A Study To Asses Mass Balance And Absolute Bioavailability Of 14C PF-06826647 In Healthy Male Participants

A PHASE 1, OPEN LABEL, 2-PERIOD, FIXED SEQUENCE, STUDY TO ASSESS THE MASS BALANCE, ABSOLUTE BIOAVAILABILITY OF 14C PF 06826647 IN HEALTHY MALE PARTICIPANTS

The purpose of the study is to determine the metabolism and excretion following a single oral administration of 14C-PF-06826647-LR (14C labelled PF-06826647 with lower radioactivity per mass unit) in fed conditions. This information will enable assessment of clearance mechanisms of PF-06826647 as well as identify metabolites. In addition, this study will determine absolute bioavailability of PF-06826647 and understand intravenous (IV) pharmacokinetic (PK).

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Drug: 14C-PF-06826647-LR 600 mg PO; Drug: PF-06826647 600 mg PO; Drug: 14C-PF-06826647 100 ug IV

• Study Type: Interventional
• Enrollment (Actual): 6
• Phase: Phase 1

Contacts and Locations

Study Locations

• Netherlands
  • Groningen, Netherlands, 9728 NZ
    • PRA Health Sciences
  • Utrecht, Netherlands, 3584 BL
    • PRA Health Sciences Utrecht

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 55 years (Adult)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: Male

Description

Inclusion Criteria:

• Healthy Male participants must be 18 to 55 years of age, inclusive.
• Male participants who are overtly healthy as determined by medical evaluation including medical history, physical examination, including BP and pulse rate measurement, laboratory tests, and 12 lead ECG.
• Participants who are willing and able to comply with all scheduled visits, treatment plan, laboratory tests, lifestyle considerations, and other study procedures.
• BMI of 17.5 to 30 kg/m2; and a total body weight >50 kg (110 lb).

Exclusion Criteria:

• Evidence or history of clinically significant hematological, renal, endocrine, pulmonary, gastrointestinal, cardiovascular, hepatic, psychiatric, neurological, or allergic disease (including drug allergies, but excluding untreated, asymptomatic, seasonal allergies at the time of dosing).
• 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.
• Participants who currently use or have formerly used (within 6 months of dosing) tobacco or nicotine containing products.
• Total 14C radioactivity measured in plasma exceeding 11 mBq/mL.

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Other
• Allocation: N/A
• Interventional Model: Single Group Assignment
• Masking: None (Open Label)

Number of Arms

1

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: PF-06826647 600 mg PO>PF-06826647 600 mg PO+100 ug IV; PF-06826647 600 mg single dose in Period 1 followed by PF-06826647 600 mg PO and IV infusion of 100 ug of PF-06826647 in Period 2.	Drug: 14C-PF-06826647-LR 600 mg PO; 14C-PF-06826647-LR 600 mg with 300 nCi orally as extemp prep; Drug: PF-06826647 600 mg PO; Unlabeled PF-06826647 600 mg; Drug: 14C-PF-06826647 100 ug IV; 14C-PF-06826647 100 ug IV

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
Total radioactivity in urine and feces together expressed as percent of total oral radioactive dose	Up to Day 14

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Number of Participants With Laboratory Test Values of Potential Clinical Importance	Pre-defined criteria were established for each laboratory test to define the values that would be identified as of potential clinical importance.	Up to Day 28
Number of participants with abnormal ECG	Criteria for ECG abnormalities: maximum PR interval >=300 milliseconds (msec) and maximum increase PR interval increase from baseline (IFB): percent change (Pctchg) >=25 percent (%) for baseline value of >200 msec and Pctchg>=50% for baseline value of <=200 msec for PR interval, maximum QRS interval >=140 msec and a maximum IFB: Pctchg>=50%, maximum QTCF interval (Fridericia's Correction) of 450 msec to <480 msec, 480 msec to <500 msec or >=500 msec and a maximum change of <=30change<60 or >=60 msec from baseline.	Up to Day 28
Number of Participants With Clinically Significant Change From Baseline in Vital Signs	Following parameters were analyzed for examination of vital signs: systolic and diastolic blood pressure, respiratory rate, radial pulse and body temperature.	Up to Day 28
The ratio of dose normalized AUCinf of PF-06826647 and 14C-PF-06826647	The ratio of dose normalized AUCinf of PF-06826647 (LCMS) and 14C-PF-06826647 (AMS). AUCinf= Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time . It is obtained from AUC (0 - t) plus AUC (t - ∞).	0 hours to 96 hours

Collaborators and Investigators

• Sponsor: Pfizer

Publications and helpful links

Helpful Links

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

Study record dates

Study Major Dates

• Study Start (Actual): November 10, 2020
• Primary Completion (Actual): January 28, 2021
• Study Completion (Actual): January 28, 2021

Study Registration Dates

• First Submitted: September 9, 2020
• First Submitted That Met QC Criteria: October 13, 2020
• First Posted (Actual): October 19, 2020

Study Record Updates

• Last Update Posted (Actual): February 21, 2021
• Last Update Submitted That Met QC Criteria: February 17, 2021
• Last Verified: February 1, 2021

More Information

Terms related to this study

• Keywords: ADME, Mass Balance, Absolute Bioavailability, AMS
• Other Study ID Numbers: C2501006

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: NO
• IPD Plan Description: Pfizer will provide access to individual de-identified participant data and related study documents (e.g. protocol, Statistical Analysis Plan (SAP), Clinical Study Report (CSR)) upon request from qualified researchers, and subject to certain criteria, conditions, and exceptions. Further details on Pfizer's data sharing criteria and process for requesting access can be found at: https://www.pfizer.com/science/clinical_trials/trial_data_and_results/data_requests.

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: No
• Studies a U.S. FDA-regulated device product: No