Single Dose Study With Unlabeled Dose and 14C-labeled Microdose of PF-06700841 in Healthy Male Subjects
- Conditions
- Healthy Male Subjects
- Interventions
- Registration Number
- NCT03770039
- Lead Sponsor
- Pfizer
- Brief Summary
An open-label, fixed sequence, 2-period including a single oral dose 60 mg PF-06700841 with 14C-labeled microtracer in 1st period, and a single oral dose of 60 mg unlabeled PF-06700841 followed by intravenous administration of 14C-labeled microdose of PF-06700841 1 hour after oral dose in period 2 to characterize the absorption, disposition, metabolism and excretion of PF-06700841 and evaluate the absolute bioavailability and fraction absorbed in the GI tract
- Detailed Description
Not available
Recruitment & Eligibility
- Status
- COMPLETED
- Sex
- Male
- Target Recruitment
- 6
Not provided
- Any clinically significant malabsorption condition (eg, gastrectomy, bowel resection).
- Total 14C radioactivity measured in plasma exceeding 11 mBq/mL
- History of tuberculosis or active or latent or inadequately treated infection, positive QuantiFERON®-TB Gold test
- Use of tobacoo/nicotine containing products 3-m prior to dosing or positive urine cotinine test
- Use of herbal supplements within 28 days prior to the first dose of study medication
- Use of prescription or nonprescription drugs (including vitamins and dietary supplements) within 7 days or 5 half-lives (whichever is longer) prior to the first dose of study medication. As an exception, acetaminophen may be used at doses of 1 g/day. Limited use of non-prescription medications that are not believed to affect subject safety or the overall results of the study may be permitted on a case-by-case basis following approval by Pfizer
- Inability to have at least one bowel movement every 2 days on average eGFR of <90 mL/mim/1.73 m2 based on MDRD equation
- Have been vaccinated with live or attenuated live vaccine within the 6 weeks prior to the first dose of investigational product, or expects to be vaccinated with these vaccines during study treatment, or within the 6 weeks following the last dose of investigational product.
Study & Design
- Study Type
- INTERVENTIONAL
- Study Design
- CROSSOVER
- Arm && Interventions
Group Intervention Description 2-period, fixed sequence Oral PF-06700841 containing 14C microtracer fixed sequence with 2 treatment period 2-period, fixed sequence Oral unlabeled PF-06700841 fixed sequence with 2 treatment period 2-period, fixed sequence IV 14C-labeled PF-06700841 fixed sequence with 2 treatment period
- Primary Outcome Measures
Name Time Method mass balance_urine hour 0 up to 312 hours post dose cumulative recovery of radioactivity over time in urine, as percentage of total radioactive dose administered
mass balance_feces hour 0 up to 312 hours post dose cumulative recovery of radioactivity over time in feces, as percentage of total radioactive dose administered
- Secondary Outcome Measures
Name Time Method plasma Tmax for total 14C radioactivity hour 0 up to 312 hours post dose time with highest concentration of radioactivity in plasma following a single oral dose of 14C-labeled PF-06700841
plasma AUCinf for total 14C radioactivity hour 0 up to 312 hours post dose area under curve of total 14C radioactivity in plasma from time 0 to infinite following a single oral dose of 14C-labeled PF-06700841
plasma Cmax for PF-06700841 hour 0 up to 96 hours post dose maximum concentration of PF-06700841 in plasma following a single oral dose of 14C-labeled or unlabeled PF-06700841
plasma Tmax for PF-06700841 hour 0 up to 96 hours post dose time with highest concentration of PF-06700841 in plasma following a single oral dose of 14C-labeled or unlabeled PF-06700841
plasma AUCinf for 14C-labeled PF-06700841 hour 0 up to 96 hours post dose area under curve of 14C-PF-06700841 in plasma from time 0 to infinite following a single iv dose of 14C-labeled PF-06700841
Oral clearance for total 14C radioactivity hour 0 up to 312 hours post dose oral clearance (CL/F) of total activity following a single oral dose of 14C-labeled PF-06700841
