A Study to Learn How the Medicine Called [14C] PF-06821497 is Taken up Into and Removed From the Body.

NCT06392230 | Completed Phase 1

• 2 other identifiers: C23210072023-508371-36-00
• Study Type: interventional
• Target: 6
• Locations: 1 country
• Sites: 1

Brief Summary

The purpose of this study is to learn how a certain amount of \[14C\] PF-06821497 is taken up into the bloodstream and removed from the body. The study is seeking participants who are:

• Males aged 18 years or older.
• Are confirmed to be healthy after performing some medical and physical tests.
• Weigh more than 50 kilograms and have a body mass index of 16 to 32 kg per meter squared. The study consists of two parts. In part one, all participants will receive one full dose of \[14C\]PF-06821497 by mouth. Part two will begin at least 14 days after the dose in part one. In part two participants will receive one full dose of PF-06821497 by mouth and one small dose of \[14C\]PF-06821497 by intravenous (IV) infusion. IV infusion will be directly injected into the veins. To understand how the medicine is processed in the body, samples of blood, urine, and feces will be collected after each dose is given. This will help understand:
• How much PF-06821497 is taken up into the bloodstream when taken by mouth compared to the dose given by IV
• How the body removes it from the bloodstream. Participants will take part in the study for about 11 weeks, including the initial evaluation and follow-up periods.

Conditions

Healthy Participants

Keywords

Absorption; Distribution; Metabolism; Elimination; ADME (Absorption, Distribution, Metabolism, and Excretion); Pharmacokinetics; Bioavailability; Fraction absorbed; Mass balance; Healthy Males; Enhancer of zeste homolog 2 (EZH2) inhibitor

Outcome Measures

Primary Outcomes (2)

• 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 \[14C\]PF-06821497

  Period 1 pre-dose to maximum Day 14

• Metabolic profiling/identification and determination of relative abundance of [14C]PF-06821497 and the metabolites of [14C]PF-06821497 in plasma, urine, and feces

  Amount of metabolites of \[14C\]PF-06821497 in plasma, urine, and feces

  Period 1 pre-dose to maximum Day 14

Secondary Outcomes (19)

• Absolute oral bioavailability (F) of [14C]PF-06821497

  Period 2 pre-dose to maximum Day 5

• Fraction of [14C]PF 06821497 dose absorbed (Fa)

  Period 1 pre-dose to maximum Day 14; Period 2 pre-IV dose to maximum Day 5

• AUClast of total radioactivity and PF-06821497 in plasma

  Period 1 pre-dose to maximum Day 14

• Cmax of total radioactivity and PF-06821497 in plasma

  Period 1 pre-dose to maximum Day 14

• Tmax of total radioactivity and PF-06821497 in plasma

  Period 1 pre-dose to maximum Day 14

Study Arms (1)

Cohort 1

EXPERIMENTAL

Participants will receive one dose of \[14C\] PF-06821497 by mouth in Period 1. After a washout, participants will receive one dose of PF-06821497 by mouth and one intravenous (IV) infusion of \[14C\] PF-06821497 in Period 2

Drug: Oral [14C] PF-06821497; Drug: Oral PF-06821497; Drug: IV [14C] PF-06821497

Interventions

Oral [14C] PF-06821497 DRUG

A single oral dose of \[14C\] PF-06821497 will be administered as an extemporaneous suspension in Period 1

Cohort 1

Oral PF-06821497 DRUG

A single oral dose of PF-06821497 will be administered as an extemporaneous oral suspension in Period 2

Cohort 1

IV [14C] PF-06821497 DRUG

A single IV infusion of \[14C\] PF-06821497 will be administered at the Tmax after administration of the unlabeled oral dose of PF-06821497 in Period 2

Cohort 1

Eligibility Criteria

• Age: 18 Years+
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• Male participants aged 18 years at screening who are overtly healthy as determined by medical evaluation including medical history, physical examination, laboratory tests, and cardiac monitoring.
• Body mass index (BMI) of 16-32 kg/m2; and a total body weight of \>50kg (110lb)
• Participants who are willing to comply with all scheduled visits, treatment plan, laboratory tests, lifestyle considerations, and other study procedures

You may not qualify if:

• Any condition possibly affecting drug absorption (eg, gastrectomy, cholecystectomy, prior bariatric surgery, ileal resection, inflammatory gastrointestinal disease, chronic diarrhea, known diverticular disease).
• Chronic liver diseases including alcoholic liver disease, viral hepatitis, primary biliary cirrhosis, primary sclerosing cholangitis, autoimmune hepatitis, Wilson's disease, hemochromatosis, alpha-1 antitrypsin deficiency, human immunodeficiency virus, or other chronic liver disease.
• Previous administration with an investigational product (drug or vaccine) within 30 days (or as determined by the local requirement) or 5 half lives preceding the first dose of study intervention used in this study (whichever is longer). Participation in studies of other investigational products (drug or vaccine) at any time during their participation in this study.
• Total \[14C\] radioactivity measured in plasma at screening exceeding 11 mBq/mL

Sponsors & Collaborators

• Pfizer: lead

Study Sites (1)

PRA Health Sciences

Groningen, 9728 NZ, Netherlands

Location

Related Links

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

MeSH Terms

Interventions

PF06821497

Study Officials

• Pfizer CT.gov Call Center

  Pfizer

  STUDY DIRECTOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NA
• Masking: NONE
• Purpose: BASIC SCIENCE
• Intervention Model: SINGLE GROUP
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: April 12, 2024
• First Posted: April 30, 2024
• Study Start: August 30, 2024
• Primary Completion: November 11, 2024
• Study Completion: November 11, 2024
• Last Updated: January 23, 2025

Record last verified: 2025-01

Data Sharing

• IPD Sharing: Will not share

Locations

NL (1)