A Study to Understand How the Study Medicine (PF-07081532) is Processed and Eliminated in Healthy Men
Study Details
Study Description
Brief Summary
The purpose of this clinical trial is to learn about how much PF-07081532 will be taken up and processed by healthy male participants. The study consists of two parts, called study periods. In Period 1, participants will take one dose of PF-07081532 by mouth. In Period 2, participants will take one dose by mouth and one dose as an injection through a vein at the study clinic.
In Period 1, participants will stay at the clinic site for up to 21 days. In Period 2, they will stay at the clinic site for 7 days. During their stays, participants will have their blood, urine, and feces collected by the study doctors several times. We will measure the level of PF-07081532 in participants' blood, urine, and feces samples. This will help us know how much the study medicine is getting taken in by the body. At the end of the study, participants will be contacted by phone to check in. Participants will be involved in this study for about 12 weeks.
| Condition or Disease | Intervention/Treatment | Phase |
|---|---|---|
|
Phase 1 |
Study Design
Arms and Interventions
| Arm | Intervention/Treatment |
|---|---|
| Experimental: One group of healthy adult male participants
|
Drug: Oral [14C]PF-07081532
A single oral dose of [14C]PF-07081532, will be administered as a liquid formulation in study period 1.
Drug: Oral PF-07081532 and IV [14C]PF-07081532
In study period 2: a single, oral, unlabeled dose of PF-07081532 will be administered as a liquid formulation. Approximately 1 hours after the administration of the unlabeled oral dose, a single dose of [14C]PF-07081532 will be administered via intravenous infusion.
|
Outcome Measures
Primary Outcome Measures
- Total recovery of radioactivity in urine, feces, and emesis (if any), and both routes combined, expressed as a percent of total oral radioactive dose administered. [Period 1 Pre-dose to maximum Day 21]
To characterize the extent of excretion of total radioactivity in urine, feces, and emesis (if any) following administration of a single oral dose of [14C]PF-07081532.
- Amount of metabolites of [14C]PF-07081532 in plasma, urine, and feces. [0, 0.5, 1, 2, 4, 6, 8, 10, 12, 24, 36, 48, 72, 96, 120, 144-480 hour]
To characterize the metabolic profile and identify circulating and excreted metabolites following administration of a single oral dose of [14C]PF-07081532.
Secondary Outcome Measures
- AUClast of oral radiolabeled PF-07081532 in plasma [Period 1: Pre-dose, 0.5, 1, 2, 4, 6, 8, 12, 15, 24, 36, 48, 72, 96, 120, 144 hours post-dose]
Area under the plasma concentration-time profile from time zero to time of the last quantifiable concentration (Clast) of radiolabeled PF-07081532 following administration of a single oral dose of radiolabeled PF-07081532.
- Cmax of oral radiolabeled PF-07081532 in plasma [Period 1: Pre-dose, 0.5, 1, 2, 4, 6, 8, 12, 15, 24, 36, 48, 72, 96, 120, 144 hours post-dose]
Maximum plasma concentration of radiolabeled PF-07081532 following administration of a single oral dose of radiolabeled PF-07081532.
- Tmax of oral radiolabeled PF-07081532 in plasma [Period 1: Pre-dose, 0.5, 1, 2, 4, 6, 8, 12, 15, 24, 36, 48, 72, 96, 120, 144 hours post-dose]
Time to Cmax of radiolabeled PF-07081532 following administration of a single oral dose of radiolabeled PF-07081532.
- AUCinf of oral radiolabeled PF-07081532 in plasma (if data permit) [Period 1: Pre-dose, 0.5, 1, 2, 4, 6, 8, 12, 15, 24, 36, 48, 72, 96, 120, 144 hours post-dose]
Area under the plasma concentration-time profile from time zero extrapolated to infinite time following administration of a single oral dose of radiolabeled PF-07081532.
- t1/2 of oral radiolabeled PF-07081532 in plasma (if data permit) [Period 1: Pre-dose, 0.5, 1, 2, 4, 6, 8, 12, 15, 24, 36, 48, 72, 96, 120, 144 hours post-dose]
Terminal elimination half-life following administration of a single oral dose of radiolabeled PF-07081532.
- AUClast of total radioactivity in plasma [Period 1: Pre-dose, 0.5, 1, 2, 4, 6, 8, 12, 15, 24, 36, 48, 72, 96, 120, 144-480 hours post-dose]
Area under the plasma concentration-time profile from time zero to time of the last quantifiable concentration (Clast) of total radioactivity following administration of a single oral dose of radiolabeled PF-07081532.
