B7981011: Study to Characterize Absorption, Distribution, Metabolism and Excretion of 14C PF-06651600 and to Evaluate the Absolute Oral Bioavailability and Fraction Absorbed of PF-06651600.

Sponsor

Pfizer (Industry)

Overall Status

Completed

CT.gov ID

NCT03929510

Collaborator

(none)

Enrollment

Locations

Arms

2.4

Actual Duration (Months)

Patients Per Site

1.3

Patients Per Site Per Month

Study Details

Study Description

Brief Summary

This study will investigate the absorption, distribution, metabolism and excretion (ADME) of 14C PF-06651600 and characterize plasma, fecal and urinary radioactivity and identify any metabolites, if possible, of 14C PF-06651600 in humans.

Condition or Disease	Intervention/Treatment	Phase
Healthy Volunteers	Drug: 14C-PF-06651600 Drug: 14C-PF-06651600 IV Drug: PF-06651600	Phase 1

Study Design

Study Type:

Interventional

Actual Enrollment :

6 participants

Allocation:

Non-Randomized

Intervention Model:

Sequential Assignment

Masking:

None (Open Label)

Primary Purpose:

Basic Science

Official Title:

A PHASE 1, OPEN-LABEL, NON-RANDOMIZED, 2-PERIOD, FIXED SEQUENCE STUDY TO INVESTIGATE THE ABSORPTION, DISTRIBUTION, METABOLISM AND EXCRETION OF 14C-PF-06651600 AND TO ASSESS THE ABSOLUTE BIOAVAILABILITY AND FRACTION ABSORBED OF PF-06651600 IN HEALTHY MALE PARTICIPANTS USING A 14C-MICROTRACER APPROACH

Actual Study Start Date :

Apr 23, 2019

Actual Primary Completion Date :

Jul 5, 2019

Actual Study Completion Date :

Jul 5, 2019

Arms and Interventions

Arm	Intervention/Treatment
Experimental: Period A Single oral dose of 200 mg 14C labeled PF-06651600 containing approximately 300 nCi 14C (ie, radiolabeled PF 06651600).	Drug: 14C-PF-06651600 Oral solution of 200 mg 14C labeled PF-06651600 containing approximately 300 nCi radioactivity
Experimental: Period B Single oral dose of 200 milligrams (mg) unlabeled PF-06651600 followed at time of peak plasma concentration (Tmax) by an Intravenous (IV) dose of 60 micrograms.14C -PF-06651600 containing approximately 300 nCi 14C (ie, radiolabeled PF-06651600).	Drug: 14C-PF-06651600 IV IV solution 60 micrograms of 14C labeled PF-06651600 containing approximately 300 nCi radioactivity Drug: PF-06651600 Oral solution 200mg

Arm

Intervention/Treatment

Experimental: Period A

Single oral dose of 200 mg 14C labeled PF-06651600 containing approximately 300 nCi 14C (ie, radiolabeled PF 06651600).

Drug: 14C-PF-06651600

Oral solution of 200 mg 14C labeled PF-06651600 containing approximately 300 nCi radioactivity

Experimental: Period B

Single oral dose of 200 milligrams (mg) unlabeled PF-06651600 followed at time of peak plasma concentration (Tmax) by an Intravenous (IV) dose of 60 micrograms.14C -PF-06651600 containing approximately 300 nCi 14C (ie, radiolabeled PF-06651600).

Drug: 14C-PF-06651600 IV

IV solution 60 micrograms of 14C labeled PF-06651600 containing approximately 300 nCi radioactivity

Drug: PF-06651600

Oral solution 200mg

Outcome Measures

Primary Outcome Measures

Mass Balance: Cumulative recovery (%) of radioactivity in urine [from time zero to the time of last measurable concentration following oral administration of 14C PF-06651600 microtracer dose up to day 24]
Cumulative recovery (%) of radioactivity in urine.
Mass Balance: Cumulative recovery (%) of radioactivity in feces [from time zero to the time of last measurable concentration following oral administration of 14C PF-06651600 microtracer dose up to day 24]
Cumulative recovery (%) of radioactivity in feces

