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

Healthy Participants Clinical Trial

Official title:

A PHASE 1, OPEN-LABEL, FIXED-SEQUENCE, 2-PERIOD STUDY IN HEALTHY ADULT MALE PARTICIPANTS TO ASSESS THE EXTENT OF EXCRETION, ABSOLUTE BIOAVAILABILITY, FRACTION ABSORBED, AND PHARMACOKINETICS OF [14C]PF-06865571 USING A 14C-MICROTRACER APPROACH

Clinical Trial Details — Status: Completed

Administrative data

• NCT number: NCT04866225
• Other study ID #: C2541007
• Status: Completed
• Phase: Phase 1
• Start date: May 11, 2021
• Est. completion date: August 6, 2021

Study information

• Verified date: October 2021
• Source: Pfizer
• Contact: n/a
• Is FDA regulated: No
• Study type: Interventional

Clinical Trial 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.

Recruitment information / eligibility

• Status: Completed
• Enrollment: 6
• Est. completion date: August 6, 2021
• Est. primary completion date: July 11, 2021
• Accepts healthy volunteers: Accepts Healthy Volunteers
• Gender: Male
• Age group: 18 Years to 60 Years

Eligibility

Inclusion Criteria:

• 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).

Exclusion Criteria:

• 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.

Related Conditions & MeSH terms

• Healthy Participants

Intervention

Drug:
• Oral [14C]PF-06865571
Oral radiolabeled PF-06865571
• Oral PF-06865571
Oral PF-06865571
• IV [14C]PF-06865571
IV radiolabeled PF-06865571

Locations

Country	Name	City	State
United States	Covance Clinical Research Unit	Madison	Wisconsin

Sponsors (1)

