 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, AUCt: Area Under the Plasma and Whole Blood Concentration-time Curve From Time 0 to Time t for Mobocertinib and Its Metabolites (AP32960 and AP32914) | Plasma: AP32914 | 63.61 ng*hr/mL | Geometric Coefficient of Variation 45.7 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, AUCt: Area Under the Plasma and Whole Blood Concentration-time Curve From Time 0 to Time t for Mobocertinib and Its Metabolites (AP32960 and AP32914) | Whole Blood: Mobocertinib | 717.7 ng*hr/mL | Geometric Coefficient of Variation 33.2 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, AUCt: Area Under the Plasma and Whole Blood Concentration-time Curve From Time 0 to Time t for Mobocertinib and Its Metabolites (AP32960 and AP32914) | Whole Blood: AP32960 | 542.8 ng*hr/mL | Geometric Coefficient of Variation 20.5 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, AUCt: Area Under the Plasma and Whole Blood Concentration-time Curve From Time 0 to Time t for Mobocertinib and Its Metabolites (AP32960 and AP32914) | Whole Blood: AP32914 | 45.74 ng*hr/mL | Geometric Coefficient of Variation 40.4 |
Primary
Period 2, AUCt : Area Under the Plasma Radioactivity Concentration Equivalents-time Curve From Time 0 to Time t for [14C]-Mobocertinib
Time frame: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 2.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, AUCt : Area Under the Plasma Radioactivity Concentration Equivalents-time Curve From Time 0 to Time t for [14C]-Mobocertinib | 145400 nanogram equivalent*hour per milliliter | Geometric Coefficient of Variation 35.3 |
Primary
Period 2, AUCt : Area Under the Whole Blood Radioactivity Concentration Equivalents-time Curve From Time 0 to Time t for [14C]-Mobocertinib
Time frame: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 2.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, AUCt : Area Under the Whole Blood Radioactivity Concentration Equivalents-time Curve From Time 0 to Time t for [14C]-Mobocertinib | 70190 nanogram equivalent*hour per gram | Geometric Coefficient of Variation 32.4 |
Primary
Period 2, CLR: Renal Clearance for Mobocertinib and Its Metabolites (AP32960 and AP32914)
Time frame: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 2.
| Arm | Measure | Group | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|---|
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, CLR: Renal Clearance for Mobocertinib and Its Metabolites (AP32960 and AP32914) | Mobocertinib | 0.657 liter per hour ( L/h) | Geometric Coefficient of Variation 44.3 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, CLR: Renal Clearance for Mobocertinib and Its Metabolites (AP32960 and AP32914) | AP32960 | 1.95 liter per hour ( L/h) | Geometric Coefficient of Variation 22.5 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, CLR: Renal Clearance for Mobocertinib and Its Metabolites (AP32960 and AP32914) | AP32914 | 2.85 liter per hour ( L/h) | Geometric Coefficient of Variation 27.9 |
Primary
Period 2, Cmax: Maximum Observed Plasma and Whole Blood Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914)
Time frame: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 2.
| Arm | Measure | Group | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|---|
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Cmax: Maximum Observed Plasma and Whole Blood Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914) | Plasma: Mobocertinib | 51.0 ng/mL | Geometric Coefficient of Variation 34.9 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Cmax: Maximum Observed Plasma and Whole Blood Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914) | Plasma: AP32960 | 22.7 ng/mL | Geometric Coefficient of Variation 19.8 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Cmax: Maximum Observed Plasma and Whole Blood Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914) | Plasma: AP32914 | 4.28 ng/mL | Geometric Coefficient of Variation 34.7 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Cmax: Maximum Observed Plasma and Whole Blood Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914) | Whole Blood: Mobocertinib | 40.5 ng/mL | Geometric Coefficient of Variation 29.1 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Cmax: Maximum Observed Plasma and Whole Blood Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914) | Whole Blood: AP32960 | 26.7 ng/mL | Geometric Coefficient of Variation 10.6 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Cmax: Maximum Observed Plasma and Whole Blood Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914) | Whole Blood: AP32914 | 3.05 ng/mL | Geometric Coefficient of Variation 28.6 |
Primary
Period 2, Cmax: Maximum Observed Plasma Radioactivity Concentration Equivalents for [14C]-Mobocertinib
Time frame: Day 1 pre-dose at multiple time points (up to 240 hours) post-dose
Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 2.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Cmax: Maximum Observed Plasma Radioactivity Concentration Equivalents for [14C]-Mobocertinib | 1250 nanogram equivalent/milliliter(ng eq/mL) | Geometric Coefficient of Variation 13.4 |
Primary
Period 2, Cmax: Maximum Observed Whole Blood Radioactivity Concentration Equivalents for [14C]-Mobocertinib
Time frame: Day 1 pre-dose at multiple time points (up to 240 hours) post-dose
Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 2.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Cmax: Maximum Observed Whole Blood Radioactivity Concentration Equivalents for [14C]-Mobocertinib | 725 nanogram equivalent/ gram (ng eq/g) | Geometric Coefficient of Variation 14.6 |
Primary
Period 2, Percentage Change of [14C]-Radioactivity in Whole Blood Relative to Plasma Over the Time for [14C]-Mobocertinib, (Whole Blood : Plasma Partitioning Ratio)
Time frame: At 0.5 hours (hrs), 1 hr, 2 hrs, 3 hrs, 4 hrs, 5 hrs, 6 hrs, 8 hrs, 12 hrs, 24 hrs, 36 hrs, 48 hrs, 72 hrs, 96 hrs, 120 hrs, 144 hrs, 168 hrs, 192 hrs, 216 hrs and 240 hrs post-dose
Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. Here number analyzed n are the participants who were evaluable for the outcome measure at given timepoints. Here, '0' in the number analyzed field signifies that no participants were evaluable at specified time points. This OM was planned to be assessed only in Period 2.
