A Study in Healthy Adult Male Participants to Assess Absorption, Distribution, Metabolism and Excretion (ADME) of Radiolabeled PF-06865571.

A PHASE 1, OPEN-LABEL, FIXED-SEQUENCE, 2-PERIOD STUDY IN HEALTHY ADULT MALE PARTICIPANTS TO ASSESS THE EXTENT OF EXCRETION, ABSOLUTE BIOAVAILABILITY, FRACTION ABSORBED, AND PHARMACOKINETICS OF [14C]PF-06865571 USING A 14C-MICROTRACER APPROACH

Status

Completed

Phases

Phase 1

Study type

Interventional

Source

ClinicalTrials.gov

Registry ID

NCT04866225

Enrollment

Registered

2021-04-29

Start date

2021-05-11

Completion date

2021-08-06

Last updated

2024-07-31

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

Conditions

Healthy Participants

Keywords

ADME

Brief summary

This study is a Phase 1, open-label, non-randomized, 2-period, fixed-sequence, single-dose study of PF-06865571 in healthy male participants to characterize the ADME properties of \[14C\]PF-06865571 following oral administration; and to evaluate the absolute oral bioavailability (F) and fraction absorbed (Fa) of PF-06865571 following oral administration of unlabeled PF-06865571 and IV administration of \[14C\]PF-06865571.

Interventions

DRUGOral [14C]PF-06865571

Oral radiolabeled PF-06865571

DRUGOral PF-06865571

Oral PF-06865571

DRUGIV [14C]PF-06865571

IV radiolabeled PF-06865571

Study design

Allocation

NON_RANDOMIZED

Intervention model

SEQUENTIAL

Primary purpose

BASIC_SCIENCE

Masking

NONE

Eligibility

Sex/Gender

MALE

Age

18 Years to 60 Years

Healthy volunteers

Yes

Inclusion criteria

* Male participants, 18 to 60 years of age, inclusive, at the time of signing the informed consent document. * Male participants who are overtly healthy as determined by medical evaluation including medical history, physical examination, laboratory tests, and cardiac tests. * Participants who are nonsmoking for at least 3 months at the time of signing the informed consent document. * BMI of 17.5 to 30.4 kg/m2, inclusive; and a total body weight \>50 kg (110 lb).

Exclusion criteria

* Any condition possibly affecting drug absorption (eg, gastrectomy, cholecystectomy). * History of irregular bowel movements including irritable bowel syndrome or frequent episodes of diarrhea or constipation, defined by less than 1 bowel movement on average per 2 days, or lactose intolerance. * History of HIV infection, hepatitis B, or hepatitis C; positive testing for HIV, HBsAg,or HCVAb. Hepatitis B vaccination is allowed. * History of SARS-CoV-2 PCR or antibody (eg, IgG, IgM, etc) positive result would necessitate accompanying history of asymptomatic state for at least 6 months prior to screening. * Use of prescription or nonprescription drugs. * Previous administration with an unapproved drug within 60 days preceding the first dose of study intervention used in this study. * A positive urine drug test. * A positive urine cotinine test. * A positive COVID-19 (SARS-CoV-2) PCR test. * Blood donation (excluding plasma donations) of approximately 1 pint (500 mL) or more within 60 days prior to dosing.

Design outcomes

Primary

Measure	Time frame	Description
Total Recovery of Radioactivity in Urine as Percentage of Total Radioactive Dose of PF-06865571 Administered	Period 1: Day -1 to maximum Day 21; Period 2: Day 1 to maximum Day 3	The total recovery of radioactivity in urine was listed and summarized using descriptive statistics. In this outcome measure, the percentages of dose excreted in urine in Period 1 and Period 2 were reported.
Total Recovery of Radioactivity in Feces as Percentage of Total Radioactive Dose of PF-06865571 Administered	Period 1: Day -1 to maximum Day 21; Period 2: Day 1 to maximum Day 3	The total recovery of radioactivity in feces was listed and summarized using descriptive statistics. In this outcome measure, the percentages of dose excreted in feces in Period 1 and Period 2 were reported.
Total Recovery of Radioactivity in Total Excreta (Urine + Feces) as Percentage of Total Radioactive Dose of PF-06865571 Administered	Period 1: Day -1 to maximum Day 21; Period 2: Day 1 to maximum Day 3	The total recovery of radioactivity in the combination of urine and feces was listed and summarized using descriptive statistics. In this outcome measure, the percentages of dose excreted in total excreta (urine + feces) in Period 1 and Period 2 were reported.
Relative Abundance (Mean Value) of Radiolabeled PF-06865571 in Plasma in Period 1	Period 1: 0, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose (Day 1 to Day 6)	Plasma samples were analyzed for radiolabeled PF-06865571 and its metabolites. \[14C\]PF-06865571 and the major metabolites in plasma, after oral administration of 300 mg \[14C\]PF-06865571 were identified. In this outcome measure, relative abundance of radiolabeled PF-06865571 in plasma based on \[14C\] quantitation was reported. The measure type was the mean value based on pooled sampling, which means blood samples from the 6 participants were pooled together and then analyzed as 1 sample, thus the confidence interval could not be calculated. Therefore, Number is selected as the Measure Type.
Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Plasma in Period 1	Period 1: 0, 0.5, 3, 6, 12, 24, 36, 48, 72, 96 and 120 hours post-dose (Day 1 to Day 6)	Plasma samples were analyzed for radiolabeled PF-06865571 and its metabolites. \[14C\]PF-06865571 and the major metabolites in plasma, after oral administration of 300 mg \[14C\]PF-06865571 were identified. In this outcome measure, relative abundance of the metabolites of \[14C\]PF-06865571 in plasma based on \[14C\] quantitation was reported. The metabolites included 487, 391, 412, 556, M6 (PF-07822633), M7 (PF-07911964), 584, M1 (PF-06878236), 426, M4 (PF-06887477), 600, M5 (PF-06885984) and M2 (PF-06868609). The measure type was the mean value based on pooled sampling, which means blood samples from the 6 participants were pooled together and then analyzed as 1 sample, thus the confidence interval could not be calculated. Therefore, Number is selected as the Measure Type.
Relative Abundance (Mean Value) of Radiolabeled PF-06865571 in Urine in Period 1	Period 1: Day -1 to maximum Day 21	Urine samples were analyzed for radiolabeled PF-06865571 and its metabolites. \[14C\]PF-06865571 and the major metabolites in urine, after oral administration of 300 mg \[14C\]PF-06865571 were identified. In this outcome measure, relative abundance of radiolabeled PF-06865571 in urine based on \[14C\] quantitation was reported. The measure type was the mean value based on pooled sampling, which means blood samples from the 6 participants were pooled together and then analyzed as 1 sample, thus the confidence interval could not be calculated. Therefore, Number is selected as the Measure Type.
Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Urine in Period 1	Period 1: Day -1 to maximum Day 21	Urine samples were analyzed for radiolabeled PF-06865571 and its metabolites. \[14C\]PF-06865571 and the major metabolites in urine, after oral administration of 300 mg \[14C\]PF-06865571 were identified. In this outcome measure, relative abundance of the metabolites of \[14C\]PF-06865571 in urine based on \[14C\] quantitation was reported. The metabolites included 487, 391, 412, 556, M6 (PF-07822633), M7 (PF-07911964), 584, M1 (PF-06878236), 426, M4 (PF-06887477), 600, M5 (PF-06885984) and M2 (PF-06868609). The measure type was the mean value based on pooled sampling, which means blood samples from the 6 participants were pooled together and then analyzed as 1 sample, thus the confidence interval could not be calculated. Therefore, Number is selected as the Measure Type.
Relative Abundance (Mean Value) of Radiolabeled PF-06865571 in Feces in Period 1	Period 1: Day -1 to maximum Day 21	Fecal samples were analyzed for radiolabeled PF-06865571 and its metabolites. \[14C\]PF-06865571 and the major metabolites in feces, after oral administration of 300 mg \[14C\]PF-06865571 were identified. In this outcome measure, relative abundance of radiolabeled PF-06865571 in feces based on \[14C\] quantitation was reported. The measure type was the mean value based on pooled sampling, which means blood samples from the 6 participants were pooled together and then analyzed as 1 sample, thus the confidence interval could not be calculated. Therefore, Number is selected as the Measure Type.
Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Feces in Period 1	Period 1: Day -1 to maximum Day 21	Fecal samples were analyzed for radiolabeled PF-06865571 and its metabolites. \[14C\]PF-06865571 and the major metabolites in feces, after oral administration of 300 mg \[14C\]PF-06865571 were identified. In this outcome measure, relative abundance of the metabolites of \[14C\]PF-06865571 in feces based on \[14C\] quantitation was reported. The metabolites included 487, 391, 412, 556, M6 (PF-07822633), M7 (PF-07911964), 584, M1 (PF-06878236), 426, M4 (PF-06887477), 600, M5 (PF-06885984) and M2 (PF-06868609). The measure type was the mean value based on pooled sampling, which means blood samples from the 6 participants were pooled together and then analyzed as 1 sample, thus the confidence interval could not be calculated. Therefore, Number is selected as the Measure Type.

