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

NCT04495140 | Completed Phase 1 FDA Drug

• 2 other identifiers: C34210092019-002584-10
• Study Type: interventional
• Target: 6
• Locations: 1 country
• Sites: 2

Brief Summary

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.

Conditions

Healthy Volunteer

Keywords

bioavailability; excretion; metabolism; absorption

Outcome Measures

Primary Outcomes (1)

• 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.

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

Secondary Outcomes (20)

• Metabolite profiling/identification in plasma, urine, and feces

  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

  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

  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

  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

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

Study Arms (2)

Oral [14C]PF-06882961, 50 mg

EXPERIMENTAL

In this arm, a single oral dose of \[14C\]PF-06882961, 50 mg will be administered as a liquid formulation.

Drug: [14C]PF-06882961, 50 mg

Oral PF-06882961 50 mg and intravenous [14C]PF-06882961 100 ug

EXPERIMENTAL

In this arm, single oral dose of unlabeled 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, 100 ug, will be administered via intravenous infusion.

Drug: PF-06882961, 50 mg and [14C]PF-06882961, 100 ug

Interventions

[14C]PF-06882961, 50 mg DRUG

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

Oral [14C]PF-06882961, 50 mg

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

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.

Oral PF-06882961 50 mg and intravenous [14C]PF-06882961 100 ug

Eligibility Criteria

• Age: 18 Years - 54 Years
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• 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).

You may not qualify if:

• 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.

Sponsors & Collaborators

• Pfizer: lead

Study Sites (2)

PRA Health Sciences

Groningen, 9728 NZ, Netherlands

Location

PRA Health Sciences Utrecht

Utrecht, 3584 BL, Netherlands

Location

Related Links

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

MeSH Terms

Interventions

danuglipron

Study Officials

• Pfizer CT.gov Call Center

  Pfizer

  STUDY DIRECTOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NON RANDOMIZED
• Masking: NONE
• Purpose: BASIC SCIENCE
• Intervention Model: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: July 16, 2020
• First Posted: July 31, 2020
• Study Start: July 22, 2020
• Primary Completion: October 15, 2020
• Study Completion: October 15, 2020
• Last Updated: November 25, 2020

Record last verified: 2020-11

Data Sharing

• IPD Sharing: Will not share

Locations

NL (2)