Phase 1
N=6
A Study in Healthy Adult Male Participants to Assess Absorption, Distribution, Metabolism and Excretion (ADME) of Radiolabeled PF-06865571.
Healthy Participants
Bottom Line
View on ClinicalTrials.gov: NCT04866225 ↗Enrolled (actual)
6
Serious AEs
0.0%
Results posted
Jul 2024
Primary outcome: Primary: Total Recovery of Radioactivity in Urine as Percentage of Total Radioactive Dose of PF-06865571 Administered — 48.9; 51.5 Percentage of Dose
Study Design & Population
- Study type
- Interventional
- Phase
- Phase 1
- Interventions
- Oral [14C]PF-06865571 (Drug); Oral PF-06865571 (Drug); IV [14C]PF-06865571 (Drug)
- Age
- Adult · 18+ yrs
- Sex
- Male
- Sponsor
- Pfizer
- Primary completion
- Jul 2021
Outcome Measures
| Outcome | Result | p-value |
|---|---|---|
| PRIMARY Total Recovery of Radioactivity in Urine as Percentage of Total Radioactive Dose of PF-06865571 Administered |
48.9; 51.5 | — |
| PRIMARY Total Recovery of Radioactivity in Feces as Percentage of Total Radioactive Dose of PF-06865571 Administered |
30.1; 18.8 | — |
| PRIMARY Total Recovery of Radioactivity in Total Excreta (Urine + Feces) as Percentage of Total Radioactive Dose of PF-06865571 Administered |
79.0; 70.3 | — |
| PRIMARY Relative Abundance (Mean Value) of Radiolabeled PF-06865571 in Plasma in Period 1 |
43.8 | — |
| PRIMARY Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Plasma in Period 1 |
0; 3.0; 0; 2.7; 11.3; 0.01 | — |
| PRIMARY Relative Abundance (Mean Value) of Radiolabeled PF-06865571 in Urine in Period 1 |
2.7 | — |
| PRIMARY Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Urine in Period 1 |
2.0; 6.0; 0; 4.7; 23.3; 23.3 | — |
| PRIMARY Relative Abundance (Mean Value) of Radiolabeled PF-06865571 in Feces in Period 1 |
4.1 | — |
| PRIMARY Relative Abundance (Mean Value) of Metabolites of Radiolabeled PF-06865571 in Feces in Period 1 |
0; 0; 1.1; 0; 0; 21.0 | — |
| SECONDARY Area Under the Plasma Concentration-time Profile From Time Zero to Time of The Last Quantifiable Concentration (AUClast) of Total Radioactivity of [14C]PF-06865571 in Plasma in Period 1 |
20080 | — |
| SECONDARY Maximum Plasma Concentration (Cmax) of Total Radioactivity of [14C]PF-06865571 in Plasma in Period 1 |
4417 | — |
| SECONDARY Time for Cmax (Tmax) of Total Radioactivity of [14C]PF-06865571 in Plasma in Period 1 |
3.00 | — |
| SECONDARY Area Under the Plasma Concentration Time Profile From Time Zero Extrapolated to Infinite Time (AUCinf) of Total Radioactivity of [14C]PF-06865571 in Plasma in Period 1 |
20400 | — |
| SECONDARY Terminal Elimination Half-life (t1/2) of Total Radioactivity of [14C]PF-06865571 in Plasma in Period 1 |
3.622 | — |
| SECONDARY AUClast of Oral PF-06865571 in Plasma in Period 1 |
7962 | — |
| SECONDARY Cmax of Oral PF-06865571 in Plasma in Period 1 |
2096 | — |
| SECONDARY Tmax of Oral PF-06865571 in Plasma in Period 1 |
3.00 | — |
| SECONDARY AUCinf of Oral PF-06865571 in Plasma in Period 1 |
7964 | — |
| SECONDARY t1/2 of Oral PF-06865571 in Plasma in Period 1 |
6.275 | — |
| SECONDARY AUClast of Intravenous (IV) Radiolabeled PF-06865571 in Plasma in Period 2 |
4.145 | — |
| SECONDARY Cmax of IV Radiolabeled PF-06865571 in Plasma in Period 2 |
2.893 | — |
| SECONDARY Tmax of IV Radiolabeled PF-06865571 in Plasma in Period 2 |