Secondary

Measure	Time frame	Description
t1/2 of Oral PF-06865571 in Plasma in Period 1	Period 1: 0, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose (Day 1 to Day 6)	Terminal elimination half-life (t1/2) was the time measured for the plasma concentration to decrease by one half. The determination method of t1/2 was loge(2)/kel, where kel was the terminal phase rate constant calculated by a linear regression of the log-linear concentration-time curve.
AUClast of Intravenous (IV) Radiolabeled PF-06865571 in Plasma in Period 2	Period 2: -3, 0, 0.08, 0.17, 0.25, 0.5, 0.75, 1, 3, 6, 9, 13, 21, 33 and 45 hours post-dose (Day 1 to Day 3)	AUClast is defined as area under the plasma concentration-time profile from time zero to time of the last quantifiable concentration (Clast). The determination method of AUClast was linear/log trapezoidal rule.
Cmax of IV Radiolabeled PF-06865571 in Plasma in Period 2	Period 2: -3, 0, 0.08, 0.17, 0.25, 0.5, 0.75, 1, 3, 6, 9, 13, 21, 33 and 45 hours post-dose (Day 1 to Day 3)	Cmax is defined as maximum plasma concentration. The determination method of Cmax was observing directly from data.
Tmax of IV Radiolabeled PF-06865571 in Plasma in Period 2	Period 2: -3, 0, 0.08, 0.17, 0.25, 0.5, 0.75, 1, 3, 6, 9, 13, 21, 33 and 45 hours post-dose (Day 1 to Day 3)	Tmax is defined as time to reach maximum observed plasma concentration. The determination method of Tmax was observing directly from data as time of first occurrence.
t1/2 of IV Radiolabeled PF-06865571 in Plasma in Period 2	Period 2: -3, 0, 0.08, 0.17, 0.25, 0.5, 0.75, 1, 3, 6, 9, 13, 21, 33 and 45 hours post-dose (Day 1 to Day 3)	Terminal elimination half-life (t1/2) was the time measured for the plasma concentration to decrease by one half. The determination method of t1/2 was loge(2)/kel, where kel was the terminal phase rate constant calculated by a linear regression of the log-linear concentration-time curve.
AUCinf of IV Radiolabeled PF-06865571 in Plasma in Period 2	Period 2: -3, 0, 0.08, 0.17, 0.25, 0.5, 0.75, 1, 3, 6, 9, 13, 21, 33 and 45 hours post-dose (Day 1 to Day 3)	AUCinf = Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0-inf). The determination method of AUCinf was AUClast + (Clast\/ kel), where Clast\ was the predicted plasma concentration at the last quantifiable time point estimated from the log-linear regression analysis, kel was the terminal phase rate constant.
Systemic Clearance (CL) of IV Radiolabeled PF-06865571 in Plasma in Period 2	Period 2: -3, 0, 0.08, 0.17, 0.25, 0.5, 0.75, 1, 3, 6, 9, 13, 21, 33 and 45 hours post-dose (Day 1 to Day 3)	CL is a quantitative measure of the rate at which a drug substance is removed from the body. The determination method of CL was dose/AUCinf.
Area Under the Plasma Concentration-time Profile From Time Zero to Time of The Last Quantifiable Concentration (AUClast) of Total Radioactivity of [14C]PF-06865571 in Plasma in Period 1	Period 1: 0, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose (Day 1 to Day 6)	AUClast is defined as area under the plasma concentration-time profile from time zero to time of the last quantifiable concentration (Clast). The determination method of AUClast was linear/log trapezoidal rule.
Dose-Normalized AUCinf (AUCinf[dn]) of Oral Unlabeled PF-06865571 in Plasma in Period 2	Period 2: -3, 0, 0.08, 0.17, 0.25, 0.5, 0.75, 1, 3, 6, 9, 13, 21, 33 and 45 hours post-dose (Day 1 to Day 3)	AUCinf = Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0-inf). It is obtained from AUC (0-t) plus AUC (t-inf). AUCinf(dn) is defined as dose normalized (to 1 mg equivalent) AUCinf, which equals to AUCinf/Dose.
AUCinf(dn) of IV Microtracer of Radiolabeled PF-06865571 in Plasma in Period 2	Period 2: -3, 0, 0.08, 0.17, 0.25, 0.5, 0.75, 1, 3, 6, 9, 13, 21, 33 and 45 hours post-dose (Day 1 to Day 3)	AUCinf = Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0-inf). It is obtained from AUC (0-t) plus AUC (t-inf). AUCinf(dn) is defined as dose normalized (to 1 mg equivalent) AUCinf, which equals to AUCinf/Dose.
Absolute Oral Bioavailability (F) of Oral Unlabeled and IV Radiolabeled PF-06865571 for Plasma AUCinf(dn) in Period 2	Period 2: -3, 0, 0.08, 0.17, 0.25, 0.5, 0.75, 1, 3, 6, 9, 13, 21, 33 and 45 hours post-dose (Day 1 to Day 3)	Absolute Oral Bioavailability (F) provided information on the amount of PF-06865571 reaching the systemic circulation. F was estimated as the ratio of adjusted geometric means of dose-normalized AUCinf for oral unlabeled PF-06865571 and IV labeled 14C PF-06865571 in plasma (from Period 2 only) which was equivalent to the following equation: F = \[PF-06865571\_AUCpo/\[14C\]PF-06865571\_AUCiv\]×\[ \[14C\]PF-06865571\_Doseiv/ PF-06865571\_Dosepo\], where PF-06865571\_AUCpo = AUCinf(dn) of oral unlabeled PF-06865571, \[14C\]PF-06865571\_AUCiv = AUCinf(dn) of intravenous radiolabeled PF-06865571, \[14C\]PF-06865571\_Doseiv = dose of intravenous radiolabeled PF-06865571, PF-06865571\_Dosepo = dose of oral unlabeled PF-06865571.
Percentage of Total 14C in Urine Following Oral Administration (%14C_Urine_PO) of Radiolabeled PF-06865571 in Period 1	Period 1: up to 48 hours post-dose (Day 1 to Day 3)	%14C\_Urine\_PO is defined as percentage of the radioactive dose administered that is excreted in the urine following oral administration. %14C\_Urine\_PO = Total 14C\_Urine\_PO/14C Dosepo × 100, where PO = orally, Total 14C\_Urine\_PO = total radioactivity excreted into the urine post-dose following oral administration of \[14C\]PF-06865571, 14C Dosepo = dose of 14C following oral administration of \[14C\]PF-06865571.