| Arm | Measure | Group | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|---|
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Percentage Change of [14C]-Radioactivity in Whole Blood Relative to Plasma Over the Time for [14C]-Mobocertinib, (Whole Blood : Plasma Partitioning Ratio) | At 0.5 hour | 1.022 ratio | Geometric Coefficient of Variation 21.9 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Percentage Change of [14C]-Radioactivity in Whole Blood Relative to Plasma Over the Time for [14C]-Mobocertinib, (Whole Blood : Plasma Partitioning Ratio) | At 1 hour | 0.9851 ratio | Geometric Coefficient of Variation 36 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Percentage Change of [14C]-Radioactivity in Whole Blood Relative to Plasma Over the Time for [14C]-Mobocertinib, (Whole Blood : Plasma Partitioning Ratio) | At 2 hours | 0.9055 ratio | Geometric Coefficient of Variation 25.3 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Percentage Change of [14C]-Radioactivity in Whole Blood Relative to Plasma Over the Time for [14C]-Mobocertinib, (Whole Blood : Plasma Partitioning Ratio) | At 3 hours | 0.8403 ratio | Geometric Coefficient of Variation 22.4 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Percentage Change of [14C]-Radioactivity in Whole Blood Relative to Plasma Over the Time for [14C]-Mobocertinib, (Whole Blood : Plasma Partitioning Ratio) | At 4 hours | 0.8221 ratio | Geometric Coefficient of Variation 23.3 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Percentage Change of [14C]-Radioactivity in Whole Blood Relative to Plasma Over the Time for [14C]-Mobocertinib, (Whole Blood : Plasma Partitioning Ratio) | At 5 hours | 0.8545 ratio | Geometric Coefficient of Variation 17.2 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Percentage Change of [14C]-Radioactivity in Whole Blood Relative to Plasma Over the Time for [14C]-Mobocertinib, (Whole Blood : Plasma Partitioning Ratio) | At 6 hours | 0.7647 ratio | Geometric Coefficient of Variation 18.6 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Percentage Change of [14C]-Radioactivity in Whole Blood Relative to Plasma Over the Time for [14C]-Mobocertinib, (Whole Blood : Plasma Partitioning Ratio) | At 8 hours | 0.7634 ratio | Geometric Coefficient of Variation 20.7 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Percentage Change of [14C]-Radioactivity in Whole Blood Relative to Plasma Over the Time for [14C]-Mobocertinib, (Whole Blood : Plasma Partitioning Ratio) | At 12 hours | 0.7573 ratio | Geometric Coefficient of Variation 17.6 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Percentage Change of [14C]-Radioactivity in Whole Blood Relative to Plasma Over the Time for [14C]-Mobocertinib, (Whole Blood : Plasma Partitioning Ratio) | At 24 hours | 0.8139 ratio | Geometric Coefficient of Variation 23 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Percentage Change of [14C]-Radioactivity in Whole Blood Relative to Plasma Over the Time for [14C]-Mobocertinib, (Whole Blood : Plasma Partitioning Ratio) | At 36 hours | 0.7028 ratio | Geometric Coefficient of Variation 13.2 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Percentage Change of [14C]-Radioactivity in Whole Blood Relative to Plasma Over the Time for [14C]-Mobocertinib, (Whole Blood : Plasma Partitioning Ratio) | At 48 hours | 0.7113 ratio | Geometric Coefficient of Variation 14.7 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Percentage Change of [14C]-Radioactivity in Whole Blood Relative to Plasma Over the Time for [14C]-Mobocertinib, (Whole Blood : Plasma Partitioning Ratio) | At 72 hours | 0.6453 ratio | Geometric Coefficient of Variation 18.8 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Percentage Change of [14C]-Radioactivity in Whole Blood Relative to Plasma Over the Time for [14C]-Mobocertinib, (Whole Blood : Plasma Partitioning Ratio) | At 96 hours | 0.6164 ratio | Geometric Coefficient of Variation 18 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Percentage Change of [14C]-Radioactivity in Whole Blood Relative to Plasma Over the Time for [14C]-Mobocertinib, (Whole Blood : Plasma Partitioning Ratio) | At 120 hours | 0.6260 ratio | Geometric Coefficient of Variation 13.2 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Percentage Change of [14C]-Radioactivity in Whole Blood Relative to Plasma Over the Time for [14C]-Mobocertinib, (Whole Blood : Plasma Partitioning Ratio) | At 144 hours | 0.5946 ratio | — |