- Cmax of total radioactivity in plasma [Period 1: Pre-dose, 0.5, 1, 2, 4, 6, 8, 12, 15, 24, 36, 48, 72, 96, 120, 144-480 hours post-dose]
Maximum plasma concentration of total radioactivity following administration of a single oral dose of radiolabeled PF-07081532.
- Tmax of total radioactivity in plasma [Period 1: Pre-dose, 0.5, 1, 2, 4, 6, 8, 12, 15, 24, 36, 48, 72, 96, 120, 144-480 hours post-dose]
Time to Cmax of total radioactivity following administration of a single oral dose of radiolabeled PF-07081532.
- AUCinf of total radioactivity in plasma (if data permit) [Period 1: Pre-dose, 0.5, 1, 2, 4, 6, 8, 12, 15, 24, 36, 48, 72, 96, 120, 144-480 hours post-dose]
Area under the plasma total radioactivity concentration-time profile from time zero extrapolated to infinite time following administration of a single oral dose of radiolabeled PF-07081532.
- t1/2 of total radioactivity in plasma (if data permit) [Period 1: Pre-dose, 0.5, 1, 2, 4, 6, 8, 12, 15, 24, 36, 48, 72, 96, 120, 144-480 hours post-dose]
Terminal elimination half-life following administration of a single oral dose of radiolabeled PF-07081532.
- CL/F of oral radiolabeled PF-07081532 in plasma (if data permit) [Period 1: Pre-dose, 0.5, 1, 2, 4, 6, 8, 12, 15, 24, 36, 48, 72, 96, 120, 144 hours post-dose]
Apparent clearance following administration of a single oral dose of radiolabeled PF-07081532.
- Vz/F of oral radiolabeled PF-07081532 in plasma (if data permit) [Period 1: Pre-dose, 0.5, 1, 2, 4, 6, 8, 12, 15, 24, 36, 48, 72, 96, 120, 144 hours post-dose]
Apparent volume of distribution following administration of a single oral dose of radiolabeled PF-07081532.
- AUClast of intravenous radiolabeled PF-07081532 in plasma [Period 2: Pre-dose, 0.17, 0.25, 0.33, 0.5, 1, 3, 5, 7, 9, 11, 14, 23, 35, 47, 71, 95, 119, 143 hours post-dose]
Area under the plasma concentration-time profile from time zero to time of the last quantifiable concentration (Clast) of radiolabeled PF-07081532 following administration of a single intravenous dose of radiolabeled PF-07081532.
- Dose normalized AUClast of intravenous radiolabeled PF-07081532 in plasma [Period 2: Pre-dose, 0.17, 0.25, 0.33, 0.5, 1, 3, 5, 7, 9, 11, 14, 23, 35, 47, 71, 95, 119, 143 hours post-dose]
Dose normalized area under the plasma concentration-time profile from time zero to time of the last quantifiable concentration (Clast) of radiolabeled PF-07081532 following administration of a single intravenous dose of radiolabeled PF-07081532.
- Cmax of intravenous radiolabeled PF-07081532 in plasma [Period 2: Pre-dose, 0.17, 0.25, 0.33, 0.5, 1, 3, 5, 7, 9, 11, 14, 23, 35, 47, 71, 95, 119, 143 hours post-dose]
Maximum plasma concentration of radiolabeled PF-07081532 following administration of a single intravenous dose of radiolabeled PF-07081532.
- Dose normalized Cmax of intravenous radiolabeled PF-07081532 in plasma [Period 2: Pre-dose, 0.17, 0.25, 0.33, 0.5, 1, 3, 5, 7, 9, 11, 14, 23, 35, 47, 71, 95, 119, 143 hours post-dose]
Dose normalized maximum plasma concentration of radiolabeled PF-07081532 following administration of a single intravenous dose of radiolabeled PF-07081532.
- Tmax of intravenous radiolabeled PF-07081532 in plasma [Period 2: Pre-dose, 0.17, 0.25, 0.33, 0.5, 1, 3, 5, 7, 9, 11, 14, 23, 35, 47, 71, 95, 119, 143 hours post-dose]
Time to Cmax of radiolabeled PF-07081532 following administration of a single intravenous dose of radiolabeled PF-07081532.
- AUCinf of intravenous radiolabeled PF-07081532 in plasma (if data permit) [Period 2: Pre-dose, 0.17, 0.25, 0.33, 0.5, 1, 3, 5, 7, 9, 11, 14, 23, 35, 47, 71, 95, 119, 143 hours post-dose]
Area under the plasma concentration-time profile from time zero extrapolated to infinite time following administration of a single intravenous dose of radiolabeled PF-07081532.
