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Single Dose Study With Unlabeled Dose and 14C-labeled Microdose of PF-06700841 in Healthy Male Subjects

A PHASE 1, OPEN-LABEL, NON-RANDOMIZED, 2-PERIOD, FIXED SEQUENCE STUDY TO INVESTIGATE THE ABSORPTION, DISTRIBUTION, METABOLISM AND EXCRETION OF [14C-PF-06700841] AND TO ASSESS THE ABSOLUTE BIOAVAILABILITY AND FRACTION ABSORBED OF PF-06700841 IN HEALTHY MALE SUBJECTS USING A 14C-MICROTRACER APPROACH

Status
Completed
Phases
Phase 1
Study type
Interventional
Source
ClinicalTrials.gov
Registry ID
NCT03770039
Enrollment
6
Registered
2018-12-10
Start date
2018-12-10
Completion date
2019-02-21
Last updated
2019-03-06

For informational purposes only — not medical advice. Sourced from public registries and may not reflect the latest updates. Terms

Conditions

Healthy Male Subjects

Keywords

PF-06700841, mass balance, metabolites, absolute bioavailability

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

Interventions

DRUGOral PF-06700841 containing 14C microtracer

Oral dose of 60 mg unlabeled PF-06700841 co-formulated with 30 ug 14C-labeled (300 nCi) PF-06700841 in 1st period

DRUGOral unlabeled PF-06700841

60 mg unlabeled PF-06700841 oral dose in 2nd period

DRUGIV 14C-labeled PF-06700841

30 ug 14C-labeled (300 nCi) PF-06700841 intravenous infusion over 5 min in 2nd period

Sponsors

Pfizer
Lead SponsorINDUSTRY

Study design

Allocation
NON_RANDOMIZED
Intervention model
CROSSOVER
Primary purpose
BASIC_SCIENCE
Masking
NONE

Eligibility

Sex/Gender
MALE
Age
18 Years to 55 Years
Healthy volunteers
Yes

Exclusion criteria

* 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.

Design outcomes

Primary

MeasureTime frameDescription
mass balance_urinehour 0 up to 312 hours post dosecumulative recovery of radioactivity over time in urine, as percentage of total radioactive dose administered
mass balance_feceshour 0 up to 312 hours post dosecumulative recovery of radioactivity over time in feces, as percentage of total radioactive dose administered

Secondary

MeasureTime frameDescription
plasma Tmax for total 14C radioactivityhour 0 up to 312 hours post dosetime with highest concentration of radioactivity in plasma following a single oral dose of 14C-labeled PF-06700841
plasma AUClast for total 14C radioactivityhour 0 up to 312 hours post dosearea under curve of total 14C radioactivity in plasma from time 0 to tlast following a single oral dose of 14C-labeled PF-06700841
plasma AUCinf for total 14C radioactivityhour 0 up to 312 hours post dosearea under curve of total 14C radioactivity in plasma from time 0 to infinite following a single oral dose of 14C-labeled PF-06700841
Oral clearance for total 14C radioactivityhour 0 up to 312 hours post doseoral clearance (CL/F) of total activity following a single oral dose of 14C-labeled PF-06700841
plasma half-life for total 14C radioactivityhour 0 up to 312 hours post dosehalf-life (t1/2) of total radioactivity in plasma following a single oral dose of 14C-labeled PF-06700841
volume of distribution for total 14C radioactivityhour 0 up to 312 hours post doseapparent volume of distribution (Vz/F) of total radioactivity following a single oral dose of 14C-labeled PF-06700841
plasma Cmax for PF-06700841hour 0 up to 96 hours post dosemaximum concentration of PF-06700841 in plasma following a single oral dose of 14C-labeled or unlabeled PF-06700841
plasma Tmax for PF-06700841hour 0 up to 96 hours post dosetime with highest concentration of PF-06700841 in plasma following a single oral dose of 14C-labeled or unlabeled PF-06700841
plasma AUClast for PF-06700841hour 0 up to 96 hours post dosearea under curve of PF-06700841 in plasma from time 0 to tlast following a single oral dose of 14C-labeled or unlabeled PF-06700841
plasma AUCinf for PF-06700841hour 0 up to 96 hours post dosearea under curve of PF-06700841 in plasma from time 0 to infinite following a single oral dose of 14C-labeled or unlabeled PF-06700841
Oral clearance for PF-06700841hour 0 up to 96 hours post doseoral clearance (CL/F) of PF-06700841 following a single oral dose of 14C-labeled or unlabeled PF-06700841
plasma half-life for PF-06700841hour 0 up to 96 hours post dosehalf-life (t1/2) of PF-06700841 in plasma following a single oral dose of 14C-labeled or unlabeled PF-06700841
volume of distribution for PF-06700841hour 0 up to 96 hours post doseapparent volume of distribution (Vz/F) of PF-06700841 following a single oral dose of 14C-labeled or unlabeled PF-06700841
metabolite identification_plasmahour 0 up to 312 hours post dosemetabolic identification and profiling in plasma following a single oral dose of 14C-labeled PF-06700841
plasma Tmax for 14C-labeled PF-06700841hour 0 up to 96 hours post dosetime 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-06700841hour 0 up to 96 hours post dosearea under curve of 14C-labeled PF-06700841 in plasma from time 0 to tlast following a single iv dose of 14C-labeled PF-06700841
plasma AUCinf for 14C-labeled PF-06700841hour 0 up to 96 hours post dosearea under curve of 14C-PF-06700841 in plasma from time 0 to infinite following a single iv dose of 14C-labeled PF-06700841
clearance for 14C-labeled PF-06700841hour 0 up to 96 hours post doseclearance (CL) of 14C-labeled PF-06700841 following a single iv dose of 14C-labeled PF-06700841
plasma half-life for 14C-labeled PF-06700841hour 0 up to 96 hours post dosehalf-life (t1/2) of 14C-labeled PF-06700841 in plasma following a single iv dose of 14C-labeled PF-06700841
volume of distribution for 14C-labeled PF-06700841hour 0 up to 96 hours post dosevolume of distribution (Vz/F) of 14C-labeled PF-06700841 following a single iv dose of 14C-labeled PF-06700841
unchanged PF-06700841 recovered in urinehour 0 up to 96 hours post dosepercentage of unchanged PF-06700841 recovered in urine (Ae%) following a single oral dose of PF-06700841
renal clearance of PF-06700841hour 0 up to 96 hours post doserenal clearance (CLr) following a single oral dose of PF-06700841 (Ae%/AUCinf for PF-06700841)
Bioavailability of oral PF-06700841hour 0 up to 96 hours post doseAbsolute bioavailability (F) following a single oral dose relative to a single iv dose of PF-06700841
Fraction absorbed of oral PF-06700841hour 0 up to 144 hours post doseFraction absorbed in gut (Fa) following oral dose of PF-06700841
metabolite identification_urinehour 0 up to 312 hours post dosemetabolic identification and profiling in urine following a single oral dose of 14C-labeled PF-06700841
metabolite identification_feceshour 0 up to 312 hours post dosemetabolic identification and profiling in feces following a single oral dose of 14C-labeled PF-06700841
plasma Cmax for 14C-labeled PF-06700841hour 0 up to 96 hours post dosemaximum concentration of 14C-labeled PF-06700841 in plasma following a single iv dose of 14C-labeled PF-06700841
plasma Cmax for total 14C radioactivityhour 0 up to 312 hours post dosemaximum concentration of total 14C radioactivity in plasma following a single oral dose of 14C-labeled PF-06700841

Countries

Netherlands

Outcome results

None listed

Source: ClinicalTrials.gov · Data processed: Feb 13, 2026