Percentage of Total 14C in Urine Following IV Microtracer Administration (%14C_Urine_IV) of Radiolabeled PF-06865571 in Period 2	Period 2: up to 48 hours post-dose (Day 1 to Day 3)	%14C\_Urine\_IV is defined as percentage of the radioactive dose administered that is excreted in the urine following IV administration. %14C\_Urine\_IV = Total 14C \_Urine\_IV/14C Doseiv × 100, where IV = intravenous, Total 14C\_Urine\_IV = total radioactivity excreted into the urine following IV administration of \[14C\]PF 06865571, 14C Doseiv = dose of 14C following IV administration of \[14C\]PF 06865571.
Fraction Absorbed (Fa) for Percentage of Excretion of Total 14C in Urine for Oral and IV Radiolabeled PF-06865571	Period 1 and Period 2: up to 48 hours post-dose (Day 1 to Day 3)	Determination of the Fraction Absorbed (Fa) (obtained from Periods 1 and 2) provided information on the fraction of the total PF-06865571 dose absorbed, regardless of the fate of that dose after absorption (ie, metabolism, degradation, etc). Fa was estimated as the ratio of the adjusted geometric means of % of administered radioactive dose excreted into the urine following oral and IV administration of \[14C\]PF-06865571 microtracer dose over the same collection time (up to 48 hours post dose) in Periods 1 and 2, respectively: Fa = \[% 14C\_Urine\_PO/% 14C\_Urine\_IV\].
Steady State Volume of Distribution (Vss) of IV Radiolabeled PF-06865571 in Plasma in Period 2	Period 2: -3, 0, 0.08, 0.17, 0.25, 0.5, 0.75, 1, 3, 6, 9, 13, 21, 33 and 45 hours post-dose (Day 1 to Day 3)	Volume of distribution is defined as the theoretical volume in which the total amount of drug would need to be uniformly distributed to produce the desired blood concentration of a drug. Vss is the apparent volume of distribution at steady-state.
Maximum Plasma Concentration (Cmax) of Total Radioactivity of [14C]PF-06865571 in Plasma in Period 1	Period 1: 0, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose (Day 1 to Day 6)	Cmax is defined as maximum plasma concentration. The determination method of Cmax was observing directly from data.
Time for Cmax (Tmax) of Total Radioactivity of [14C]PF-06865571 in Plasma in Period 1	Period 1: 0, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose (Day 1 to Day 6)	Tmax is defined as time to reach maximum observed plasma concentration. The determination method of Tmax was observing directly from data as time of first occurrence.
Area Under the Plasma Concentration Time Profile From Time Zero Extrapolated to Infinite Time (AUCinf) of Total Radioactivity of [14C]PF-06865571 in Plasma in Period 1	Period 1: 0, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose (Day 1 to Day 6)	AUCinf = Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0-inf). The determination method of AUCinf was AUClast + (Clast\/ kel), where Clast\ was the predicted plasma concentration at the last quantifiable time point estimated from the log-linear regression analysis, kel was the terminal phase rate constant.
Terminal Elimination Half-life (t1/2) of Total Radioactivity of [14C]PF-06865571 in Plasma in Period 1	Period 1: 0, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose (Day 1 to Day 6)	Terminal elimination half-life (t1/2) was the time measured for the plasma concentration to decrease by one half. The determination method of t1/2 was loge(2)/kel, where kel was the terminal phase rate constant calculated by a linear regression of the log-linear concentration-time curve.
AUClast of Oral PF-06865571 in Plasma in Period 1	Period 1: 0, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose (Day 1 to Day 6)	AUClast is defined as area under the plasma concentration-time profile from time zero to time of the last quantifiable concentration (Clast). The determination method of AUClast was linear/log trapezoidal rule.
Cmax of Oral PF-06865571 in Plasma in Period 1	Period 1: 0, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose (Day 1 to Day 6)	Cmax is defined as maximum plasma concentration. The determination method of Cmax was observing directly from data.
Tmax of Oral PF-06865571 in Plasma in Period 1	Period 1: 0, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose (Day 1 to Day 6)	Tmax is defined as time to reach maximum observed plasma concentration. The determination method of Tmax was observing directly from data as time of first occurrence.
AUCinf of Oral PF-06865571 in Plasma in Period 1	Period 1: 0, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose (Day 1 to Day 6)	AUCinf = Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0-inf). The determination method of AUCinf was AUClast + (Clast\/ kel), where Clast\ was the predicted plasma concentration at the last quantifiable time point estimated from the log-linear regression analysis, kel was the terminal phase rate constant.

Countries

United States

Participant flow

Participants by arm

Arm	Count
Period 1:[14C]PF-06865571 300 mg Oral; Period 2:PF-06865571 300 mg Oral & [14C]PF-06865571 100 μg IV Six healthy male participants were enrolled and received 2 regimens (A and B) in Periods 1 and 2, respectively. For regimen A in Period 1, an oral dose of 300 mg PF-06865571 containing approximately 300 nCi 14C (ie, radiolabeled PF-06865571) was administered. For regimen B in Period 2, an oral dose of 300 mg unlabeled PF-06865571 followed by an intravenous (IV) dose of 300 nCi \[14C\] in 100 μg of PF-06865571 was administered.	6
Total	6

Arm

Count

Period 1:[14C]PF-06865571 300 mg Oral; Period 2:PF-06865571 300 mg Oral & [14C]PF-06865571 100 μg IV

Six healthy male participants were enrolled and received 2 regimens (A and B) in Periods 1 and 2, respectively. For regimen A in Period 1, an oral dose of 300 mg PF-06865571 containing approximately 300 nCi 14C (ie, radiolabeled PF-06865571) was administered. For regimen B in Period 2, an oral dose of 300 mg unlabeled PF-06865571 followed by an intravenous (IV) dose of 300 nCi \[14C\] in 100 μg of PF-06865571 was administered.

