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

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.

Study Overview

• Status: Completed
• Conditions: Healthy Participants
• Intervention / Treatment: Drug: Oral [14C]PF-06865571; Drug: Oral PF-06865571; Drug: IV [14C]PF-06865571

• Study Type: Interventional
• Enrollment (Actual): 6
• Phase: Phase 1

Contacts and Locations

Study Locations

• United States
  • Wisconsin
    • Madison, Wisconsin, United States, 53704
      • Covance Clinical Research Unit

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 60 years (Adult)
• Accepts Healthy Volunteers: No
• Genders Eligible for Study: Male

Description

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.

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Basic Science
• Allocation: Non-Randomized
• Interventional Model: Sequential Assignment
• Masking: None (Open Label)

Number of Arms

1

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Study arm; One arm of healthy male participants administered a single oral dose of [14C]PF-06865571; followed by a single dose of unlabeled PF-06865571, and IV administration of [14C]PF-06865571 three hours later.	Drug: Oral [14C]PF-06865571; Oral radiolabeled PF-06865571; Drug: Oral PF-06865571; Oral PF-06865571; Drug: IV [14C]PF-06865571; IV radiolabeled PF-06865571

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Total recovery of radioactivity in urine, feces and total excreta (urine + feces) as percentage of total radioactive dose administered.	To characterize the extent of excretion of total radioactivity in urine and feces following administration of a single oral dose of radiolabeled PF-06865571.	Period 1, Pre-dose to maximum Day 21.
Amount (% of administered dose) of radiolabeled PF-06865571 in plasma.	To determine the amount of radiolabeled PF-06865571 in plasma as the % of the administered dose.	Period 1, Pre-dose to Day 6.
Amount of metabolites of radiolabeled PF-06865571 (% of administered dose) in plasma.	To determine the amount of metabolites of radiolabeled PF-06865571 in plasma as the % of the administered dose.	Period 1, Pre-dose to Day 6.
Amount (% of administered dose) of radiolabeled PF-06865571 in urine.	To determine the amount of radiolabeled PF-06865571 in urine as a % of administered dose.	Period 1, Pre-dose to maximum Day 21.
Amount of metabolites of radiolabeled PF-06865571 (% of administered dose) in urine.	To determine the amount of metabolites of radiolabeled PF-06865571 in urine as a % of administered dose.	Period 1, Pre-dose to maximum Day 21.
Amount (% of administered dose) of radiolabeled PF-06865571 in feces.	To determine the amount of radiolabeled PF-06865571 in feces as a % of administered dose.	Period 1, Pre-dose to maximum Day 21.
Amount of metabolites of radiolabeled PF-06865571 (% of administered dose) in feces.	To determine the amount of metabolites of radiolabeled PF-06865571 in feces as a % of administered dose.	Period 1, Pre-dose to maximum Day 21.

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
AUClast of oral radiolabeled PF-06865571 in plasma	Area under the plasma concentration-time profile from time zero to time of the last quantifiable concentration (Clast) of radiolabeled PF-06865571 following administration of a single oral dose of radiolabeled PF-06865571.	Period 1: Pre-dose, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose
Cmax of oral radiolabeled PF-06865571 in plasma	Maximum plasma concentration of radiolabeled PF-06865571 following administration of a single oral dose of radiolabeled PF-06865571.	Period 1: Pre-dose, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose
Tmax of oral radiolabeled PF-06865571 in plasma	Time to Cmax following administration of a single oral dose of radiolabeled PF-06865571.	Period 1: Pre-dose, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose
AUCinf of oral radiolabeled PF-06865571 in plasma (if data permit)	Area under the plasma concentration-time profile from time zero extrapolated to infinite time following administration of a single oral dose of radiolabeled PF-06865571.	Period 1: Pre-dose, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose
t1/2 of oral radiolabeled PF-06865571 in plasma (if data permit)	Terminal elimination half-life following administration of a single oral dose of radiolabeled PF-06865571.	Period 1: Pre-dose, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose
AUClast of radioactivity in plasma	Area under the plasma concentration-time profile from time zero to time of the last quantifiable concentration (Clast) of radioactivity following administration of a single oral dose of radiolabeled PF-06865571.	Period 1: Pre-dose, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose
Cmax of radioactivity in plasma	Maximum plasma concentration of radioactivity following administration of a single oral dose of radiolabeled PF-06865571.	Period 1: Pre-dose, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose
Tmax of radioactivity PF-06865571 in plasma	Time to Cmax following administration of a single oral dose of radiolabeled PF-06865571.	Period 1: Pre-dose, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose
AUCinf of radioactivity in plasma (if data permit)	Area under the plasma radioactivity concentration-time profile from time zero extrapolated to infinite time following administration of a single oral dose of radiolabeled PF-06865571.	Period 1: Pre-dose, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose
t1/2 of radioactivity in plasma (if data permit)	Terminal elimination half-life following administration of a single oral dose of radiolabeled PF-06865571.	Period 1: Pre-dose, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose
AUClast of intravenous radiolabeled PF-06865571 in plasma	Area under the plasma concentration-time profile from time zero to time of the last quantifiable concentration (Clast) of radiolabeled PF-06865571 following administration of a single intravenous dose of radiolabeled PF-06865571.	Period 2: Pre-dose, 0.08, 0.17, 0.25, 0.5, 0.75, 1, 3, 6, 9, 13, 21, 33 and 45 hours post-dose
Cmax of intravenous radiolabeled PF-06865571 in plasma	Maximum plasma concentration of radiolabeled PF-06865571 following administration of a single intravenous dose of radiolabeled PF-06865571.	Period 2: Pre-dose, 0.08, 0.17, 0.25, 0.5, 0.75, 1, 3, 6, 9, 13, 21, 33 and 45 hours post-dose
Tmax of intravenous radiolabeled PF-06865571 in plasma	Time to Cmax following administration of a single intravenous dose of radiolabeled PF-06865571.	Period 2: Pre-dose, 0.08, 0.17, 0.25, 0.5, 0.75, 1, 3, 6, 9, 13, 21, 33 and 45 hours post-dose
AUCinf of intravenous radiolabeled PF-06865571 in plasma (if data permit)	Area under the plasma concentration-time profile from time zero extrapolated to infinite time following administration of a single intravenous dose of radiolabeled PF-06865571.	Period 2: Pre-dose, 0.08, 0.17, 0.25, 0.5, 0.75, 1, 3, 6, 9, 13, 21, 33 and 45 hours post-dose
t1/2 of intravenous radiolabeled PF-06865571 in plasma (if data permit)	Terminal elimination half-life following administration of a single intravenous dose of radiolabeled PF-06865571.	Period 2: Pre-dose, 0.08, 0.17, 0.25, 0.5, 0.75, 1, 3, 6, 9, 13, 21, 33 and 45 hours post-dose
CL of intravenous radiolabeled PF-06865571 in plasma (if data permit)	Systemic clearance following administration of a single intravenous dose of radiolabeled PF-06865571.	Period 2: Pre-dose, 0.08, 0.17, 0.25, 0.5, 0.75, 1, 3, 6, 9, 13, 21, 33 and 45 hours post-dose
Vss of intravenous radiolabeled PF-06865571 in plasma (if data permit)	Steady-state volume of distribution following administration of a single intravenous dose of radiolabeled PF-06865571.	Period 2: Pre-dose, 0.08, 0.17, 0.25, 0.5, 0.75, 1, 3, 6, 9, 13, 21, 33 and 45 hours post-dose
Absolute oral bioavailability of PF-06865571	Dose-normalized plasma AUCinf (if data permit, otherwise AUClast) following oral unlabeled PF-06865571 compared to IV microtracer PF-06865571 in Period 2.	Period 2: Pre-dose up to 48 hours post-dose
Fraction of the dose absorbed (Fa) for oral PF-06865571	Total urinary radioactivity following oral administration of radiolabeled PF-06865571 in Period 1 and IV microtracer administration of PF-06865571 in Period 2.	Pre-dose up to 48 hours post-dose

Collaborators and Investigators

• Sponsor: Pfizer

Publications and helpful links

Helpful Links

• To obtain contact information for a study center near you, click here.

Study record dates

Study Major Dates

• Study Start (Actual): May 11, 2021
• Primary Completion (Actual): July 11, 2021
• Study Completion (Actual): August 6, 2021

Study Registration Dates

• First Submitted: April 19, 2021
• First Submitted That Met QC Criteria: April 28, 2021
• First Posted (Actual): April 29, 2021

Study Record Updates

• Last Update Posted (Actual): October 8, 2021
• Last Update Submitted That Met QC Criteria: October 7, 2021
• Last Verified: October 1, 2021

More Information

Terms related to this study

• Keywords: ADME
• Other Study ID Numbers: C2541007

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: No
• IPD Plan Description: Pfizer will provide access to individual de-identified participant data and related study documents (e.g. protocol, Statistical Analysis Plan (SAP), Clinical Study Report (CSR)) upon request from qualified researchers, and subject to certain criteria, conditions, and exceptions. Further details on Pfizer's data sharing criteria and process for requesting access can be found at: https://www.pfizer.com/science/clinical_trials/trial_data_and_results/data_requests.

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: Yes
• Studies a U.S. FDA-regulated device product: No