Primary
Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Feces for Mobocertinib
Time frame: Day 1: at Pre-dose, 0-24 hours (hrs), 24-48 hrs, 48-72 hrs, 72-96 hrs, 96-120 hrs, 120-144 hrs, 144-168 hrs, 168-192 hrs, 192-216 hrs, 216-240 hrs; 240-264 hrs, 264-288 hrs, 288-312 hrs, 213-408 hrs and 408-432 hrs
Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. Here number analyzed n are the participants who were evaluable for the outcome measure at given timepoints. This OM was planned to be assessed only in Period 2.
| Arm | Measure | Group | Value (MEAN) | Dispersion |
|---|---|---|---|---|
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Feces for Mobocertinib | Pre-dose | 0.00 percentage of radioactive dose | Standard Deviation 0 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Feces for Mobocertinib | 0-24 hours | 16.13 percentage of radioactive dose | Standard Deviation 16.772 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Feces for Mobocertinib | 24-48 hours | 27.78 percentage of radioactive dose | Standard Deviation 19.584 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Feces for Mobocertinib | 48-72 hours | 16.10 percentage of radioactive dose | Standard Deviation 21.089 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Feces for Mobocertinib | 72-96 hours | 4.214 percentage of radioactive dose | Standard Deviation 5.3488 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Feces for Mobocertinib | 96-120 hours | 3.066 percentage of radioactive dose | Standard Deviation 2.8311 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Feces for Mobocertinib | 120-144 hours | 1.638 percentage of radioactive dose | Standard Deviation 1.808 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Feces for Mobocertinib | 144-168 hours | 2.756 percentage of radioactive dose | Standard Deviation 3.3943 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Feces for Mobocertinib | 168-192 hours | 0.9919 percentage of radioactive dose | Standard Deviation 0.83406 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Feces for Mobocertinib | 192-216 hours | 2.069 percentage of radioactive dose | Standard Deviation 1.0034 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Feces for Mobocertinib | 216-240 hours | 1.695 percentage of radioactive dose | Standard Deviation 1.1513 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Feces for Mobocertinib | 240-264 hours | 0.1056 percentage of radioactive dose | Standard Deviation 0.14927 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Feces for Mobocertinib | 264-288 hours | 0.2216 percentage of radioactive dose | Standard Deviation 0.31341 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Feces for Mobocertinib | 288-312 hours | 0.7632 percentage of radioactive dose | — |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Feces for Mobocertinib | 312-408 hours | 0.3107 percentage of radioactive dose | — |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Feces for Mobocertinib | 408-432 hours | 0.1143 percentage of radioactive dose | — |
Primary
Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Urine for Mobocertinib
Time frame: Day 1: Pre-dose, 0-12 hours (hrs), 12-24 hrs, 24-48 hrs, 48-72 hrs, 72-96 hrs, 96-120 hrs, 120-144 hrs, 144-168 hrs, 168-192 hrs, 192-216 hrs, 216-240 hrs post-dose
Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. Here number analyzed n are the participants who were evaluable for the outcome measure at given timepoints. This OM was planned to be assessed only in Period 2.