Secondary Outcome Measures

Amount (% of the administered dose) of major metabolites of PF-06651600 in plasma [Hour 0 up to 312 hours post-dose.]
Amount (% of the administered dose) of major metabolites of PF-06651600 in urine [Hour 0 up to 312 hours post-dose.]
Amount (% of the administered dose) of major metabolites of PF-06651600 in feces [Hour 0 up to 312 hours post-dose.]
Cmax [Pre-dose, 0.25. 0.5, 1, 1.5, 2, 3.5, 4.5, 6.5, 8.5, 12.5, 24, 48, 72, 96 hours post-dose]
Maximum plasma concentration
AUClast [Pre-dose, 0.25. 0.5, 1, 1.5, 2, 3.5, 4.5, 6.5, 8.5, 12.5, 24, 48, 72, 96 hours post-dose]
Area under the plasma concentration time profile from time 0 to time of the last quantifiable concentration (Clast)
AUCinf [Pre-dose, 0.25. 0.5, 1, 1.5, 2, 3.5, 4.5, 6.5, 8.5, 12.5, 24, 48, 72, 96 hours post-dose]
Area under the plasma concentration time profile from time 0 to infinity
Tmax [Pre-dose, 0.25. 0.5, 1, 1.5, 2, 3.5, 4.5, 6.5, 8.5, 12.5, 24, 48, 72, 96 hours post-dose]
Time for Cmax
t1/2 [Pre-dose, 0.25. 0.5, 1, 1.5, 2, 3.5, 4.5, 6.5, 8.5, 12.5, 24, 48, 72, 96 hours post-dose]
Plasma decay half-life is the time measured for the plasma concentration to decrease by one half.
CL (IV) [Pre-dose, 0.25. 0.5, 1, 1.5, 2, 3.5, 4.5, 6.5, 8.5, 12.5, 24, 48, 72, 96 hours post-dose]
Drug clearance is a quantitative measure of the rate at which a drug substance is removed from the blood (rate at which a drug is metabolized or eliminated by normal biological processes). Clearance obtained after intravenous infusion dose (apparent clearance) is influenced by the fraction of the dose absorbed.
CL/F (oral) [Pre-dose, 0.25. 0.5, 1, 1.5, 2, 3.5, 4.5, 6.5, 8.5, 12.5, 24, 48, 72, 96 hours post-dose]
Drug clearance is a quantitative measure of the rate at which a drug substance is removed from the blood (rate at which a drug is metabolized or eliminated by normal biological processes). Clearance obtained after intravenous infusion dose (apparent clearance) is influenced by the fraction of the dose absorbed.
Vss [Pre-dose, 0.25. 0.5, 1, 1.5, 2, 3.5, 4.5, 6.5, 8.5, 12.5, 24, 48, 72, 96 hours post-dose]
Steady state volume of distribution following IV infusion
Vz/F [Pre-dose, 0.25. 0.5, 1, 1.5, 2, 3.5, 4.5, 6.5, 8.5, 12.5, 24, 48, 72, 96 hours post-dose]
Apparent volume of distribution following oral administration
Total 14C_Urine_PO [Pre-dose, Day1, day 2, day 3, day 4, day 5, day 6 and day 7 post-dose]
Total radioactivity excreted into the urine from time zero to the time of last measurable concentration following oral administration of 14C PF 06651600 microtracer dose
Total 14C_Urine_IV [Pre-dose, Day1, day 2, day 3, day 4, day 5, day 6 and day 7 post-dose]
Total radioactivity excreted into the urine from time zero to the time of last measurable concentration following IV administration of 14C PF 06651600 microtracer dose
AE [Baseline (Day 0) up to 90 days after last dose of study medication]
Number of subjects and number of AEs which are any untoward medical occurrence regardless of attribution to study drug in a participant who received study drug.
Number of participants with clinically significant changes to the physical examination [Baseline (Day 0) up to Day 24]
clinically significant changes to the physical examination
Number of Participants With Clinically Significant Change From Baseline in Vital Signs [Baseline (Day 0) up to Day 24]
Vital signs (temperature, respiratory rate, pulse, systolic and diastolic blood pressure) obtained from each participant. Clinical significance of vital signs was determined at the investigator's discretion.
Number of Participants With Clinically Significant Change From Baseline in Laboratory Abnormalities [Baseline (Day 0) up to Day 24]
Laboratory parameters include: hematological and chemical parameters

Eligibility Criteria

Criteria

Ages Eligible for Study:

18 Years to 55 Years

Sexes Eligible for Study:

Male

Accepts Healthy Volunteers:

Yes

Inclusion Criteria:

Male participants who are healthy as determined by medical evaluation including a detailed medical history, full physical examination, including blood pressure (BP) and pulse rate (PR) measurement, 12 lead ECG, and clinical laboratory tests.
Body mass index (BMI) of 17.5 to 30.5 kg/m2; and a total body weight >50 kg (110 lb).

Exclusion Criteria:

Known immunodeficiency disorder, including positive serology for human immunodeficiency virus (HIV) at screening, or a first degree relative with a hereditary immunodeficiency.
Infection with hepatitis B or hepatitis C viruses.
Participants with selected acute or chronic infections or infection history.
Participants have a known present or a history of malignancy other than a successfully treated or excised non metastatic basal cell or squamous cell cancer of the skin.
History of alcohol abuse or binge drinking and/or any other illicit drug use or dependence within 6 months of Screening.
Use of tobacco/nicotine containing products within 3 months prior to dosing or positive urine cotinine test.

Contacts and Locations

Locations

	Site	City	State	Country	Postal Code
1	PRA Health Sciences	Groningen		Netherlands	9728 NZ
2	PRA Health Sciences Utrecht	Utrecht		Netherlands	3584 BL

Sponsors and Collaborators

Pfizer

Investigators

Study Director: Pfizer CT.gov Call Center, Pfizer

Study Documents (Full-Text)

None provided.

More Information

Additional Information:

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

Publications

None provided.

Responsible Party:

Pfizer

ClinicalTrials.gov Identifier:

NCT03929510

Other Study ID Numbers:

B7981011
2018-003551-38

First Posted:

Apr 29, 2019

Last Update Posted:

Jul 24, 2019

Last Verified:

Jul 1, 2019

Individual Participant Data (IPD) Sharing Statement:

Plan to Share IPD:

Studies a U.S. FDA-regulated Drug Product:

Yes

Studies a U.S. FDA-regulated Device Product:

Product Manufactured in and Exported from the U.S.:

Yes

Keywords provided by Pfizer

Phase 1

Male

healthy

Study Results

No Results Posted as of Jul 24, 2019