- Dose normalized AUCinf of intravenous radiolabeled PF-07081532 in plasma (if data permit) [Period 2: Pre-dose, 0.17, 0.25, 0.33, 0.5, 1, 3, 5, 7, 9, 11, 14, 23, 35, 47, 71, 95, 119, 143 hours post-dose]
Dose normalized area under the plasma concentration-time profile from time zero extrapolated to infinite time following administration of a single intravenous dose of radiolabeled PF-07081532.
- t1/2 of intravenous radiolabeled PF-07081532 in plasma (if data permit) [Period 2: Pre-dose, 0.17, 0.25, 0.33, 0.5, 1, 3, 5, 7, 9, 11, 14, 23, 35, 47, 71, 95, 119, 143 hours post-dose]
Terminal elimination half-life following administration of a single intravenous dose of radiolabeled PF-07081532.
- CL of intravenous radiolabeled PF-07081532 in plasma (if data permit) [Period 2: Pre-dose, 0.17, 0.25, 0.33, 0.5, 1, 3, 5, 7, 9, 11, 14, 23, 35, 47, 71, 95, 119, 143 hours post-dose]
Systemic clearance following administration of a single intravenous dose of radiolabeled PF-07081532.
- Vss of intravenous radiolabeled PF-07081532 in plasma (if data permit) [Period 2: Pre-dose, 0.17, 0.25, 0.33, 0.5, 1, 3, 5, 7, 9, 11, 14, 23, 35, 47, 71, 95, 119, 143 hours post-dose]
Steady-state volume of distribution following administration of a single intravenous dose of radiolabeled PF-07081532.
- Mean residence Time (MRT) of intravenous radiolabeled PF-07081532 in plasma (if data permit) [Period 2: Pre-dose, 0.17, 0.25, 0.33, 0.5, 1, 3, 5, 7, 9, 11, 14, 23, 35, 47, 71, 95, 119, 143 hours post-dose]
- Absolute oral bioavailability (F) of PF-07081532 [Period 2: Pre-dose up to 144 hours post-dose]
Dose-normalized plasma AUCinf (if data permit, otherwise AUClast) following oral unlabeled PF-07081532 compared to IV microtracer PF-07081532 in Period 2.
- Fraction of the dose absorbed (Fa) for oral PF-07081532 [Period 2: Pre-dose up to 144 hours post-dose]
Total urinary radioactivity following oral administration of radiolabeled PF-07081532 in Period 1 and IV microtracer administration of PF-07081532 in Period 2.
- Number of participants with treatment emergent clinically significant laboratory abnormalities [Baseline, day 7-21 of period 1, baseline, day 7 of period 2]
- Number of participants with treatment emergent clinically significant abnormal ECG measurements [Pre-dose, day 7-21 of period 1, Pre-dose, day 7 of period 2]
- Number of participants with treatment emergent clinically significant abnormal vital measurements [Pre-dose, day 7-21 of period 1, Pre-dose, day 7 of period 2]
- Number of participants with adverse events [Pre-dose, day 7-21 of period 1, Pre-dose, day 7 of period 2]
Eligibility Criteria
Criteria
Key Eligibility criteria for this study include, but are not limited to the following:
Inclusion criteria:
Healthy Male participants must be 18 to 60 years of age, inclusive.
Overtly healthy as determined by medical evaluation including medical history, physical examination, blood pressure and pulse rate measurement, standard 12-lead ECG, and laboratory tests.
BMI of 17.5 to 30.5 kg/m2; and a total body weight >50 kg (110 lb).
Participants who are willing and able to comply with all scheduled visits, treatment plan, laboratory tests, lifestyle considerations, and other study procedures
Exclusion criteria:
History of irregular bowel movements (eg, irritable bowel syndrome, frequent episodes of diarrhea, or constipation defined by less than 1 bowel movement on average per 2 days) or lactose intolerance
Any condition possibly affecting drug absorption (eg, gastrectomy, cholecystectomy).
Previous administration with an investigational product (drug or vaccine) within 90 days (or as determined by the local requirement) preceding the first dose of study intervention used in this study.
Total 14C radioactivity measured in plasma exceeding 11 mBq/mL.
Contacts and Locations
Locations
| Site | City | State | Country | Postal Code | |
|---|---|---|---|---|---|
| 1 | PRA Health Sciences | Groningen | Netherlands | 9728 NZ |
Sponsors and Collaborators
- Pfizer
Investigators
- Study Director: Pfizer CT.gov Call Center, Pfizer
Study Documents (Full-Text)
None provided.More Information
Additional Information:
Publications
None provided.- C3991006