| Arm | Measure | Group | Value (MEAN) | Dispersion |
|---|---|---|---|---|
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Urine for Mobocertinib | Pre-dose | 0.00 percentage of radioactive dose | Standard Deviation 0 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Urine for Mobocertinib | 0-12 hours | 1.061 percentage of radioactive dose | Standard Deviation 0.22924 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Urine for Mobocertinib | 12-24 hours | 0.7462 percentage of radioactive dose | Standard Deviation 0.15716 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Urine for Mobocertinib | 24-48 hours | 0.7364 percentage of radioactive dose | Standard Deviation 0.12118 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Urine for Mobocertinib | 48-72 hours | 0.3443 percentage of radioactive dose | Standard Deviation 0.051037 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Urine for Mobocertinib | 72-96 hours | 0.2173 percentage of radioactive dose | Standard Deviation 0.040842 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Urine for Mobocertinib | 96-120 hours | 0.1425 percentage of radioactive dose | Standard Deviation 0.027883 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Urine for Mobocertinib | 120-144 hours | 0.1050 percentage of radioactive dose | Standard Deviation 0.021753 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Urine for Mobocertinib | 144-168 hours | 0.07582 percentage of radioactive dose | Standard Deviation 0.04118 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Urine for Mobocertinib | 168-192 hours | 0.07517 percentage of radioactive dose | Standard Deviation 0.012835 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Urine for Mobocertinib | 192-216 hours | 0.05243 percentage of radioactive dose | Standard Deviation 0.029772 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Urine for Mobocertinib | 216-240 hours | 0.05137 percentage of radioactive dose | Standard Deviation 0.029359 |
Primary
Period 2: Percentage of Total Radioactivity (Cum%Dose) Recovered in Feces Relative to the Administered Radioactive Dose
Time frame: Day 1 pre-dose and at multiple time points (up to 432 hours) post-dose
Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 2.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2: Percentage of Total Radioactivity (Cum%Dose) Recovered in Feces Relative to the Administered Radioactive Dose | 76.0 percentage of radioactive dose | Geometric Coefficient of Variation 6.5 |
Primary
Period 2: Percentage of Total Radioactivity (Cum%Dose) Recovered in Urine Relative to the Administered Radioactive Dose
Time frame: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 2.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2: Percentage of Total Radioactivity (Cum%Dose) Recovered in Urine Relative to the Administered Radioactive Dose | 3.57 percentage of radioactive dose | Geometric Coefficient of Variation 12.6 |
Primary
Period 2: t(1/2): Terminal Disposition Phase Half-life of Mobocertinib and Its Metabolites (AP32960 and AP32914) in Plasma and Whole Blood
Time frame: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 2.
| Arm | Measure | Group | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|---|
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2: t(1/2): Terminal Disposition Phase Half-life of Mobocertinib and Its Metabolites (AP32960 and AP32914) in Plasma and Whole Blood | Plasma: Mobocertinib | 22.8 hours | Geometric Coefficient of Variation 26.6 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2: t(1/2): Terminal Disposition Phase Half-life of Mobocertinib and Its Metabolites (AP32960 and AP32914) in Plasma and Whole Blood | Plasma: AP32960 | 30.5 hours | Geometric Coefficient of Variation 21.1 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2: t(1/2): Terminal Disposition Phase Half-life of Mobocertinib and Its Metabolites (AP32960 and AP32914) in Plasma and Whole Blood | Plasma: AP32914 | 14.0 hours | Geometric Coefficient of Variation 30.6 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2: t(1/2): Terminal Disposition Phase Half-life of Mobocertinib and Its Metabolites (AP32960 and AP32914) in Plasma and Whole Blood | Whole Blood: Mobocertinib | 20.5 hours | Geometric Coefficient of Variation 25.4 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2: t(1/2): Terminal Disposition Phase Half-life of Mobocertinib and Its Metabolites (AP32960 and AP32914) in Plasma and Whole Blood | Whole Blood: AP32960 | 30.9 hours | Geometric Coefficient of Variation 12.1 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2: t(1/2): Terminal Disposition Phase Half-life of Mobocertinib and Its Metabolites (AP32960 and AP32914) in Plasma and Whole Blood | Whole Blood: AP32914 | 12.8 hours | Geometric Coefficient of Variation 23.1 |
Primary
Period 2, t(1/2z): Terminal Disposition Phase Half-life of Plasma and Whole Blood Radioactivity Concentration Equivalents for [14C]-Mobocertinib
Time frame: Day 1 pre-dose at multiple time points (up to 240 hours) post-dose
Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 2.
| Arm | Measure | Group | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|---|
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, t(1/2z): Terminal Disposition Phase Half-life of Plasma and Whole Blood Radioactivity Concentration Equivalents for [14C]-Mobocertinib | Plasma | 281 hours | Geometric Coefficient of Variation 29.1 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, t(1/2z): Terminal Disposition Phase Half-life of Plasma and Whole Blood Radioactivity Concentration Equivalents for [14C]-Mobocertinib | Whole Blood | 301 hours | Geometric Coefficient of Variation 28.1 |
Primary
Period 2, Tmax: Time to Reach the Maximum Plasma and Whole Blood Concentration (Cmax) for Mobocertinib and Its Metabolites (AP32960 and AP32914)
Time frame: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 2.
