A Study to Understand How the Study Medicine (PF-07081532) is Processed and Eliminated in Healthy Men

NCT05652647 | Completed Phase 1 Results FDA Drug

• 1 other identifier: C3991006
• Study Type: interventional
• Target: 6
• Locations: 1 country
• Sites: 1

Brief Summary

The purpose of this clinical trial is to learn about how much PF-07081532 will be taken up and processed by healthy male participants. The study consists of two parts, called study periods. In Period 1, participants will take one dose of PF-07081532 by mouth. In Period 2, participants will take one dose by mouth and one dose as an injection through a vein at the study clinic. In Period 1, participants will stay at the clinic site for up to 21 days. In Period 2, they will stay at the clinic site for 7 days. During their stays, participants will have their blood, urine, and feces collected by the study doctors several times. We will measure the level of PF-07081532 in participants' blood, urine, and feces samples. This will help us know how much the study medicine is getting taken in by the body. At the end of the study, participants will be contacted by phone to check in. Participants will be involved in this study for about 12 weeks.

Conditions

Healthy Participants

Keywords

Absorption; Distribution; Metabolism; Elimination; Bioavailability; Fraction absorbed; Mass balance; Healthy Males

Outcome Measures

Primary Outcomes (3)

• Total Recovery of Radioactivity in Urine, Feces and Both Routes Combined, as Percentage of Orally Administered Radioactive Dose of [14C]PF-07081532

  Urine and feces samples collected after a single oral dose of \[14C\]PF-07081532 30 mg (\~250 nCi) in Period 1 were analyzed using Accelerator Mass Spectrometry (AMS). "Blank" pre-dose urine samples were collected within the 24 hours prior to dosing, "blank" fecal samples were collected from at least 1 bowel movement within the 48 hours prior to dosing. Following oral dosing, each urine void was collected across intervals of 0-12 hours, 12-24 hours, and each subsequent 24 hour interval up to 360 hours post dose, and all feces excreted were collected across each 24 hour interval up to 360 hours post dose. Recovery of radioactivity in urine, feces, and both routes combined, determined as percentage of the orally administered radioactive dose, are reported.

  360 hours

• Relative Abundance of [14C]PF-07081532 and Its Metabolites in Plasma After A Single Oral Dose of [14]PF-07081532 in Period 1

  Plasma samples collected after a single oral dose of \[14C\]PF-07081532 30 mg (\~250 nCi) were analyzed using Ultra Performance Liquid Chromatography coupled to High Resolution Mass Spectrometry (UPLC-HRMS). Relative abundance = (sum of radioactive content of fractions contributing to a particular peak/total circulating drug-related material \[total \[14C\] radioactivity in plasma\]) x 100%. Metabolites that were detected and identifiable (including coeluting metabolites reported together) are reported in this outcome measure (OM).

  Pre-dose (0 hours [hrs]) and 0.5 hrs, 1 hr, 2 hrs, 4 hrs, 6 hrs, 8 hrs, 10 hrs, 12 hrs, 24 hrs, 36 hrs, 48 hrs, and 72 hrs post Period 1 Day 1 dosing

• Relative Abundance of [14C]PF-07081532 and Its Metabolites in Urine and Feces After A Single Oral Dose of [14]PF-07081532 in Period 1

  Urine and feces samples collected after a single oral dose of \[14C\]PF-07081532 30 mg (\~250 nCi) were analyzed using UPLC-HRMS. "Blank" pre-dose urine samples were collected within the 24 hours prior to dosing, "blank" fecal samples were collected from at least 1 bowel movement within the 48 hours prior to dosing. To obtain samples for evaluation of relative abundance in urine and feces, following oral dosing, each urine void was collected across intervals of 0-12 hours, 12-24 hours, and each subsequent 24 hour interval up to 96 hours post dose, and all feces excreted were collected across each 24 hour interval up to 144 hours post dose. Relative abundance was determined as sum of radioactive content of fractions contributing to a particular peak divided by total radioactive dose excreted in urine/feces respectively. Metabolites that were detected and identifiable (including coeluting metabolites reported together) are reported in this OM.

