A Study in Healthy Adult Male Participants to Assess Absorption, Distribution, Metabolism and Excretion (ADME) of Radiolabeled PF-06865571.

NCT04866225 | Completed Phase 1 Results FDA Drug

• 1 other identifier: C2541007
• Study Type: interventional
• Target: 6
• Locations: 1 country
• Sites: 1

Brief Summary

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.

Conditions

Healthy Participants

Keywords

ADME

Outcome Measures

Primary Outcomes (9)

• Total Recovery of Radioactivity in Urine as Percentage of Total Radioactive Dose of PF-06865571 Administered

  The total recovery of radioactivity in urine was listed and summarized using descriptive statistics. In this outcome measure, the percentages of dose excreted in urine in Period 1 and Period 2 were reported.

  Period 1: Day -1 to maximum Day 21; Period 2: Day 1 to maximum Day 3

• Total Recovery of Radioactivity in Feces as Percentage of Total Radioactive Dose of PF-06865571 Administered

  The total recovery of radioactivity in feces was listed and summarized using descriptive statistics. In this outcome measure, the percentages of dose excreted in feces in Period 1 and Period 2 were reported.

  Period 1: Day -1 to maximum Day 21; Period 2: Day 1 to maximum Day 3

• Total Recovery of Radioactivity in Total Excreta (Urine + Feces) as Percentage of Total Radioactive Dose of PF-06865571 Administered

  The total recovery of radioactivity in the combination of urine and feces was listed and summarized using descriptive statistics. In this outcome measure, the percentages of dose excreted in total excreta (urine + feces) in Period 1 and Period 2 were reported.

  Period 1: Day -1 to maximum Day 21; Period 2: Day 1 to maximum Day 3

• Relative Abundance (Mean Value) of Radiolabeled PF-06865571 in Plasma in Period 1

  Plasma samples were analyzed for radiolabeled PF-06865571 and its metabolites. \[14C\]PF-06865571 and the major metabolites in plasma, after oral administration of 300 mg \[14C\]PF-06865571 were identified. In this outcome measure, relative abundance of radiolabeled PF-06865571 in plasma based on \[14C\] quantitation was reported. The measure type was the mean value based on pooled sampling, which means blood samples from the 6 participants were pooled together and then analyzed as 1 sample, thus the confidence interval could not be calculated. Therefore, "Number" is selected as the Measure Type.

  Period 1: 0, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose (Day 1 to Day 6)

• Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Plasma in Period 1

  Plasma samples were analyzed for radiolabeled PF-06865571 and its metabolites. \[14C\]PF-06865571 and the major metabolites in plasma, after oral administration of 300 mg \[14C\]PF-06865571 were identified. In this outcome measure, relative abundance of the metabolites of \[14C\]PF-06865571 in plasma based on \[14C\] quantitation was reported. The metabolites included 487, 391, 412, 556, M6 (PF-07822633), M7 (PF-07911964), 584, M1 (PF-06878236), 426, M4 (PF-06887477), 600, M5 (PF-06885984) and M2 (PF-06868609). The measure type was the mean value based on pooled sampling, which means blood samples from the 6 participants were pooled together and then analyzed as 1 sample, thus the confidence interval could not be calculated. Therefore, "Number" is selected as the Measure Type.

  Period 1: 0, 0.5, 3, 6, 12, 24, 36, 48, 72, 96 and 120 hours post-dose (Day 1 to Day 6)

• Relative Abundance (Mean Value) of Radiolabeled PF-06865571 in Urine in Period 1

  Urine samples were analyzed for radiolabeled PF-06865571 and its metabolites. \[14C\]PF-06865571 and the major metabolites in urine, after oral administration of 300 mg \[14C\]PF-06865571 were identified. In this outcome measure, relative abundance of radiolabeled PF-06865571 in urine based on \[14C\] quantitation was reported. The measure type was the mean value based on pooled sampling, which means blood samples from the 6 participants were pooled together and then analyzed as 1 sample, thus the confidence interval could not be calculated. Therefore, "Number" is selected as the Measure Type.