| Arm | Measure | Group | Value (MEDIAN) |
|---|---|---|---|
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Tmax: Time to Reach the Maximum Plasma and Whole Blood Concentration (Cmax) for Mobocertinib and Its Metabolites (AP32960 and AP32914) | Plasma: Mobocertinib | 6.00 hours |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Tmax: Time to Reach the Maximum Plasma and Whole Blood Concentration (Cmax) for Mobocertinib and Its Metabolites (AP32960 and AP32914) | Plasma: AP32960 | 4.00 hours |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Tmax: Time to Reach the Maximum Plasma and Whole Blood Concentration (Cmax) for Mobocertinib and Its Metabolites (AP32960 and AP32914) | Plasma: AP32914 | 6.00 hours |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Tmax: Time to Reach the Maximum Plasma and Whole Blood Concentration (Cmax) for Mobocertinib and Its Metabolites (AP32960 and AP32914) | Whole Blood: Mobocertinib | 5.01 hours |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Tmax: Time to Reach the Maximum Plasma and Whole Blood Concentration (Cmax) for Mobocertinib and Its Metabolites (AP32960 and AP32914) | Whole Blood: AP32960 | 5.01 hours |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Tmax: Time to Reach the Maximum Plasma and Whole Blood Concentration (Cmax) for Mobocertinib and Its Metabolites (AP32960 and AP32914) | Whole Blood: AP32914 | 5.01 hours |
Primary
Period 2, Tmax: Time to Reach the Maximum Plasma and Whole Blood Radioactivity Concentration (Cmax) Equivalents for [14C]-Mobocertinib
Time frame: Day 1 pre-dose at multiple time points (up to 240 hours) post-dose
Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 2.
| Arm | Measure | Group | Value (MEDIAN) |
|---|---|---|---|
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Tmax: Time to Reach the Maximum Plasma and Whole Blood Radioactivity Concentration (Cmax) Equivalents for [14C]-Mobocertinib | Plasma | 24.0 hours |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 2, Tmax: Time to Reach the Maximum Plasma and Whole Blood Radioactivity Concentration (Cmax) Equivalents for [14C]-Mobocertinib | Whole Blood | 24.0 hours |
Secondary
Number of Participants Reporting One or More Treatment-emergent Adverse Events (TEAEs)
Time frame: Baseline up to 30 days after last dose of study drug in Period 2 (Day 41)
Population: The safety set included all participants who received at least one dose of study drug.
| Arm | Measure | Value (COUNT_OF_PARTICIPANTS) |
|---|---|---|
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Number of Participants Reporting One or More Treatment-emergent Adverse Events (TEAEs) | 6 Participants |
| [14C]-Mobocertinib 160 mg | Number of Participants Reporting One or More Treatment-emergent Adverse Events (TEAEs) | 4 Participants |
Secondary
Number of Participants With Clinically Significant Change From Baseline in 12-lead Electrocardiogram (ECG) Findings
Time frame: Baseline up to 30 days after last dose of study drug in Period 2 (Day 41)
Population: The safety set included all participants who received at least one dose of study drug.
| Arm | Measure | Value (COUNT_OF_PARTICIPANTS) |
|---|---|---|
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Number of Participants With Clinically Significant Change From Baseline in 12-lead Electrocardiogram (ECG) Findings | 0 Participants |
| [14C]-Mobocertinib 160 mg | Number of Participants With Clinically Significant Change From Baseline in 12-lead Electrocardiogram (ECG) Findings | 0 Participants |
Secondary
Number of Participants With Clinically Significant Change From Baseline in Laboratory Values
Time frame: Baseline up to 30 days after last dose of study drug in Period 2 (Day 41)
Population: The safety set included all participants who received at least one dose of study drug.
| Arm | Measure | Value (COUNT_OF_PARTICIPANTS) |
|---|---|---|
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Number of Participants With Clinically Significant Change From Baseline in Laboratory Values | 0 Participants |
| [14C]-Mobocertinib 160 mg | Number of Participants With Clinically Significant Change From Baseline in Laboratory Values | 0 Participants |
Secondary
Number of Participants With Clinically Significant Change From Baseline in Vital Signs
Time frame: Baseline up to 30 days after last dose of study drug in Period 2 (Day 41)
Population: The safety set included all participants who received at least one dose of study drug.
| Arm | Measure | Value (COUNT_OF_PARTICIPANTS) |
|---|---|---|
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Number of Participants With Clinically Significant Change From Baseline in Vital Signs | 0 Participants |
| [14C]-Mobocertinib 160 mg | Number of Participants With Clinically Significant Change From Baseline in Vital Signs | 0 Participants |
Secondary
Period 1, AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for [14C]-Mobocertinib and Its Metabolites ( [14C]-AP32960 and [14C]-AP32914) After Intravenous Administration
Time frame: Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose
Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. Here number analyzed n are the participants who were evaluable for the outcome measure at given timepoints. This OM was planned to be assessed only in Period 1.
| Arm | Measure | Group | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|---|
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 1, AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for [14C]-Mobocertinib and Its Metabolites ( [14C]-AP32960 and [14C]-AP32914) After Intravenous Administration | [14C]-Mobocertinib | 680 picogram*hour/ milliliter (pg*hr/mL) | Geometric Coefficient of Variation 30.4 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 1, AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for [14C]-Mobocertinib and Its Metabolites ( [14C]-AP32960 and [14C]-AP32914) After Intravenous Administration | [14C]- AP32960 | 187.8 picogram*hour/ milliliter (pg*hr/mL) | Geometric Coefficient of Variation 60.2 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 1, AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for [14C]-Mobocertinib and Its Metabolites ( [14C]-AP32960 and [14C]-AP32914) After Intravenous Administration | [14C]- AP32914 | 89.71 picogram*hour/ milliliter (pg*hr/mL) | — |
Secondary
Period 1, AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for Mobocertinib and Its Metabolites (AP32960 and AP32914) After Oral Administration
Time frame: Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose
Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 1.
| Arm | Measure | Group | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|---|
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 1, AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for Mobocertinib and Its Metabolites (AP32960 and AP32914) After Oral Administration | Mobocertinib | 1050 ng*hr/mL | Geometric Coefficient of Variation 64.9 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 1, AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for Mobocertinib and Its Metabolites (AP32960 and AP32914) After Oral Administration | AP32960 | 478.2 ng*hr/mL | Geometric Coefficient of Variation 30.6 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 1, AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for Mobocertinib and Its Metabolites (AP32960 and AP32914) After Oral Administration | AP32914 | 73.02 ng*hr/mL | Geometric Coefficient of Variation 53.2 |
Secondary
Period 1, AUClast: Area Under the Plasma Concentration-time Curve From Time 0 to Last Quantifiable Concentration for [14C]-Mobocertinib and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) After Intravenous Administration
Time frame: Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose
Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. Here number analyzed n are the participants who were evaluable for the outcome measure at given timepoints. This OM was planned to be assessed only in Period 1.
| Arm | Measure | Group | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|---|
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 1, AUClast: Area Under the Plasma Concentration-time Curve From Time 0 to Last Quantifiable Concentration for [14C]-Mobocertinib and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) After Intravenous Administration | [14C]-Mobocertinib | 617.9 pg*hr/mL | Geometric Coefficient of Variation 34 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 1, AUClast: Area Under the Plasma Concentration-time Curve From Time 0 to Last Quantifiable Concentration for [14C]-Mobocertinib and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) After Intravenous Administration | [14C]-AP32960 | 133.1 pg*hr/mL | Geometric Coefficient of Variation 63.1 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 1, AUClast: Area Under the Plasma Concentration-time Curve From Time 0 to Last Quantifiable Concentration for [14C]-Mobocertinib and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) After Intravenous Administration | [14C]-AP32914 | 31.52 pg*hr/mL | Geometric Coefficient of Variation 113.7 |
Secondary
Period 1, AUClast: Area Under the Plasma Concentration-time Curve From Time 0 to Last Quantifiable Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914) After Oral Administration
Time frame: Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose
Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 1.
| Arm | Measure | Group | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|---|
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 1, AUClast: Area Under the Plasma Concentration-time Curve From Time 0 to Last Quantifiable Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914) After Oral Administration | Mobocertinib | 1032 ng*hr/mL | Geometric Coefficient of Variation 65.6 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 1, AUClast: Area Under the Plasma Concentration-time Curve From Time 0 to Last Quantifiable Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914) After Oral Administration | AP32960 | 461.2 ng*hr/mL | Geometric Coefficient of Variation 30.1 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 1, AUClast: Area Under the Plasma Concentration-time Curve From Time 0 to Last Quantifiable Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914) After Oral Administration | AP32914 | 66.92 ng*hr/mL | Geometric Coefficient of Variation 53.6 |
Secondary
Period 1, AUCt: Area Under the Plasma Concentration-time Curve From Time 0 to Time t for [14C]-Mobocertinib and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) After Intravenous Administration
Time frame: Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose
Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. Here number analyzed n are the participants who were evaluable for the outcome measure at given timepoints. This OM was planned to be assessed only in Period 1.
| Arm | Measure | Group | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|---|
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 1, AUCt: Area Under the Plasma Concentration-time Curve From Time 0 to Time t for [14C]-Mobocertinib and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) After Intravenous Administration | [14C]-Mobocertinib | 617.9 picogram*hour per milliliter (pg*hr/mL) | Geometric Coefficient of Variation 34 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 1, AUCt: Area Under the Plasma Concentration-time Curve From Time 0 to Time t for [14C]-Mobocertinib and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) After Intravenous Administration | [14C]- AP32960 | 133.1 picogram*hour per milliliter (pg*hr/mL) | Geometric Coefficient of Variation 63.1 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 1, AUCt: Area Under the Plasma Concentration-time Curve From Time 0 to Time t for [14C]-Mobocertinib and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) After Intravenous Administration | [14C]- AP32914 | 31.52 picogram*hour per milliliter (pg*hr/mL) | Geometric Coefficient of Variation 113.7 |
Secondary
Period 1, Ceoi: Plasma Concentration at the End of Infusion for [14C]-Mobocertinib, and Its Metabolites ([14C]-AP32960 and [14C]-AP32914)
Time frame: Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose
Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 1.
| Arm | Measure | Group | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|---|
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 1, Ceoi: Plasma Concentration at the End of Infusion for [14C]-Mobocertinib, and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) | [14C]-Mobocertinib | 146.3 picograms per milliliter (pg /mL) | Geometric Coefficient of Variation 46.4 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 1, Ceoi: Plasma Concentration at the End of Infusion for [14C]-Mobocertinib, and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) | [14C]- AP32960 | 1.842 picograms per milliliter (pg /mL) | Geometric Coefficient of Variation 20.5 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 1, Ceoi: Plasma Concentration at the End of Infusion for [14C]-Mobocertinib, and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) | [14C]- AP32914 | 2.432 picograms per milliliter (pg /mL) | Geometric Coefficient of Variation 9.3 |
Secondary
Period 1, Cmax: Maximum Observed Plasma Concentration for [14C]-Mobocertinib and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) After Intravenous Administration
Time frame: Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose
Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 1.
| Arm | Measure | Group | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|---|
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 1, Cmax: Maximum Observed Plasma Concentration for [14C]-Mobocertinib and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) After Intravenous Administration | [14C]-mobocertinib | 148 pg/mL | Geometric Coefficient of Variation 44 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 1, Cmax: Maximum Observed Plasma Concentration for [14C]-Mobocertinib and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) After Intravenous Administration | [14C]-AP32960 | 6.631 pg/mL | Geometric Coefficient of Variation 76.4 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 1, Cmax: Maximum Observed Plasma Concentration for [14C]-Mobocertinib and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) After Intravenous Administration | [14C]-AP32914 | 3.772 pg/mL | Geometric Coefficient of Variation 33.8 |
Secondary
Period 1, Cmax: Maximum Observed Plasma Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914) After Oral Administration
Time frame: Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose
Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 1.
| Arm | Measure | Group | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|---|
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 1, Cmax: Maximum Observed Plasma Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914) After Oral Administration | Mobocertinib | 56.7 ng/mL | Geometric Coefficient of Variation 52.2 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 1, Cmax: Maximum Observed Plasma Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914) After Oral Administration | AP32960 | 23.29 ng/mL | Geometric Coefficient of Variation 21.2 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 1, Cmax: Maximum Observed Plasma Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914) After Oral Administration | AP32914 | 4.086 ng/mL | Geometric Coefficient of Variation 36 |
Secondary
Period 1, t(1/2):Terminal Disposition Phase Half-Life of Mobocertinib and Its Metabolites (AP32960 and AP32914) in Plasma After Oral, and [14C]-Mobocertinib and Its Metabolites ( [14C]-AP32960 and [14C]-AP32914) in Plasma After Intravenous Administration
Data for mobocertinib and its metabolites (AP32960 and AP32914) is reported following the oral administration, and data for \[14C\]-mobocertinib and its metabolites (\[14C\]-AP32960 and \[14C\]-AP32914) is reported following intravenous administration.
Time frame: Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose
Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. Here number analyzed n are the participants who were evaluable for the outcome measure at given timepoints. This OM was planned to be assessed only in Period 1.
| Arm | Measure | Group | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|---|
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 1, t(1/2):Terminal Disposition Phase Half-Life of Mobocertinib and Its Metabolites (AP32960 and AP32914) in Plasma After Oral, and [14C]-Mobocertinib and Its Metabolites ( [14C]-AP32960 and [14C]-AP32914) in Plasma After Intravenous Administration | [14C]- AP32914 | 11.900 hours | — |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 1, t(1/2):Terminal Disposition Phase Half-Life of Mobocertinib and Its Metabolites (AP32960 and AP32914) in Plasma After Oral, and [14C]-Mobocertinib and Its Metabolites ( [14C]-AP32960 and [14C]-AP32914) in Plasma After Intravenous Administration | Mobocertinib | 22.9 hours | Geometric Coefficient of Variation 17.9 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 1, t(1/2):Terminal Disposition Phase Half-Life of Mobocertinib and Its Metabolites (AP32960 and AP32914) in Plasma After Oral, and [14C]-Mobocertinib and Its Metabolites ( [14C]-AP32960 and [14C]-AP32914) in Plasma After Intravenous Administration | AP32960 | 29.077 hours | Geometric Coefficient of Variation 18.2 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 1, t(1/2):Terminal Disposition Phase Half-Life of Mobocertinib and Its Metabolites (AP32960 and AP32914) in Plasma After Oral, and [14C]-Mobocertinib and Its Metabolites ( [14C]-AP32960 and [14C]-AP32914) in Plasma After Intravenous Administration | AP32914 | 12.545 hours | Geometric Coefficient of Variation 37.5 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 1, t(1/2):Terminal Disposition Phase Half-Life of Mobocertinib and Its Metabolites (AP32960 and AP32914) in Plasma After Oral, and [14C]-Mobocertinib and Its Metabolites ( [14C]-AP32960 and [14C]-AP32914) in Plasma After Intravenous Administration | [14C]-Mobocertinib | 22.2 hours | Geometric Coefficient of Variation 41.3 |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 1, t(1/2):Terminal Disposition Phase Half-Life of Mobocertinib and Its Metabolites (AP32960 and AP32914) in Plasma After Oral, and [14C]-Mobocertinib and Its Metabolites ( [14C]-AP32960 and [14C]-AP32914) in Plasma After Intravenous Administration | [14C]- AP32960 | 20.317 hours | Geometric Coefficient of Variation 39.1 |
Secondary
Period 1, Time to Reach the Maximum Plasma Concentration (Cmax) for Mobocertinib and Its Metabolites (AP32960 and AP32914) After Oral, and [14C]-Mobocertinib and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) After Intravenous Administration
Data for mobocertinib and its metabolites (AP32960 and AP32914) is reported following the oral administration, and data for \[14C\]-mobocertinib and its metabolites (\[14C\]-AP32960 and \[14C\]-AP32914) is reported following intravenous administration.
Time frame: Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose
Population: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 1.
| Arm | Measure | Group | Value (MEDIAN) |
|---|---|---|---|
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 1, Time to Reach the Maximum Plasma Concentration (Cmax) for Mobocertinib and Its Metabolites (AP32960 and AP32914) After Oral, and [14C]-Mobocertinib and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) After Intravenous Administration | Mobocertinib | 5.00 hours |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 1, Time to Reach the Maximum Plasma Concentration (Cmax) for Mobocertinib and Its Metabolites (AP32960 and AP32914) After Oral, and [14C]-Mobocertinib and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) After Intravenous Administration | AP32960 | 4.502 hours |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 1, Time to Reach the Maximum Plasma Concentration (Cmax) for Mobocertinib and Its Metabolites (AP32960 and AP32914) After Oral, and [14C]-Mobocertinib and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) After Intravenous Administration | AP32914 | 5.000 hours |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 1, Time to Reach the Maximum Plasma Concentration (Cmax) for Mobocertinib and Its Metabolites (AP32960 and AP32914) After Oral, and [14C]-Mobocertinib and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) After Intravenous Administration | [14C]-mobocertinib | 0.26 hours |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 1, Time to Reach the Maximum Plasma Concentration (Cmax) for Mobocertinib and Its Metabolites (AP32960 and AP32914) After Oral, and [14C]-Mobocertinib and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) After Intravenous Administration | [14C]- AP32960 | 3.257 hours |
| Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg | Period 1, Time to Reach the Maximum Plasma Concentration (Cmax) for Mobocertinib and Its Metabolites (AP32960 and AP32914) After Oral, and [14C]-Mobocertinib and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) After Intravenous Administration | [14C]- AP32914 | 2.26 hours |