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.
Study Type
INTERVENTIONAL
Allocation
NON_RANDOMIZED
Purpose
BASIC_SCIENCE
Masking
NONE
Enrollment
6
Oral solution of 200 mg 14C labeled PF-06651600 containing approximately 300 nCi radioactivity
IV solution 60 micrograms of 14C labeled PF-06651600 containing approximately 300 nCi radioactivity
Oral solution 200mg
PRA Health Sciences
Groningen, Netherlands
PRA Health Sciences Utrecht
Utrecht, Netherlands
Mass Balance: Cumulative recovery (%) of radioactivity in urine
Cumulative recovery (%) of radioactivity in urine.
Time frame: from time zero to the time of last measurable concentration following oral administration of 14C PF-06651600 microtracer dose up to day 24
Mass Balance: Cumulative recovery (%) of radioactivity in feces
Cumulative recovery (%) of radioactivity in feces
Time frame: from time zero to the time of last measurable concentration following oral administration of 14C PF-06651600 microtracer dose up to day 24
Amount (% of the administered dose) of major metabolites of PF-06651600 in plasma
Time frame: Hour 0 up to 312 hours post-dose.
Amount (% of the administered dose) of major metabolites of PF-06651600 in urine
Time frame: Hour 0 up to 312 hours post-dose.
Amount (% of the administered dose) of major metabolites of PF-06651600 in feces
Time frame: Hour 0 up to 312 hours post-dose.
Cmax
Maximum plasma concentration
Time frame: 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
AUClast
Area under the plasma concentration time profile from time 0 to time of the last quantifiable concentration (Clast)
Time frame: 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
AUCinf
Area under the plasma concentration time profile from time 0 to infinity
This platform is for informational purposes only and does not constitute medical advice. Always consult a qualified healthcare professional.
Time frame: 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
Tmax
Time for Cmax
Time frame: 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
t1/2
Plasma decay half-life is the time measured for the plasma concentration to decrease by one half.
Time frame: 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
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.
Time frame: 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
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.
Time frame: 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
Vss
Steady state volume of distribution following IV infusion
Time frame: 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
Vz/F
Apparent volume of distribution following oral administration
Time frame: 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
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
Time frame: Pre-dose, Day1, day 2, day 3, day 4, day 5, day 6 and day 7 post-dose
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
Time frame: Pre-dose, Day1, day 2, day 3, day 4, day 5, day 6 and day 7 post-dose
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.
Time frame: Baseline (Day 0) up to 90 days after last dose of study medication
Number of participants with clinically significant changes to the physical examination
clinically significant changes to the physical examination
Time frame: Baseline (Day 0) up to Day 24
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.
Time frame: Baseline (Day 0) up to Day 24
Number of Participants With Clinically Significant Change From Baseline in Laboratory Abnormalities
Laboratory parameters include: hematological and chemical parameters
Time frame: Baseline (Day 0) up to Day 24