  Period 1: Day -1 to maximum Day 21

• Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Urine in Period 1

  Urine samples were analyzed for radiolabeled PF-06865571 and its metabolites. \[14C\]PF-06865571 and the major metabolites in urine, after oral administration of 300 mg \[14C\]PF-06865571 were identified. In this outcome measure, relative abundance of the metabolites of \[14C\]PF-06865571 in urine based on \[14C\] quantitation was reported. The metabolites included 487, 391, 412, 556, M6 (PF-07822633), M7 (PF-07911964), 584, M1 (PF-06878236), 426, M4 (PF-06887477), 600, M5 (PF-06885984) and M2 (PF-06868609). The measure type was the mean value based on pooled sampling, which means blood samples from the 6 participants were pooled together and then analyzed as 1 sample, thus the confidence interval could not be calculated. Therefore, "Number" is selected as the Measure Type.

  Period 1: Day -1 to maximum Day 21

• Relative Abundance (Mean Value) of Radiolabeled PF-06865571 in Feces in Period 1

  Fecal samples were analyzed for radiolabeled PF-06865571 and its metabolites. \[14C\]PF-06865571 and the major metabolites in feces, after oral administration of 300 mg \[14C\]PF-06865571 were identified. In this outcome measure, relative abundance of radiolabeled PF-06865571 in feces based on \[14C\] quantitation was reported. The measure type was the mean value based on pooled sampling, which means blood samples from the 6 participants were pooled together and then analyzed as 1 sample, thus the confidence interval could not be calculated. Therefore, "Number" is selected as the Measure Type.

  Period 1: Day -1 to maximum Day 21

• Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Feces in Period 1

  Fecal samples were analyzed for radiolabeled PF-06865571 and its metabolites. \[14C\]PF-06865571 and the major metabolites in feces, after oral administration of 300 mg \[14C\]PF-06865571 were identified. In this outcome measure, relative abundance of the metabolites of \[14C\]PF-06865571 in feces based on \[14C\] quantitation was reported. The metabolites included 487, 391, 412, 556, M6 (PF-07822633), M7 (PF-07911964), 584, M1 (PF-06878236), 426, M4 (PF-06887477), 600, M5 (PF-06885984) and M2 (PF-06868609). The measure type was the mean value based on pooled sampling, which means blood samples from the 6 participants were pooled together and then analyzed as 1 sample, thus the confidence interval could not be calculated. Therefore, "Number" is selected as the Measure Type.

  Period 1: Day -1 to maximum Day 21

Secondary Outcomes (23)

• Area Under the Plasma Concentration-time Profile From Time Zero to Time of The Last Quantifiable Concentration (AUClast) of Total Radioactivity of [14C]PF-06865571 in Plasma in Period 1

  Period 1: 0, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose (Day 1 to Day 6)

• Maximum Plasma Concentration (Cmax) of Total Radioactivity of [14C]PF-06865571 in Plasma in Period 1

  Period 1: 0, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose (Day 1 to Day 6)

• Time for Cmax (Tmax) of Total Radioactivity of [14C]PF-06865571 in Plasma in Period 1

  Period 1: 0, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose (Day 1 to Day 6)

• Area Under the Plasma Concentration Time Profile From Time Zero Extrapolated to Infinite Time (AUCinf) of Total Radioactivity of [14C]PF-06865571 in Plasma in Period 1

  Period 1: 0, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose (Day 1 to Day 6)

• Terminal Elimination Half-life (t1/2) of Total Radioactivity of [14C]PF-06865571 in Plasma in Period 1

  Period 1: 0, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose (Day 1 to Day 6)

Study Arms (1)

Study arm

EXPERIMENTAL

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; Drug: Oral PF-06865571; Drug: IV [14C]PF-06865571

Interventions

Oral [14C]PF-06865571 DRUG

Oral radiolabeled PF-06865571

Study arm

Oral PF-06865571 DRUG

Oral PF-06865571

Study arm

IV [14C]PF-06865571 DRUG

IV radiolabeled PF-06865571

Study arm

Eligibility Criteria

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

You may qualify if:

• 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).

You may not qualify if:

• 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.

Sponsors & Collaborators

• Pfizer: lead

Study Sites (1)

Labcorp Clinical Research Unit

Madison, Wisconsin, 53704, United States

Location

Related Links

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

MeSH Terms

Interventions

ervogastat

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: NON RANDOMIZED
• Masking: NONE
• Purpose: BASIC SCIENCE
• Intervention Model: SEQUENTIAL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: April 19, 2021
• First Posted: April 29, 2021
• Study Start: May 11, 2021
• Primary Completion: July 11, 2021
• Study Completion: August 6, 2021
• Last Updated: July 31, 2024
• Results First Posted: July 31, 2024

Record last verified: 2024-02

Data Sharing

• IPD Sharing: Will not share

Locations

US (1)