Total

Baseline characteristics

Characteristic	Period 1:[14C]PF-06865571 300 mg Oral; Period 2:PF-06865571 300 mg Oral & [14C]PF-06865571 100 μg IV
Age, Continuous Mean	42.0 Years STANDARD_DEVIATION 13.9
Age, Customized 18-25 years	1 Participants
Age, Customized <18 years	0 Participants
Age, Customized 26-35 years	1 Participants
Age, Customized 36-45 years	1 Participants
Age, Customized >45 years	3 Participants
Ethnicity (NIH/OMB) Hispanic or Latino	2 Participants
Ethnicity (NIH/OMB) Not Hispanic or Latino	4 Participants
Ethnicity (NIH/OMB) Unknown or Not Reported	0 Participants
Race/Ethnicity, Customized Black or African American	2 Participants
Race/Ethnicity, Customized White	4 Participants
Sex: Female, Male Female	0 Participants
Sex: Female, Male Male	6 Participants

Adverse events

Event type	EG000 affected / at risk	EG001 affected / at risk
deaths Total, all-cause mortality	0 / 6	0 / 6
other Total, other adverse events	4 / 6	0 / 6
serious Total, serious adverse events	0 / 6	0 / 6

Outcome results

Primary

Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Feces in Period 1

Fecal samples were analyzed for radiolabeled PF-06865571 and its metabolites. \[14C\]PF-06865571 and the major metabolites in feces, after oral administration of 300 mg \[14C\]PF-06865571 were identified. In this outcome measure, relative abundance of the metabolites of \[14C\]PF-06865571 in feces based on \[14C\] quantitation was reported. The metabolites included 487, 391, 412, 556, M6 (PF-07822633), M7 (PF-07911964), 584, M1 (PF-06878236), 426, M4 (PF-06887477), 600, M5 (PF-06885984) and M2 (PF-06868609). The measure type was the mean value based on pooled sampling, which means blood samples from the 6 participants were pooled together and then analyzed as 1 sample, thus the confidence interval could not be calculated. Therefore, Number is selected as the Measure Type.

Time frame: Period 1: Day -1 to maximum Day 21

Population: Analysis population included all participants assigned to study intervention and who took at least 1 dose of study intervention.

Arm	Measure	Group	Value (NUMBER)
[14C]PF-06865571 300 mg Oral	Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Feces in Period 1	412	1.1 Percentage of Radioactivity in Feces
[14C]PF-06865571 300 mg Oral	Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Feces in Period 1	556	0 Percentage of Radioactivity in Feces
[14C]PF-06865571 300 mg Oral	Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Feces in Period 1	M6 (PF-07822633)	0 Percentage of Radioactivity in Feces
[14C]PF-06865571 300 mg Oral	Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Feces in Period 1	M7 (PF-07911964)	21.0 Percentage of Radioactivity in Feces
[14C]PF-06865571 300 mg Oral	Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Feces in Period 1	584	0 Percentage of Radioactivity in Feces
[14C]PF-06865571 300 mg Oral	Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Feces in Period 1	M4 (PF-06887477)	33.2 Percentage of Radioactivity in Feces
[14C]PF-06865571 300 mg Oral	Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Feces in Period 1	600	0 Percentage of Radioactivity in Feces
[14C]PF-06865571 300 mg Oral	Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Feces in Period 1	M5 (PF-06885984)	0 Percentage of Radioactivity in Feces
[14C]PF-06865571 300 mg Oral	Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Feces in Period 1	M2 (PF-06868609)	23.1 Percentage of Radioactivity in Feces
[14C]PF-06865571 300 mg Oral	Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Feces in Period 1	487	0 Percentage of Radioactivity in Feces
[14C]PF-06865571 300 mg Oral	Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Feces in Period 1	391	0 Percentage of Radioactivity in Feces
[14C]PF-06865571 300 mg Oral	Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Feces in Period 1	M1 (PF-06878236)	15.0 Percentage of Radioactivity in Feces
[14C]PF-06865571 300 mg Oral	Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Feces in Period 1	426	33.2 Percentage of Radioactivity in Feces

Primary

Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Plasma in Period 1

Plasma samples were analyzed for radiolabeled PF-06865571 and its metabolites. \[14C\]PF-06865571 and the major metabolites in plasma, after oral administration of 300 mg \[14C\]PF-06865571 were identified. In this outcome measure, relative abundance of the metabolites of \[14C\]PF-06865571 in plasma based on \[14C\] quantitation was reported. The metabolites included 487, 391, 412, 556, M6 (PF-07822633), M7 (PF-07911964), 584, M1 (PF-06878236), 426, M4 (PF-06887477), 600, M5 (PF-06885984) and M2 (PF-06868609). The measure type was the mean value based on pooled sampling, which means blood samples from the 6 participants were pooled together and then analyzed as 1 sample, thus the confidence interval could not be calculated. Therefore, Number is selected as the Measure Type.

Time frame: Period 1: 0, 0.5, 3, 6, 12, 24, 36, 48, 72, 96 and 120 hours post-dose (Day 1 to Day 6)

Population: Analysis population included all participants assigned to study intervention and who took at least 1 dose of study intervention.

Arm	Measure	Group	Value (NUMBER)
[14C]PF-06865571 300 mg Oral	Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Plasma in Period 1	487	0 Percentage of Radioactivity in Plasma
[14C]PF-06865571 300 mg Oral	Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Plasma in Period 1	391	3.0 Percentage of Radioactivity in Plasma
[14C]PF-06865571 300 mg Oral	Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Plasma in Period 1	412	0 Percentage of Radioactivity in Plasma
[14C]PF-06865571 300 mg Oral	Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Plasma in Period 1	556	2.7 Percentage of Radioactivity in Plasma
[14C]PF-06865571 300 mg Oral	Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Plasma in Period 1	M6 (PF-07822633)	11.3 Percentage of Radioactivity in Plasma
[14C]PF-06865571 300 mg Oral	Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Plasma in Period 1	M7 (PF-07911964)	0.01 Percentage of Radioactivity in Plasma
[14C]PF-06865571 300 mg Oral	Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Plasma in Period 1	584	1.1 Percentage of Radioactivity in Plasma
[14C]PF-06865571 300 mg Oral	Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Plasma in Period 1	M1 (PF-06878236)	0 Percentage of Radioactivity in Plasma
[14C]PF-06865571 300 mg Oral	Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Plasma in Period 1	426	1.5 Percentage of Radioactivity in Plasma
[14C]PF-06865571 300 mg Oral	Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Plasma in Period 1	M4 (PF-06887477)	1.5 Percentage of Radioactivity in Plasma
[14C]PF-06865571 300 mg Oral	Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Plasma in Period 1	600	0 Percentage of Radioactivity in Plasma
[14C]PF-06865571 300 mg Oral	Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Plasma in Period 1	M5 (PF-06885984)	0 Percentage of Radioactivity in Plasma
[14C]PF-06865571 300 mg Oral	Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Plasma in Period 1	M2 (PF-06868609)	36.6 Percentage of Radioactivity in Plasma

Primary

Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Urine in Period 1

Urine samples were analyzed for radiolabeled PF-06865571 and its metabolites. \[14C\]PF-06865571 and the major metabolites in urine, after oral administration of 300 mg \[14C\]PF-06865571 were identified. In this outcome measure, relative abundance of the metabolites of \[14C\]PF-06865571 in urine based on \[14C\] quantitation was reported. The metabolites included 487, 391, 412, 556, M6 (PF-07822633), M7 (PF-07911964), 584, M1 (PF-06878236), 426, M4 (PF-06887477), 600, M5 (PF-06885984) and M2 (PF-06868609). The measure type was the mean value based on pooled sampling, which means blood samples from the 6 participants were pooled together and then analyzed as 1 sample, thus the confidence interval could not be calculated. Therefore, Number is selected as the Measure Type.