plasma half-life for total 14C radioactivity hour 0 up to 312 hours post dose half-life (t1/2) of total radioactivity in plasma following a single oral dose of 14C-labeled PF-06700841
plasma AUClast for PF-06700841 hour 0 up to 96 hours post dose area under curve of PF-06700841 in plasma from time 0 to tlast following a single oral dose of 14C-labeled or unlabeled PF-06700841
Oral clearance for PF-06700841 hour 0 up to 96 hours post dose oral clearance (CL/F) of PF-06700841 following a single oral dose of 14C-labeled or unlabeled PF-06700841
plasma half-life for PF-06700841 hour 0 up to 96 hours post dose half-life (t1/2) of PF-06700841 in plasma following a single oral dose of 14C-labeled or unlabeled PF-06700841
plasma Cmax for 14C-labeled PF-06700841 hour 0 up to 96 hours post dose maximum concentration of 14C-labeled PF-06700841 in plasma following a single iv dose of 14C-labeled PF-06700841
plasma half-life for 14C-labeled PF-06700841 hour 0 up to 96 hours post dose half-life (t1/2) of 14C-labeled PF-06700841 in plasma following a single iv dose of 14C-labeled PF-06700841
renal clearance of PF-06700841 hour 0 up to 96 hours post dose renal clearance (CLr) following a single oral dose of PF-06700841 (Ae%/AUCinf for PF-06700841)
metabolite identification_plasma hour 0 up to 312 hours post dose metabolic identification and profiling in plasma following a single oral dose of 14C-labeled PF-06700841
plasma Cmax for total 14C radioactivity hour 0 up to 312 hours post dose maximum concentration of total 14C radioactivity in plasma following a single oral dose of 14C-labeled PF-06700841
plasma AUClast for total 14C radioactivity hour 0 up to 312 hours post dose area under curve of total 14C radioactivity in plasma from time 0 to tlast following a single oral dose of 14C-labeled PF-06700841
volume of distribution for total 14C radioactivity hour 0 up to 312 hours post dose apparent volume of distribution (Vz/F) of total radioactivity following a single oral dose of 14C-labeled PF-06700841
plasma AUCinf for PF-06700841 hour 0 up to 96 hours post dose area under curve of PF-06700841 in plasma from time 0 to infinite following a single oral dose of 14C-labeled or unlabeled PF-06700841
volume of distribution for PF-06700841 hour 0 up to 96 hours post dose apparent volume of distribution (Vz/F) of PF-06700841 following a single oral dose of 14C-labeled or unlabeled PF-06700841
plasma Tmax for 14C-labeled PF-06700841 hour 0 up to 96 hours post dose time with highest concentration of 14C-labeled PF-06700841 in plasma following a single iv dose of 14C-labeled PF-06700841
plasma AUClast for 14C-labeled PF-06700841 hour 0 up to 96 hours post dose area under curve of 14C-labeled PF-06700841 in plasma from time 0 to tlast following a single iv dose of 14C-labeled PF-06700841
clearance for 14C-labeled PF-06700841 hour 0 up to 96 hours post dose clearance (CL) of 14C-labeled PF-06700841 following a single iv dose of 14C-labeled PF-06700841
Bioavailability of oral PF-06700841 hour 0 up to 96 hours post dose Absolute bioavailability (F) following a single oral dose relative to a single iv dose of PF-06700841
metabolite identification_urine hour 0 up to 312 hours post dose metabolic identification and profiling in urine following a single oral dose of 14C-labeled PF-06700841
metabolite identification_feces hour 0 up to 312 hours post dose metabolic identification and profiling in feces following a single oral dose of 14C-labeled PF-06700841
volume of distribution for 14C-labeled PF-06700841 hour 0 up to 96 hours post dose volume of distribution (Vz/F) of 14C-labeled PF-06700841 following a single iv dose of 14C-labeled PF-06700841
unchanged PF-06700841 recovered in urine hour 0 up to 96 hours post dose percentage of unchanged PF-06700841 recovered in urine (Ae%) following a single oral dose of PF-06700841
Fraction absorbed of oral PF-06700841 hour 0 up to 144 hours post dose Fraction absorbed in gut (Fa) following oral dose of PF-06700841
Trial Locations
- Locations (2)
PRA Health Sciences
🇳🇱Groningen, Netherlands
PRA Health Sciences Utrecht
🇳🇱Utrecht, Netherlands