Lead Sponsor	Collaborator
Pfizer

Country where clinical trial is conducted

United States, 

Outcome

Type	Measure	Description	Time frame	Safety issue
Primary	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 radiolabeled PF-06865571.	Period 1, Pre-dose to maximum Day 21.
Primary	Amount (% of administered dose) of radiolabeled PF-06865571 in plasma.	To determine the amount of radiolabeled PF-06865571 in plasma as the % of the administered dose.	Period 1, Pre-dose to Day 6.
Primary	Amount of metabolites of radiolabeled PF-06865571 (% of administered dose) in plasma.	To determine the amount of metabolites of radiolabeled PF-06865571 in plasma as the % of the administered dose.	Period 1, Pre-dose to Day 6.
Primary	Amount (% of administered dose) of radiolabeled PF-06865571 in urine.	To determine the amount of radiolabeled PF-06865571 in urine as a % of administered dose.	Period 1, Pre-dose to maximum Day 21.
Primary	Amount of metabolites of radiolabeled PF-06865571 (% of administered dose) in urine.	To determine the amount of metabolites of radiolabeled PF-06865571 in urine as a % of administered dose.	Period 1, Pre-dose to maximum Day 21.
Primary	Amount (% of administered dose) of radiolabeled PF-06865571 in feces.	To determine the amount of radiolabeled PF-06865571 in feces as a % of administered dose.	Period 1, Pre-dose to maximum Day 21.
Primary	Amount of metabolites of radiolabeled PF-06865571 (% of administered dose) in feces.	To determine the amount of metabolites of radiolabeled PF-06865571 in feces as a % of administered dose.	Period 1, Pre-dose to maximum Day 21.
Secondary	AUClast of oral radiolabeled PF-06865571 in plasma	Area under the plasma concentration-time profile from time zero to time of the last quantifiable concentration (Clast) of radiolabeled PF-06865571 following administration of a single oral dose of radiolabeled PF-06865571.	Period 1: Pre-dose, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose
Secondary	Cmax of oral radiolabeled PF-06865571 in plasma	Maximum plasma concentration of radiolabeled PF-06865571 following administration of a single oral dose of radiolabeled PF-06865571.	Period 1: Pre-dose, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose
Secondary	Tmax of oral radiolabeled PF-06865571 in plasma	Time to Cmax following administration of a single oral dose of radiolabeled PF-06865571.	Period 1: Pre-dose, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose
Secondary	AUCinf of oral radiolabeled PF-06865571 in plasma (if data permit)	Area under the plasma concentration-time profile from time zero extrapolated to infinite time following administration of a single oral dose of radiolabeled PF-06865571.	Period 1: Pre-dose, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose
Secondary	t1/2 of oral radiolabeled PF-06865571 in plasma (if data permit)	Terminal elimination half-life following administration of a single oral dose of radiolabeled PF-06865571.	Period 1: Pre-dose, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose
Secondary	AUClast of radioactivity in plasma	Area under the plasma concentration-time profile from time zero to time of the last quantifiable concentration (Clast) of radioactivity following administration of a single oral dose of radiolabeled PF-06865571.	Period 1: Pre-dose, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose
Secondary	Cmax of radioactivity in plasma	Maximum plasma concentration of radioactivity following administration of a single oral dose of radiolabeled PF-06865571.	Period 1: Pre-dose, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose
Secondary	Tmax of radioactivity PF-06865571 in plasma	Time to Cmax following administration of a single oral dose of radiolabeled PF-06865571.	Period 1: Pre-dose, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose
Secondary	AUCinf of radioactivity in plasma (if data permit)	Area under the plasma radioactivity concentration-time profile from time zero extrapolated to infinite time following administration of a single oral dose of radiolabeled PF-06865571.	Period 1: Pre-dose, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose
Secondary	t1/2 of radioactivity in plasma (if data permit)	Terminal elimination half-life following administration of a single oral dose of radiolabeled PF-06865571.	Period 1: Pre-dose, 0.5, 1, 2, 3, 4, 6, 9, 12, 16, 24, 36, 48, 72, 96 and 120 hours post-dose
Secondary	AUClast of intravenous radiolabeled PF-06865571 in plasma	Area under the plasma concentration-time profile from time zero to time of the last quantifiable concentration (Clast) of radiolabeled PF-06865571 following administration of a single intravenous dose of radiolabeled PF-06865571.	Period 2: Pre-dose, 0.08, 0.17, 0.25, 0.5, 0.75, 1, 3, 6, 9, 13, 21, 33 and 45 hours post-dose
Secondary	Cmax of intravenous radiolabeled PF-06865571 in plasma	Maximum plasma concentration of radiolabeled PF-06865571 following administration of a single intravenous dose of radiolabeled PF-06865571.	Period 2: Pre-dose, 0.08, 0.17, 0.25, 0.5, 0.75, 1, 3, 6, 9, 13, 21, 33 and 45 hours post-dose
Secondary	Tmax of intravenous radiolabeled PF-06865571 in plasma	Time to Cmax following administration of a single intravenous dose of radiolabeled PF-06865571.	Period 2: Pre-dose, 0.08, 0.17, 0.25, 0.5, 0.75, 1, 3, 6, 9, 13, 21, 33 and 45 hours post-dose
Secondary	AUCinf of intravenous radiolabeled PF-06865571 in plasma (if data permit)	Area under the plasma concentration-time profile from time zero extrapolated to infinite time following administration of a single intravenous dose of radiolabeled PF-06865571.	Period 2: Pre-dose, 0.08, 0.17, 0.25, 0.5, 0.75, 1, 3, 6, 9, 13, 21, 33 and 45 hours post-dose
Secondary	t1/2 of intravenous radiolabeled PF-06865571 in plasma (if data permit)	Terminal elimination half-life following administration of a single intravenous dose of radiolabeled PF-06865571.	Period 2: Pre-dose, 0.08, 0.17, 0.25, 0.5, 0.75, 1, 3, 6, 9, 13, 21, 33 and 45 hours post-dose
Secondary	CL of intravenous radiolabeled PF-06865571 in plasma (if data permit)	Systemic clearance following administration of a single intravenous dose of radiolabeled PF-06865571.	Period 2: Pre-dose, 0.08, 0.17, 0.25, 0.5, 0.75, 1, 3, 6, 9, 13, 21, 33 and 45 hours post-dose
Secondary	Vss of intravenous radiolabeled PF-06865571 in plasma (if data permit)	Steady-state volume of distribution following administration of a single intravenous dose of radiolabeled PF-06865571.	Period 2: Pre-dose, 0.08, 0.17, 0.25, 0.5, 0.75, 1, 3, 6, 9, 13, 21, 33 and 45 hours post-dose
Secondary	Absolute oral bioavailability of PF-06865571	Dose-normalized plasma AUCinf (if data permit, otherwise AUClast) following oral unlabeled PF-06865571 compared to IV microtracer PF-06865571 in Period 2.	Period 2: Pre-dose up to 48 hours post-dose
Secondary	Fraction of the dose absorbed (Fa) for oral PF-06865571	Total urinary radioactivity following oral administration of radiolabeled PF-06865571 in Period 1 and IV microtracer administration of PF-06865571 in Period 2.	Pre-dose up to 48 hours post-dose

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