Clinical trial NCT06392230: A Study to Learn How the Medicine Called [14C] PF-06821497 is Taken up Into and Removed From the Body.
Official title: A PHASE 1, OPEN-LABEL, FIXED-SEQUENCE, 2-PERIOD STUDY IN HEALTHY ADULT MALE PARTICIPANTS TO ASSESS THE MASS BALANCE, ABSOLUTE BIOAVAILABILITY, FRACTION ABSORBED, AND PHARMACOKINETICS OF [14C]PF-06821497 USING A 14C-MICROTRACER APPROACH
Study type: INTERVENTIONAL
Overall status: COMPLETED
Phase: PHASE1
Conditions: Healthy Participants
Keywords: Absorption
Distribution
Metabolism
Elimination
ADME (Absorption, Distribution, Metabolism, and Excretion)
Pharmacokinetics
Bioavailability
Fraction absorbed
Mass balance
Healthy Males
Enhancer of zeste homolog 2 (EZH2) inhibitor
Lead sponsor: Pfizer
Sponsor class: INDUSTRY
First posted: 2024-04-30
Enrollment: 6
Sex: MALE
Minimum age (years): 18
Standard ages: ADULT
OLDER_ADULT
Accepts healthy volunteers: yes
Allocation: NA
Intervention model: SINGLE_GROUP
Primary purpose: BASIC_SCIENCE

Brief summary: The purpose of this study is to learn how a certain amount of \[14C\] PF-06821497 is taken up into the bloodstream and removed from the body.

The study is seeking participants who are:

* Males aged 18 years or older.
* Are confirmed to be healthy after performing some medical and physical tests.
* Weigh more than 50 kilograms and have a body mass index of 16 to 32 kg per meter squared.

The study consists of two parts. In part one, all participants will receive one full dose of \[14C\]PF-06821497 by mouth. Part two will begin at least 14 days after the dose in part one. In part two participants will receive one full dose of PF-06821497 by mouth and one small dose of \[14C\]PF-06821497 by intravenous (IV) infusion. IV infusion will be directly injected into the veins.

To understand how the medicine is processed in the body, samples of blood, urine, and feces will be collected after each dose is given. This will help understand:

* How much PF-06821497 is taken up into the bloodstream when taken by mouth compared to the dose given by IV
* How the body removes it from the bloodstream.

Participants will take part in the study for about 11 weeks, including the initial evaluation and follow-up periods.


Eligibility criteria: Key eligibility criteria for this study include, but are not limited to the following:

Inclusion Criteria:

* Male participants aged 18 years at screening who are overtly healthy as determined by medical evaluation including medical history, physical examination, laboratory tests, and cardiac monitoring.
* Body mass index (BMI) of 16-32 kg/m2; and a total body weight of \>50kg (110lb)
* Participants who are willing to comply with all scheduled visits, treatment plan, laboratory tests, lifestyle considerations, and other study procedures

Exclusion Criteria:

* Any condition possibly affecting drug absorption (eg, gastrectomy, cholecystectomy, prior bariatric surgery, ileal resection, inflammatory gastrointestinal disease, chronic diarrhea, known diverticular disease).
* Chronic liver diseases including alcoholic liver disease, viral hepatitis, primary biliary cirrhosis, primary sclerosing cholangitis, autoimmune hepatitis, Wilson's disease, hemochromatosis, alpha-1 antitrypsin deficiency, human immunodeficiency virus, or other chronic liver disease.
* Previous administration with an investigational product (drug or vaccine) within 30 days (or as determined by the local requirement) or 5 half lives preceding the first dose of study intervention used in this study (whichever is longer). Participation in studies of other investigational products (drug or vaccine) at any time during their participation in this study.
* Total \[14C\] radioactivity measured in plasma at screening exceeding 11 mBq/mL

Primary outcomes:
measure: Total recovery of radioactivity in urine, feces, and total excreta (urine + feces) as percentage of total radioactive dose administered
timeFrame: Period 1 pre-dose to maximum Day 14
measure: Metabolic profiling/identification and determination of relative abundance of [14C]PF-06821497 and the metabolites of [14C]PF-06821497 in plasma, urine, and feces
timeFrame: Period 1 pre-dose to maximum Day 14
Secondary outcomes:
measure: Absolute oral bioavailability (F) of [14C]PF-06821497
timeFrame: Period 2 pre-dose to maximum Day 5
measure: Fraction of [14C]PF 06821497 dose absorbed (Fa)
timeFrame: Period 1 pre-dose to maximum Day 14; Period 2 pre-IV dose to maximum Day 5
measure: AUClast of total radioactivity and PF-06821497 in plasma
timeFrame: Period 1 pre-dose to maximum Day 14
measure: Cmax of total radioactivity and PF-06821497 in plasma
timeFrame: Period 1 pre-dose to maximum Day 14
measure: Tmax of total radioactivity and PF-06821497 in plasma
timeFrame: Period 1 pre-dose to maximum Day 14
measure: AUCinf of total radioactivity and PF-06821497 in plasma
timeFrame: Period 1 pre-dose to maximum Day 14
measure: t½ of total radioactivity and PF-06821497 in plasma
timeFrame: Period 1 pre-dose to maximum Day 14
measure: AUClast of [14C]PF-06821497 in plasma
timeFrame: Period 2 pre-dose to maximum Day 5
measure: Cmax of [14C]PF-06821497 in plasma
timeFrame: Period 2 pre-dose to maximum Day 5
measure: Tmax of [14C]PF-06821497 in plasma
timeFrame: Period 2 pre-dose to maximum Day 5
measure: t½ of [14C]PF-06821497 in plasma
timeFrame: Period 2 pre-dose to maximum Day 5
measure: AUCinf of [14C]PF-06821497 in plasma
timeFrame: Period 2 pre-dose to maximum Day 5
measure: CL of [14C]PF-06821497 in plasma
timeFrame: Period 2 pre-dose to maximum Day 5
measure: Vss of [14C]PF-06821497 in plasma
timeFrame: Period 2 pre-dose to maximum Day 5
measure: Number of participants with treatment emergent clinically significant laboratory abnormalities
timeFrame: Both cohorts from pre-dose to 28 days post-dose
measure: Number of participants with treatment emergent clinically significant abnormal ECG measurements
timeFrame: Both cohorts from pre-dose to 28 days post-dose
measure: Number of participants with treatment emergent clinically significant abnormal vital measurements
timeFrame: Both cohorts from pre-dose to 28 days post-dose
measure: Number of participants with treatment emergent clinically significant abnormal physical examination
timeFrame: Both cohorts from pre-dose to 28 days post-dose
measure: Number of participants with treatment-emergent adverse events (AEs) or serious adverse events (SAEs)
timeFrame: Both cohorts from pre-dose to 28 days post-dose
Other outcomes:
Locations:
city: Groningen
country: Netherlands
facility: PRA Health Sciences
Study officials:
affiliation: Pfizer
name: Pfizer CT.gov Call Center
role: STUDY_DIRECTOR
References: