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.

Healthy Volunteers Clinical Trial

— B7981011  

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

Clinical Trial Details — Status: Completed

Administrative data

• NCT number: NCT03929510
• Other study ID #: B7981011
• Secondary ID: 2018-003551-38
• Status: Completed
• Phase: Phase 1
• Start date: April 23, 2019
• Est. completion date: July 5, 2019

Study information

• Verified date: July 2019
• Source: Pfizer
• Contact: n/a
• Is FDA regulated: No
• Study type: Interventional

Clinical Trial 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.

Recruitment information / eligibility

• Status: Completed
• Enrollment: 6
• Est. completion date: July 5, 2019
• Est. primary completion date: July 5, 2019
• Accepts healthy volunteers: Accepts Healthy Volunteers
• Gender: Male
• Age group: 18 Years to 55 Years

Eligibility

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.

Related Conditions & MeSH terms

• Healthy Volunteers

Intervention

Drug:
• 14C-PF-06651600
Oral solution of 200 mg 14C labeled PF-06651600 containing approximately 300 nCi radioactivity
• 14C-PF-06651600 IV
IV solution 60 micrograms of 14C labeled PF-06651600 containing approximately 300 nCi radioactivity
• PF-06651600
Oral solution 200mg

Locations

Country	Name	City	State
Netherlands	PRA Health Sciences	Groningen
Netherlands	PRA Health Sciences Utrecht	Utrecht

Sponsors (1)

Lead Sponsor	Collaborator
Pfizer

Country where clinical trial is conducted

Netherlands, 

Outcome

Type	Measure	Description	Time frame	Safety issue
Primary	Mass Balance: Cumulative recovery (%) of radioactivity in urine	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
Primary	Mass Balance: Cumulative recovery (%) of radioactivity in feces	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
Secondary	Amount (% of the administered dose) of major metabolites of PF-06651600 in plasma		Hour 0 up to 312 hours post-dose.
Secondary	Amount (% of the administered dose) of major metabolites of PF-06651600 in urine		Hour 0 up to 312 hours post-dose.
Secondary	Amount (% of the administered dose) of major metabolites of PF-06651600 in feces		Hour 0 up to 312 hours post-dose.
Secondary	Cmax	Maximum plasma concentration	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
Secondary	AUClast	Area under the plasma concentration time profile from time 0 to time of the last quantifiable concentration (Clast)	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
Secondary	AUCinf	Area under the plasma concentration time profile from time 0 to infinity	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
Secondary	Tmax	Time for 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
Secondary	t1/2	Plasma decay half-life is the time measured for the plasma concentration to decrease by one half.	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
Secondary	CL (IV)	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.	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
Secondary	CL/F (oral)	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.	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
Secondary	Vss	Steady state volume of distribution following IV infusion	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
Secondary	Vz/F	Apparent volume of distribution following oral administration	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
Secondary	Total 14C_Urine_PO	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	Pre-dose, Day1, day 2, day 3, day 4, day 5, day 6 and day 7 post-dose
Secondary	Total 14C_Urine_IV	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	Pre-dose, Day1, day 2, day 3, day 4, day 5, day 6 and day 7 post-dose
Secondary	AE	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.	Baseline (Day 0) up to 90 days after last dose of study medication
Secondary	Number of participants with clinically significant changes to the physical examination	clinically significant changes to the physical examination	Baseline (Day 0) up to Day 24
Secondary	Number of Participants With Clinically Significant Change From Baseline in Vital Signs	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.	Baseline (Day 0) up to Day 24
Secondary	Number of Participants With Clinically Significant Change From Baseline in Laboratory Abnormalities	Laboratory parameters include: hematological and chemical parameters	Baseline (Day 0) up to Day 24

External Links

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