Time frame: Period 1: Day -1 to maximum Day 21

Population: Analysis population included all participants assigned to study intervention and who took at least 1 dose of study intervention.

Arm	Measure	Group	Value (NUMBER)
[14C]PF-06865571 300 mg Oral	Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Urine in Period 1	412	0 Percentage of Radioactivity in Urine
[14C]PF-06865571 300 mg Oral	Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Urine in Period 1	M6 (PF-07822633)	23.3 Percentage of Radioactivity in Urine
[14C]PF-06865571 300 mg Oral	Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Urine in Period 1	M1 (PF-06878236)	0.7 Percentage of Radioactivity in Urine
[14C]PF-06865571 300 mg Oral	Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Urine in Period 1	556	4.7 Percentage of Radioactivity in Urine
[14C]PF-06865571 300 mg Oral	Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Urine in Period 1	M7 (PF-07911964)	23.3 Percentage of Radioactivity in Urine
[14C]PF-06865571 300 mg Oral	Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Urine in Period 1	584	23.3 Percentage of Radioactivity in Urine
[14C]PF-06865571 300 mg Oral	Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Urine in Period 1	426	4.2 Percentage of Radioactivity in Urine
[14C]PF-06865571 300 mg Oral	Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Urine in Period 1	M4 (PF-06887477)	4.2 Percentage of Radioactivity in Urine
[14C]PF-06865571 300 mg Oral	Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Urine in Period 1	600	1.4 Percentage of Radioactivity in Urine
[14C]PF-06865571 300 mg Oral	Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Urine in Period 1	M5 (PF-06885984)	1.4 Percentage of Radioactivity in Urine
[14C]PF-06865571 300 mg Oral	Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Urine in Period 1	M2 (PF-06868609)	50.9 Percentage of Radioactivity in Urine
[14C]PF-06865571 300 mg Oral	Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Urine in Period 1	487	2.0 Percentage of Radioactivity in Urine
[14C]PF-06865571 300 mg Oral	Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Urine in Period 1	391	6.0 Percentage of Radioactivity in Urine

Primary

Relative Abundance (Mean Value) of Radiolabeled PF-06865571 in Feces in Period 1

Fecal samples were analyzed for radiolabeled PF-06865571 and its metabolites. \[14C\]PF-06865571 and the major metabolites in feces, after oral administration of 300 mg \[14C\]PF-06865571 were identified. In this outcome measure, relative abundance of radiolabeled PF-06865571 in feces based on \[14C\] quantitation was reported. The measure type was the mean value based on pooled sampling, which means blood samples from the 6 participants were pooled together and then analyzed as 1 sample, thus the confidence interval could not be calculated. Therefore, Number is selected as the Measure Type.

Time frame: Period 1: Day -1 to maximum Day 21

Population: Analysis population included all participants assigned to study intervention and who took at least 1 dose of study intervention.

Arm	Measure	Value (NUMBER)
[14C]PF-06865571 300 mg Oral	Relative Abundance (Mean Value) of Radiolabeled PF-06865571 in Feces in Period 1	4.1 Percentage of Radioactivity in Feces

Primary

Relative Abundance (Mean Value) of Radiolabeled PF-06865571 in Plasma in Period 1

Plasma samples were analyzed for radiolabeled PF-06865571 and its metabolites. \[14C\]PF-06865571 and the major metabolites in plasma, after oral administration of 300 mg \[14C\]PF-06865571 were identified. In this outcome measure, relative abundance of radiolabeled PF-06865571 in plasma based on \[14C\] quantitation was reported. The measure type was the mean value based on pooled sampling, which means blood samples from the 6 participants were pooled together and then analyzed as 1 sample, thus the confidence interval could not be calculated. Therefore, Number is selected as the Measure Type.

Time frame: Period 1: 0, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose (Day 1 to Day 6)

Population: Analysis population included all participants assigned to study intervention and who took at least 1 dose of study intervention.

Arm	Measure	Value (NUMBER)
[14C]PF-06865571 300 mg Oral	Relative Abundance (Mean Value) of Radiolabeled PF-06865571 in Plasma in Period 1	43.8 Percentage of Radioactivity in Plasma

Primary

Relative Abundance (Mean Value) of Radiolabeled PF-06865571 in Urine in Period 1

Urine samples were analyzed for radiolabeled PF-06865571 and its metabolites. \[14C\]PF-06865571 and the major metabolites in urine, after oral administration of 300 mg \[14C\]PF-06865571 were identified. In this outcome measure, relative abundance of radiolabeled PF-06865571 in urine based on \[14C\] quantitation was reported. The measure type was the mean value based on pooled sampling, which means blood samples from the 6 participants were pooled together and then analyzed as 1 sample, thus the confidence interval could not be calculated. Therefore, Number is selected as the Measure Type.

Time frame: Period 1: Day -1 to maximum Day 21

Population: Analysis population included all participants assigned to study intervention and who took at least 1 dose of study intervention.

Arm	Measure	Value (NUMBER)
[14C]PF-06865571 300 mg Oral	Relative Abundance (Mean Value) of Radiolabeled PF-06865571 in Urine in Period 1	2.7 Percentage of Radioactivity in Urine

Primary

Total Recovery of Radioactivity in Feces as Percentage of Total Radioactive Dose of PF-06865571 Administered

The total recovery of radioactivity in feces was listed and summarized using descriptive statistics. In this outcome measure, the percentages of dose excreted in feces in Period 1 and Period 2 were reported.

Time frame: Period 1: Day -1 to maximum Day 21; Period 2: Day 1 to maximum Day 3

Population: Analysis population included all participants who received 1 dose of \[14C\]PF-06865571 and who have evaluable total radioactivity concentration (urinary and fecal) data and who had no protocol deviations or AEs (such as vomiting of the dose, diarrhoea or severe constipation) that may have affected the extent of excretion analysis.

Arm	Measure	Value (MEAN)	Dispersion
[14C]PF-06865571 300 mg Oral	Total Recovery of Radioactivity in Feces as Percentage of Total Radioactive Dose of PF-06865571 Administered	30.1 Percentage of Dose	Standard Deviation 2.9
PF-06865571 300 mg Oral & [14C]PF-06865571 100 μg IV	Total Recovery of Radioactivity in Feces as Percentage of Total Radioactive Dose of PF-06865571 Administered	18.8 Percentage of Dose	Standard Deviation 3.3

Primary

Total Recovery of Radioactivity in Total Excreta (Urine + Feces) as Percentage of Total Radioactive Dose of PF-06865571 Administered

The total recovery of radioactivity in the combination of urine and feces was listed and summarized using descriptive statistics. In this outcome measure, the percentages of dose excreted in total excreta (urine + feces) in Period 1 and Period 2 were reported.

Time frame: Period 1: Day -1 to maximum Day 21; Period 2: Day 1 to maximum Day 3

Arm	Measure	Value (MEAN)	Dispersion
[14C]PF-06865571 300 mg Oral	Total Recovery of Radioactivity in Total Excreta (Urine + Feces) as Percentage of Total Radioactive Dose of PF-06865571 Administered	79.0 Percentage of Dose	Standard Deviation 16.7
PF-06865571 300 mg Oral & [14C]PF-06865571 100 μg IV	Total Recovery of Radioactivity in Total Excreta (Urine + Feces) as Percentage of Total Radioactive Dose of PF-06865571 Administered	70.3 Percentage of Dose	Standard Deviation 15.1

Primary

Total Recovery of Radioactivity in Urine as Percentage of Total Radioactive Dose of PF-06865571 Administered

The total recovery of radioactivity in urine was listed and summarized using descriptive statistics. In this outcome measure, the percentages of dose excreted in urine in Period 1 and Period 2 were reported.

Time frame: Period 1: Day -1 to maximum Day 21; Period 2: Day 1 to maximum Day 3

Arm	Measure	Value (MEAN)	Dispersion
[14C]PF-06865571 300 mg Oral	Total Recovery of Radioactivity in Urine as Percentage of Total Radioactive Dose of PF-06865571 Administered	48.9 Percentage of Dose	Standard Deviation 16.3
PF-06865571 300 mg Oral & [14C]PF-06865571 100 μg IV	Total Recovery of Radioactivity in Urine as Percentage of Total Radioactive Dose of PF-06865571 Administered	51.5 Percentage of Dose	Standard Deviation 15.8

Secondary

Absolute Oral Bioavailability (F) of Oral Unlabeled and IV Radiolabeled PF-06865571 for Plasma AUCinf(dn) in Period 2

Absolute Oral Bioavailability (F) provided information on the amount of PF-06865571 reaching the systemic circulation. F was estimated as the ratio of adjusted geometric means of dose-normalized AUCinf for oral unlabeled PF-06865571 and IV labeled 14C PF-06865571 in plasma (from Period 2 only) which was equivalent to the following equation: F = \[PF-06865571\_AUCpo/\[14C\]PF-06865571\_AUCiv\]×\[ \[14C\]PF-06865571\_Doseiv/ PF-06865571\_Dosepo\], where PF-06865571\_AUCpo = AUCinf(dn) of oral unlabeled PF-06865571, \[14C\]PF-06865571\_AUCiv = AUCinf(dn) of intravenous radiolabeled PF-06865571, \[14C\]PF-06865571\_Doseiv = dose of intravenous radiolabeled PF-06865571, PF-06865571\_Dosepo = dose of oral unlabeled PF-06865571.

Time frame: Period 2: -3, 0, 0.08, 0.17, 0.25, 0.5, 0.75, 1, 3, 6, 9, 13, 21, 33 and 45 hours post-dose (Day 1 to Day 3)

Population: Analysis population included all participants treated who had at least one of the PF-06895571 PK parameters of interest and at least one of the 14C parameters of interest.

Arm	Measure	Value (GEOMETRIC_MEAN)
[14C]PF-06865571 300 mg Oral	Absolute Oral Bioavailability (F) of Oral Unlabeled and IV Radiolabeled PF-06865571 for Plasma AUCinf(dn) in Period 2	75.06 Percent

Secondary

Area Under the Plasma Concentration Time Profile From Time Zero Extrapolated to Infinite Time (AUCinf) of Total Radioactivity of [14C]PF-06865571 in Plasma in Period 1

AUCinf = Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0-inf). The determination method of AUCinf was AUClast + (Clast\*/ kel), where Clast\* was the predicted plasma concentration at the last quantifiable time point estimated from the log-linear regression analysis, kel was the terminal phase rate constant.

Time frame: Period 1: 0, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose (Day 1 to Day 6)

Population: Analysis population included all participants treated who had at least one of the 14C parameters of interest.

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
[14C]PF-06865571 300 mg Oral	Area Under the Plasma Concentration Time Profile From Time Zero Extrapolated to Infinite Time (AUCinf) of Total Radioactivity of [14C]PF-06865571 in Plasma in Period 1	20400 ngEq*hr/mL	Geometric Coefficient of Variation 15

Secondary

Area Under the Plasma Concentration-time Profile From Time Zero to Time of The Last Quantifiable Concentration (AUClast) of Total Radioactivity of [14C]PF-06865571 in Plasma in Period 1

AUClast is defined as area under the plasma concentration-time profile from time zero to time of the last quantifiable concentration (Clast). The determination method of AUClast was linear/log trapezoidal rule.

Time frame: Period 1: 0, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose (Day 1 to Day 6)

Population: Analysis population included all participants treated who had at least one of the 14C parameters of interest.

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
[14C]PF-06865571 300 mg Oral	Area Under the Plasma Concentration-time Profile From Time Zero to Time of The Last Quantifiable Concentration (AUClast) of Total Radioactivity of [14C]PF-06865571 in Plasma in Period 1	20080 ngEq*hr/mL (ngEq = nanogram equivalent)	Geometric Coefficient of Variation 15

Secondary

AUCinf(dn) of IV Microtracer of Radiolabeled PF-06865571 in Plasma in Period 2

AUCinf = Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0-inf). It is obtained from AUC (0-t) plus AUC (t-inf). AUCinf(dn) is defined as dose normalized (to 1 mg equivalent) AUCinf, which equals to AUCinf/Dose.

Time frame: Period 2: -3, 0, 0.08, 0.17, 0.25, 0.5, 0.75, 1, 3, 6, 9, 13, 21, 33 and 45 hours post-dose (Day 1 to Day 3)

Population: Analysis population included all participants treated who had at least one of the 14C parameters of interest.

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
[14C]PF-06865571 300 mg Oral	AUCinf(dn) of IV Microtracer of Radiolabeled PF-06865571 in Plasma in Period 2	41.92 ng*hr/mL/mg	Geometric Coefficient of Variation 20

Secondary

AUCinf of IV Radiolabeled PF-06865571 in Plasma in Period 2

Time frame: Period 2: -3, 0, 0.08, 0.17, 0.25, 0.5, 0.75, 1, 3, 6, 9, 13, 21, 33 and 45 hours post-dose (Day 1 to Day 3)

Population: Analysis population included all participants treated who had at least one of the 14C parameters of interest.

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
[14C]PF-06865571 300 mg Oral	AUCinf of IV Radiolabeled PF-06865571 in Plasma in Period 2	4.209 ng*hr/mL	Geometric Coefficient of Variation 19

Secondary

AUCinf of Oral PF-06865571 in Plasma in Period 1

Time frame: Period 1: 0, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose (Day 1 to Day 6)

Population: Analysis population included all participants treated who had at least one of the PF-06895571 PK parameters of interest.

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
[14C]PF-06865571 300 mg Oral	AUCinf of Oral PF-06865571 in Plasma in Period 1	7964 ng*hr/mL	Geometric Coefficient of Variation 19

Secondary

AUClast of Intravenous (IV) Radiolabeled PF-06865571 in Plasma in Period 2

Time frame: Period 2: -3, 0, 0.08, 0.17, 0.25, 0.5, 0.75, 1, 3, 6, 9, 13, 21, 33 and 45 hours post-dose (Day 1 to Day 3)

Population: Analysis population included all participants treated who had at least one of the 14C parameters of interest.

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
[14C]PF-06865571 300 mg Oral	AUClast of Intravenous (IV) Radiolabeled PF-06865571 in Plasma in Period 2	4.145 ng*hr/mL	Geometric Coefficient of Variation 20

Secondary

AUClast of Oral PF-06865571 in Plasma in Period 1

Time frame: Period 1: 0, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose (Day 1 to Day 6)

Population: Analysis population included all participants treated who had at least one of the PF-06895571 PK parameters of interest.

