Healthy Volunteers
Conditions
Keywords
Phase 1, Male, healthy
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.
Interventions
DRUG14C-PF-06651600
Oral solution of 200 mg 14C labeled PF-06651600 containing approximately 300 nCi radioactivity
DRUG14C-PF-06651600 IV
IV solution 60 micrograms of 14C labeled PF-06651600 containing approximately 300 nCi radioactivity
DRUGPF-06651600
Oral solution 200mg
Sponsors
Pfizer
Study design
Allocation
NON_RANDOMIZED
Intervention model
SEQUENTIAL
Primary purpose
BASIC_SCIENCE
Masking
NONE
Eligibility
Sex/Gender
MALE
Age
18 Years to 55 Years
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.
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| 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
| Measure | Time frame | Description |
|---|---|---|
| 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. |
| Amount (% of the administered dose) of major metabolites of PF-06651600 in plasma | Hour 0 up to 312 hours post-dose. | — |
| 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 |
| 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 |
| Amount (% of the administered dose) of major metabolites of PF-06651600 in urine | Hour 0 up to 312 hours post-dose. | — |
Countries
Netherlands
Outcome results
None listed