  96 hours for urine samples and 144 hours for feces samples

Secondary Outcomes (27)

• Area Under the Plasma Concentration-Time Profile From Time Zero to the Time of the Last Quantifiable Concentration (AUClast) of Total [14C] After A Single Oral Dose of [14C]PF-07081532 in Period 1

  Pre-dose (0 hrs) and 0.5 hrs, 1 hr, 2 hrs, 4 hrs, 6 hrs, 8 hrs, 10 hrs, 12 hrs, 15 hrs, 24 hrs, 36 hrs, 48 hrs, 72 hrs, 96 hrs, 120 hrs and 144 hrs post Period 1 Day 1 dosing

• AUClast of PF-07081532 After A Single Oral Dose of [14]PF-07081532 in Period 1

  Pre-dose (0 hrs) and 0.5 hrs, 1 hr, 2 hrs, 4 hrs, 6 hrs, 8 hrs, 10 hrs, 12 hrs, 15 hrs, 24 hrs, 36 hrs, 48 hrs, 72 hrs, 96 hrs, 120 hrs and 144 hrs post Period 1 Day 1 dosing

• Plasma Maximum Observed Concentration (Cmax) of Total [14C] After A Single Oral Dose of [14C]PF-07081532 in Period 1

  Pre-dose (0 hrs) and 0.5 hrs, 1 hr, 2 hrs, 4 hrs, 6 hrs, 8 hrs, 10 hrs, 12 hrs, 15 hrs, 24 hrs, 36 hrs, 48 hrs, 72 hrs, 96 hrs, 120 hrs and 144 hrs post Period 1 Day 1 dosing

• Plasma Cmax of PF-07081532 After A Single Oral Dose of [14C]PF-07081532 in Period 1

  Pre-dose (0 hrs) and 0.5 hrs, 1 hr, 2 hrs, 4 hrs, 6 hrs, 8 hrs, 10 hrs, 12 hrs, 15 hrs, 24 hrs, 36 hrs, 48 hrs, 72 hrs, 96 hrs, 120 hrs and 144 hrs post Period 1 Day 1 dosing

• Plasma Time to Reach Cmax (Tmax) of Total [14C] and PF-07081532 After A Single Oral Dose of [14C]PF-07081532 in Period 1

  Pre-dose (0 hrs) and 0.5 hrs, 1 hr, 2 hrs, 4 hrs, 6 hrs, 8 hrs, 10 hrs, 12 hrs, 15 hrs, 24 hrs, 36 hrs, 48 hrs, 72 hrs, 96 hrs, 120 hrs and 144 hrs post Period 1 Day 1 dosing

Study Arms (1)

One group of healthy adult male participants

EXPERIMENTAL

Drug: Oral [14C]PF-07081532; Drug: Oral PF-07081532 and IV [14C]PF-07081532

Interventions

Oral [14C]PF-07081532 DRUG

A single oral dose of \[14C\]PF-07081532, will be administered as a liquid formulation in study period 1.

One group of healthy adult male participants

Oral PF-07081532 and IV [14C]PF-07081532 DRUG

In study period 2: a single, oral, unlabeled dose of PF-07081532 will be administered as a liquid formulation. Approximately 1 hours after the administration of the unlabeled oral dose, a single dose of \[14C\]PF-07081532 will be administered via intravenous infusion.

One group of healthy adult male participants

Eligibility Criteria

• Age: 18 Years - 60 Years
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Healthy Male participants must be 18 to 60 years of age, inclusive.
• Overtly healthy as determined by medical evaluation including medical history, physical examination, blood pressure and pulse rate measurement, standard 12-lead ECG, and laboratory tests.
• BMI of 17.5 to 30.5 kg/m2; and a total body weight \>50 kg (110 lb).
• Participants who are willing and able to comply with all scheduled visits, treatment plan, laboratory tests, lifestyle considerations, and other study procedures

You may not qualify if:

• History of irregular bowel movements (eg, irritable bowel syndrome, frequent episodes of diarrhea, or constipation defined by less than 1 bowel movement on average per 2 days) or lactose intolerance
• Any condition possibly affecting drug absorption (eg, gastrectomy, cholecystectomy).
• Previous administration with an investigational product (drug or vaccine) within 90 days (or as determined by the local requirement) preceding the first dose of study intervention used in this study.
• Total 14C radioactivity measured in plasma 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.

Results Point of Contact

• Title: Pfizer ClinicalTrials.gov Call Center
• Organization: Pfizer Inc.

ClinicalTrials.gov_Inquiries@pfizer.com

1-800-718-1021

Study Officials

• Pfizer CT.gov Call Center

  Pfizer

  STUDY DIRECTOR

Publication Agreements

• PI is Sponsor Employee: No
• Restriction Type: OTHER
• Restrictive Agreement: Yes

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: December 7, 2022
• First Posted: December 15, 2022
• Study Start: December 21, 2022
• Primary Completion: March 15, 2023
• Study Completion: March 15, 2023
• Last Updated: September 24, 2024
• Results First Posted: September 24, 2024

Record last verified: 2024-09

Data Sharing

• IPD Sharing: Will not share

Locations

NL (1)