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
[14C]PF-06865571 300 mg Oral	AUClast of Oral PF-06865571 in Plasma in Period 1	7962 nghr/mL (nanogramhour per milliliter)	Geometric Coefficient of Variation 19

Secondary

Cmax of IV Radiolabeled PF-06865571 in Plasma in Period 2

Cmax is defined as maximum plasma concentration. The determination method of Cmax was observing directly from data.

Time frame: Period 2: -3, 0, 0.08, 0.17, 0.25, 0.5, 0.75, 1, 3, 6, 9, 13, 21, 33 and 45 hours post-dose (Day 1 to Day 3)

Population: Analysis population included all participants treated who had at least one of the 14C parameters of interest.

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
[14C]PF-06865571 300 mg Oral	Cmax of IV Radiolabeled PF-06865571 in Plasma in Period 2	2.893 ng/mL	Geometric Coefficient of Variation 13

Secondary

Cmax of Oral PF-06865571 in Plasma in Period 1

Cmax is defined as maximum plasma concentration. The determination method of Cmax was observing directly from data.

Time frame: Period 1: 0, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose (Day 1 to Day 6)

Population: Analysis population included all participants treated who had at least one of the PF-06895571 PK parameters of interest.

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
[14C]PF-06865571 300 mg Oral	Cmax of Oral PF-06865571 in Plasma in Period 1	2096 ng/mL (nanogram per milliliter)	Geometric Coefficient of Variation 15

Secondary

Dose-Normalized AUCinf (AUCinf[dn]) of Oral Unlabeled PF-06865571 in Plasma in Period 2

Time frame: Period 2: -3, 0, 0.08, 0.17, 0.25, 0.5, 0.75, 1, 3, 6, 9, 13, 21, 33 and 45 hours post-dose (Day 1 to Day 3)

Population: Analysis population included all participants treated who had at least one of the PF-06895571 PK parameters of interest.

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
[14C]PF-06865571 300 mg Oral	Dose-Normalized AUCinf (AUCinf[dn]) of Oral Unlabeled PF-06865571 in Plasma in Period 2	31.46 ng*hr/mL/mg	Geometric Coefficient of Variation 21

Secondary

Fraction Absorbed (Fa) for Percentage of Excretion of Total 14C in Urine for Oral and IV Radiolabeled PF-06865571

Determination of the Fraction Absorbed (Fa) (obtained from Periods 1 and 2) provided information on the fraction of the total PF-06865571 dose absorbed, regardless of the fate of that dose after absorption (ie, metabolism, degradation, etc). Fa was estimated as the ratio of the adjusted geometric means of % of administered radioactive dose excreted into the urine following oral and IV administration of \[14C\]PF-06865571 microtracer dose over the same collection time (up to 48 hours post dose) in Periods 1 and 2, respectively: Fa = \[% 14C\_Urine\_PO/% 14C\_Urine\_IV\].

Time frame: Period 1 and Period 2: up to 48 hours post-dose (Day 1 to Day 3)

Population: Analysis population included all participants treated who had at least one of the 14C parameters of interest.

Arm	Measure	Value (GEOMETRIC_MEAN)
[14C]PF-06865571 300 mg Oral	Fraction Absorbed (Fa) for Percentage of Excretion of Total 14C in Urine for Oral and IV Radiolabeled PF-06865571	92.78 Percent

Secondary

Maximum Plasma Concentration (Cmax) of Total Radioactivity of [14C]PF-06865571 in Plasma in Period 1

Cmax is defined as maximum plasma concentration. The determination method of Cmax was observing directly from data.

Time frame: Period 1: 0, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose (Day 1 to Day 6)

Population: Analysis population included all participants treated who had at least one of the 14C parameters of interest.

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
[14C]PF-06865571 300 mg Oral	Maximum Plasma Concentration (Cmax) of Total Radioactivity of [14C]PF-06865571 in Plasma in Period 1	4417 ngEq/mL (nanogram-equivalent/milliliter)	Geometric Coefficient of Variation 10

Secondary

Percentage of Total 14C in Urine Following IV Microtracer Administration (%14C_Urine_IV) of Radiolabeled PF-06865571 in Period 2

%14C\_Urine\_IV is defined as percentage of the radioactive dose administered that is excreted in the urine following IV administration. %14C\_Urine\_IV = Total 14C \_Urine\_IV/14C Doseiv × 100, where IV = intravenous, Total 14C\_Urine\_IV = total radioactivity excreted into the urine following IV administration of \[14C\]PF 06865571, 14C Doseiv = dose of 14C following IV administration of \[14C\]PF 06865571.

Time frame: Period 2: up to 48 hours post-dose (Day 1 to Day 3)

Population: Analysis population included all participants treated who had at least one of the 14C parameters of interest.

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
[14C]PF-06865571 300 mg Oral	Percentage of Total 14C in Urine Following IV Microtracer Administration (%14C_Urine_IV) of Radiolabeled PF-06865571 in Period 2	49.50 Percentage of Total 14C	Geometric Coefficient of Variation 44

Secondary

Percentage of Total 14C in Urine Following Oral Administration (%14C_Urine_PO) of Radiolabeled PF-06865571 in Period 1

%14C\_Urine\_PO is defined as percentage of the radioactive dose administered that is excreted in the urine following oral administration. %14C\_Urine\_PO = Total 14C\_Urine\_PO/14C Dosepo × 100, where PO = orally, Total 14C\_Urine\_PO = total radioactivity excreted into the urine post-dose following oral administration of \[14C\]PF-06865571, 14C Dosepo = dose of 14C following oral administration of \[14C\]PF-06865571.

Time frame: Period 1: up to 48 hours post-dose (Day 1 to Day 3)

Population: Analysis population included all participants treated who had at least one of the 14C parameters of interest.

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
[14C]PF-06865571 300 mg Oral	Percentage of Total 14C in Urine Following Oral Administration (%14C_Urine_PO) of Radiolabeled PF-06865571 in Period 1	45.92 Percentage of Total 14C	Geometric Coefficient of Variation 44

Secondary

Steady State Volume of Distribution (Vss) of IV Radiolabeled PF-06865571 in Plasma in Period 2

Volume of distribution is defined as the theoretical volume in which the total amount of drug would need to be uniformly distributed to produce the desired blood concentration of a drug. Vss is the apparent volume of distribution at steady-state.

Time frame: Period 2: -3, 0, 0.08, 0.17, 0.25, 0.5, 0.75, 1, 3, 6, 9, 13, 21, 33 and 45 hours post-dose (Day 1 to Day 3)

Population: Analysis population included all participants treated who had at least one of the 14C parameters of interest.

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
[14C]PF-06865571 300 mg Oral	Steady State Volume of Distribution (Vss) of IV Radiolabeled PF-06865571 in Plasma in Period 2	38.83 L (Liters)	Geometric Coefficient of Variation 16

Secondary

Systemic Clearance (CL) of IV Radiolabeled PF-06865571 in Plasma in Period 2

CL is a quantitative measure of the rate at which a drug substance is removed from the body. The determination method of CL was dose/AUCinf.

Time frame: Period 2: -3, 0, 0.08, 0.17, 0.25, 0.5, 0.75, 1, 3, 6, 9, 13, 21, 33 and 45 hours post-dose (Day 1 to Day 3)

Population: Analysis population included all participants treated who had at least one of the 14C parameters of interest.

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
[14C]PF-06865571 300 mg Oral	Systemic Clearance (CL) of IV Radiolabeled PF-06865571 in Plasma in Period 2	23.88 L/hr (liter per hour)	Geometric Coefficient of Variation 20

Secondary

t1/2 of IV Radiolabeled PF-06865571 in Plasma in Period 2

Terminal elimination half-life (t1/2) was the time measured for the plasma concentration to decrease by one half. The determination method of t1/2 was loge(2)/kel, where kel was the terminal phase rate constant calculated by a linear regression of the log-linear concentration-time curve.

Time frame: Period 2: -3, 0, 0.08, 0.17, 0.25, 0.5, 0.75, 1, 3, 6, 9, 13, 21, 33 and 45 hours post-dose (Day 1 to Day 3)

Population: Analysis population included all participants treated who had at least one of the 14C parameters of interest.

Arm	Measure	Value (MEAN)	Dispersion
[14C]PF-06865571 300 mg Oral	t1/2 of IV Radiolabeled PF-06865571 in Plasma in Period 2	1.232 hr	Standard Deviation 0.25664

Secondary

t1/2 of Oral PF-06865571 in Plasma in Period 1

Time frame: Period 1: 0, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose (Day 1 to Day 6)

Population: Analysis population included all participants treated who had at least one of the PF-06895571 PK parameters of interest.

Arm	Measure	Value (MEAN)	Dispersion
[14C]PF-06865571 300 mg Oral	t1/2 of Oral PF-06865571 in Plasma in Period 1	6.275 hr	Standard Deviation 2.9246

Secondary

Terminal Elimination Half-life (t1/2) of Total Radioactivity of [14C]PF-06865571 in Plasma in Period 1

Time frame: Period 1: 0, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose (Day 1 to Day 6)

Population: Analysis population included all participants treated who had at least one of the 14C parameters of interest.

Arm	Measure	Value (MEAN)	Dispersion
[14C]PF-06865571 300 mg Oral	Terminal Elimination Half-life (t1/2) of Total Radioactivity of [14C]PF-06865571 in Plasma in Period 1	3.622 hr	Standard Deviation 1.9605

Secondary

Time for Cmax (Tmax) of Total Radioactivity of [14C]PF-06865571 in Plasma in Period 1

Tmax is defined as time to reach maximum observed plasma concentration. The determination method of Tmax was observing directly from data as time of first occurrence.

Time frame: Period 1: 0, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose (Day 1 to Day 6)

Population: Analysis population included all participants treated who had at least one of the 14C parameters of interest.

Arm	Measure	Value (MEDIAN)
[14C]PF-06865571 300 mg Oral	Time for Cmax (Tmax) of Total Radioactivity of [14C]PF-06865571 in Plasma in Period 1	3.00 hr (hours)

Secondary

Tmax of IV Radiolabeled PF-06865571 in Plasma in Period 2

Tmax is defined as time to reach maximum observed plasma concentration. The determination method of Tmax was observing directly from data as time of first occurrence.

Time frame: Period 2: -3, 0, 0.08, 0.17, 0.25, 0.5, 0.75, 1, 3, 6, 9, 13, 21, 33 and 45 hours post-dose (Day 1 to Day 3)

Population: Analysis population included all participants treated who had at least one of the 14C parameters of interest.

Arm	Measure	Value (MEDIAN)
[14C]PF-06865571 300 mg Oral	Tmax of IV Radiolabeled PF-06865571 in Plasma in Period 2	0.250 hr

Secondary

Tmax of Oral PF-06865571 in Plasma in Period 1

Tmax is defined as time to reach maximum observed plasma concentration. The determination method of Tmax was observing directly from data as time of first occurrence.

Time frame: Period 1: 0, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose (Day 1 to Day 6)

Population: Analysis population included all participants treated who had at least one of the PF-06895571 PK parameters of interest.

Arm	Measure	Value (MEDIAN)
[14C]PF-06865571 300 mg Oral	Tmax of Oral PF-06865571 in Plasma in Period 1	3.00 hr

Source: ClinicalTrials.gov · Data processed: Feb 4, 2026

A Study in Healthy Adult Male Participants to Assess Absorption, Distribution, Metabolism and Excretion (ADME) of Radiolabeled PF-06865571.

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Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Feces in Period 1

Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Plasma in Period 1

Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Urine in Period 1

Relative Abundance (Mean Value) of Radiolabeled PF-06865571 in Feces in Period 1

Relative Abundance (Mean Value) of Radiolabeled PF-06865571 in Plasma in Period 1

Relative Abundance (Mean Value) of Radiolabeled PF-06865571 in Urine in Period 1

Total Recovery of Radioactivity in Feces as Percentage of Total Radioactive Dose of PF-06865571 Administered

Total Recovery of Radioactivity in Total Excreta (Urine + Feces) as Percentage of Total Radioactive Dose of PF-06865571 Administered

Total Recovery of Radioactivity in Urine as Percentage of Total Radioactive Dose of PF-06865571 Administered

Absolute Oral Bioavailability (F) of Oral Unlabeled and IV Radiolabeled PF-06865571 for Plasma AUCinf(dn) in Period 2

Area Under the Plasma Concentration Time Profile From Time Zero Extrapolated to Infinite Time (AUCinf) of Total Radioactivity of [14C]PF-06865571 in Plasma in Period 1

Area Under the Plasma Concentration-time Profile From Time Zero to Time of The Last Quantifiable Concentration (AUClast) of Total Radioactivity of [14C]PF-06865571 in Plasma in Period 1

AUCinf(dn) of IV Microtracer of Radiolabeled PF-06865571 in Plasma in Period 2

AUCinf of IV Radiolabeled PF-06865571 in Plasma in Period 2

AUCinf of Oral PF-06865571 in Plasma in Period 1

AUClast of Intravenous (IV) Radiolabeled PF-06865571 in Plasma in Period 2

AUClast of Oral PF-06865571 in Plasma in Period 1

Cmax of IV Radiolabeled PF-06865571 in Plasma in Period 2

Cmax of Oral PF-06865571 in Plasma in Period 1

Dose-Normalized AUCinf (AUCinf[dn]) of Oral Unlabeled PF-06865571 in Plasma in Period 2

Fraction Absorbed (Fa) for Percentage of Excretion of Total 14C in Urine for Oral and IV Radiolabeled PF-06865571

Maximum Plasma Concentration (Cmax) of Total Radioactivity of [14C]PF-06865571 in Plasma in Period 1

Percentage of Total 14C in Urine Following IV Microtracer Administration (%14C_Urine_IV) of Radiolabeled PF-06865571 in Period 2

Percentage of Total 14C in Urine Following Oral Administration (%14C_Urine_PO) of Radiolabeled PF-06865571 in Period 1

Steady State Volume of Distribution (Vss) of IV Radiolabeled PF-06865571 in Plasma in Period 2

Systemic Clearance (CL) of IV Radiolabeled PF-06865571 in Plasma in Period 2

t1/2 of IV Radiolabeled PF-06865571 in Plasma in Period 2

t1/2 of Oral PF-06865571 in Plasma in Period 1

Terminal Elimination Half-life (t1/2) of Total Radioactivity of [14C]PF-06865571 in Plasma in Period 1

Time for Cmax (Tmax) of Total Radioactivity of [14C]PF-06865571 in Plasma in Period 1

Tmax of IV Radiolabeled PF-06865571 in Plasma in Period 2

Tmax of Oral PF-06865571 in Plasma in Period 1