Study To Characterize Mass Balance, Absolute Bioavailability, Fraction Absorbed And Pharmacokinetics Of 14C PF-06882961

Pfizer6 enrolled

Overview

This study is a Phase 1, open-label, non-randomized, 2-period, fixed sequence study to characterize the metabolic profile and routes of excretion of oral \[14C\]PF-06882961 and to evaluate the absolute oral bioavailability of PF-06882961 and fraction absorbed of \[14C\]PF-06882961 in reference to intravenous \[14C\]PF-06882961 in healthy male participants.

Study Type

INTERVENTIONAL

Allocation

NON_RANDOMIZED

Purpose

BASIC_SCIENCE

Masking

NONE

Enrollment

Conditions

Healthy Volunteer

Interventions

[14C]PF-06882961, 50 mgDRUG

A single oral dose of \[14C\]PF-06882961, will be administered as a liquid formulation.

PF-06882961, 50 mg and [14C]PF-06882961, 100 ugDRUG

A single, oral, unlabeled dose of PF-06882961, 50 mg will be administered as a liquid formulation. Approximately 3 hours after the administration of the unlabeled oral dose, a single dose of \[14C\]PF-06882961 will be administered via intravenous infusion.

Eligibility

Sex: MALEMin age: 18 YearsMax age: 54 YearsHealthy volunteers:

Medical Language ↔ Plain English

Inclusion Criteria: * Male participants between 18 to 54 years of age * Healthy and capable of signing informed consent document * Willing to comply to all scheduled visits, lab tests, lifestyle considerations and study procedures * Body mass index (BMI) of 17.5 to 30 kg/m2; and a total body weight ≥50 kg (110 lb). Exclusion Criteria: * acute or chronic medical or psychiatric condition including recent (within the past year) * Surgical procedures like gastrectomy, cholecystectomy, Irregularity in bowel movements * Use of prescription or non-prescription drugs and dietary and herbal supplements within 14 days prior to the first dose of investigational product. * Previous administration with an investigational drug within 60 days (or as determined by the local requirement) preceding the first dose of investigational product used in this study. * Known prior participation in a trial involving PF-06882961 or known intolerance to a GLP-1R agonist. * A positive urine drug test on screening or Day -1. * Screening supine blood pressure (BP) ≥140 mm Hg (systolic) or ≥90 mm Hg (diastolic), following at least 5 minutes of supine rest. If BP is ≥140 mm Hg (systolic) or ≥90 mm Hg (diastolic), the BP should be repeated 2 more times and the average of the 3 BP values should be used to determine the participant's eligibility. * Participants with abnormalities in clinical laboratory tests including ECGs, vital signs, liver function tests, myocardial infarction * Positive testing for human immunodeficiency virus (HIV), hepatitis B surface antigen (HBsAg), or hepatitis C antibody (HCVAb). Hepatitis B vaccination is allowed. * History of alcohol or tobacco abuse or binge drinking and/or any other illicit drug use or dependence within past 6 months. * Subjects whose occupation requires exposure to radiation or monitoring of radiation exposure. * Blood donation (excluding plasma donations) of approximately 1 pint (500 mL) or more within 60 days prior to dosing. * History of sensitivity to heparin or heparin-induced thrombocytopenia only if heparin is planned to flush intravenous catheters. * Investigator site staff members directly involved in the conduct of the study and their family members, site staff members otherwise supervised by the investigator, or Pfizer employees, including their family members, directly involved in the conduct of the study.

Locations (2)

PRA Health Sciences

Groningen, Netherlands

PRA Health Sciences Utrecht

Utrecht, Netherlands

Outcomes

Primary Outcomes

Total recovery of radioactivity in urine and feces, following oral administration of [14C] PF-06882961 in period 1

Total recovery of radioactivity in urine and feces, and both routes combined, expressed as a percent of total oral radioactive dose administered.

Time frame: Baseline through approximately hour 312 (day 14). Period 1 is 14 days

Secondary Outcomes

Metabolite profiling/identification in plasma, urine, and feces

Metabolic profiling/identification and determination of relative abundance of \[14C\]PF-06882961 and the metabolites of \[14C\]PF-06882961 in plasma, urine, and feces.

Time frame: 0, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96-312 hour (hr)

Plasma Cmax to describe plasma PK of total radioactivity following administration of single, oral dose of [14C] PF-06882961

Maximum Observed Plasma Radioactivity

Time frame: 0, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 hr

Plasma Tmax to describe the PK of total radioactivity following administration of single, oral dose of [14C]PF-06882961

Time to Reach Maximum Observed Plasma Radioactivity

Time frame: 0, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 hr

Plasma AUClast to describe PK of total radioactivity following administration of single, oral dose of [14C] PF-06882961

Area under the plasma radioactivity-time profile from time 0 to time of the last quantifiable concentration (Clast)

Time frame: 0, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 hr

Plasma AUCinf to describe plasma PK of total radioactivity following administration of single, oral dose of [14C] PF-06882961

AUCinf is the area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0-inf).

Data from ClinicalTrials.gov

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