0.250 | — |
| SECONDARY t1/2 of IV Radiolabeled PF-06865571 in Plasma in Period 2 |
1.232 | — |
| SECONDARY AUCinf of IV Radiolabeled PF-06865571 in Plasma in Period 2 |
4.209 | — |
| SECONDARY Systemic Clearance (CL) of IV Radiolabeled PF-06865571 in Plasma in Period 2 |
23.88 | — |
| SECONDARY Steady State Volume of Distribution (Vss) of IV Radiolabeled PF-06865571 in Plasma in Period 2 |
38.83 | — |
| SECONDARY Dose-Normalized AUCinf (AUCinf[dn]) of Oral Unlabeled PF-06865571 in Plasma in Period 2 |
31.46 | — |
| SECONDARY AUCinf(dn) of IV Microtracer of Radiolabeled PF-06865571 in Plasma in Period 2 |
41.92 | — |
| SECONDARY Absolute Oral Bioavailability (F) of Oral Unlabeled and IV Radiolabeled PF-06865571 for Plasma AUCinf(dn) in Period 2 |
75.06 | — |
| SECONDARY Percentage of Total 14C in Urine Following Oral Administration (%14C_Urine_PO) of Radiolabeled PF-06865571 in Period 1 |
45.92 | — |
| SECONDARY Percentage of Total 14C in Urine Following IV Microtracer Administration (%14C_Urine_IV) of Radiolabeled PF-06865571 in Period 2 |
49.50 | — |
| SECONDARY Fraction Absorbed (Fa) for Percentage of Excretion of Total 14C in Urine for Oral and IV Radiolabeled PF-06865571 |
92.78 | — |
Summary
This study is a Phase 1, open-label, non-randomized, 2-period, fixed-sequence, single-dose study of PF-06865571 in healthy male participants to characterize the ADME properties of [14C]PF-06865571 following oral administration; and to evaluate the absolute oral bioavailability (F) and fraction absorbed (Fa) of PF-06865571 following oral administration of unlabeled PF-06865571 and IV administration of [14C]PF-06865571.
Eligibility Criteria
Inclusion Criteria
- Male participants, 18 to 60 years of age, inclusive, at the time of signing the informed consent document.
- Male participants who are overtly healthy as determined by medical evaluation including medical history, physical examination, laboratory tests, and cardiac tests.
- Participants who are nonsmoking for at least 3 months at the time of signing the informed consent document.
- BMI of 17.5 to 30.4 kg/m2, inclusive; and a total body weight >50 kg (110 lb).
Exclusion Criteria
- Any condition possibly affecting drug absorption (eg, gastrectomy, cholecystectomy).
- History of irregular bowel movements including irritable bowel syndrome or frequent episodes of diarrhea or constipation, defined by less than 1 bowel movement on average per 2 days, or lactose intolerance.
- History of HIV infection, hepatitis B, or hepatitis C; positive testing for HIV, HBsAg,or HCVAb. Hepatitis B vaccination is allowed.
- History of SARS-CoV-2 PCR or antibody (eg, IgG, IgM, etc) positive result would necessitate accompanying history of asymptomatic state for at least 6 months prior to screening.
- Use of prescription or nonprescription drugs.
- Previous administration with an unapproved drug within 60 days preceding the first dose of study intervention used in this study.
- A positive urine drug test.
- A positive urine cotinine test.
- A positive COVID-19 (SARS-CoV-2) PCR test.
- Blood donation (excluding plasma donations) of approximately 1 pint (500 mL) or more within 60 days prior to dosing.
Data sourced from ClinicalTrials.gov (NCT04866225). Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication.