Trial Outcomes & Findings for A Study to Understand How the Study Medicine (PF-07081532) is Processed and Eliminated in Healthy Men (NCT NCT05652647)
NCT ID: NCT05652647
Last Updated: 2024-09-24
Results Overview
Urine and feces samples collected after a single oral dose of \[14C\]PF-07081532 30 mg (\~250 nCi) in Period 1 were analyzed using Accelerator Mass Spectrometry (AMS). "Blank" pre-dose urine samples were collected within the 24 hours prior to dosing, "blank" fecal samples were collected from at least 1 bowel movement within the 48 hours prior to dosing. Following oral dosing, each urine void was collected across intervals of 0-12 hours, 12-24 hours, and each subsequent 24 hour interval up to 360 hours post dose, and all feces excreted were collected across each 24 hour interval up to 360 hours post dose. Recovery of radioactivity in urine, feces, and both routes combined, determined as percentage of the orally administered radioactive dose, are reported.
COMPLETED
PHASE1
6 participants
360 hours
2024-09-24
Participant Flow
A total of 6 participants were enrolled and treated in both Period 1 and Period 2 of the study.
Participant milestones
| Measure |
Period 1: [14C]PF-07081532 30 mg Oral; Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV
In Period 1, participants received a single oral dose of \[14C\]PF-07081532 30 mg; in Period 2, participants received an oral dose of unlabeled PF-07081532 30 mg, followed by intravenous (IV) infusion of \[14C\]PF-07081532 100 µg.
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|---|---|
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Overall Study
STARTED
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6
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Overall Study
COMPLETED
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6
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Overall Study
NOT COMPLETED
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0
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Reasons for withdrawal
Withdrawal data not reported
Baseline Characteristics
A Study to Understand How the Study Medicine (PF-07081532) is Processed and Eliminated in Healthy Men
Baseline characteristics by cohort
| Measure |
Period 1: [14C]PF-07081532 30 mg Oral; Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV
n=6 Participants
In Period 1, participants received a single oral dose of \[14C\]PF-07081532 30 mg; in Period 2, participants received an oral dose of unlabeled PF-07081532 30 mg, followed by IV infusion of \[14C\]PF-07081532 100 µg.
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Age, Customized
<18 years
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0 Participants
n=5 Participants
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Age, Customized
18-25 years
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0 Participants
n=5 Participants
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Age, Customized
26-35 years
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5 Participants
n=5 Participants
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Age, Customized
36-45 years
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0 Participants
n=5 Participants
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Age, Customized
>45 years
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1 Participants
n=5 Participants
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Age, Customized
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32 Years
n=5 Participants
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Sex: Female, Male
Female
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0 Participants
n=5 Participants
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Sex: Female, Male
Male
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6 Participants
n=5 Participants
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Ethnicity (NIH/OMB)
Hispanic or Latino
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1 Participants
n=5 Participants
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Ethnicity (NIH/OMB)
Not Hispanic or Latino
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5 Participants
n=5 Participants
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Ethnicity (NIH/OMB)
Unknown or Not Reported
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0 Participants
n=5 Participants
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Race/Ethnicity, Customized
White
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5 Participants
n=5 Participants
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Race/Ethnicity, Customized
Black or African American
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1 Participants
n=5 Participants
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PRIMARY outcome
Timeframe: 360 hoursPopulation: The analysis population included all evaluable participants who had received 1 dose of \[14C\]PF-07081532 in Period 1 with complete total radioactivity concentration (urinary and fecal) data and who had no protocol deviations that might have affected the extent of excretion analysis.
Urine and feces samples collected after a single oral dose of \[14C\]PF-07081532 30 mg (\~250 nCi) in Period 1 were analyzed using Accelerator Mass Spectrometry (AMS). "Blank" pre-dose urine samples were collected within the 24 hours prior to dosing, "blank" fecal samples were collected from at least 1 bowel movement within the 48 hours prior to dosing. Following oral dosing, each urine void was collected across intervals of 0-12 hours, 12-24 hours, and each subsequent 24 hour interval up to 360 hours post dose, and all feces excreted were collected across each 24 hour interval up to 360 hours post dose. Recovery of radioactivity in urine, feces, and both routes combined, determined as percentage of the orally administered radioactive dose, are reported.
Outcome measures
| Measure |
Period 1: [14C]PF-07081532 30 mg Oral
n=6 Participants
In Period 1, participants received a single oral dose of \[14C\]PF-07081532 30 mg.
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Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV
In Period 2, participants received an oral dose of unlabeled PF-07081532 30 mg, followed by IV infusion of \[14C\]PF-07081532 100 µg.
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Total Recovery of Radioactivity in Urine, Feces and Both Routes Combined, as Percentage of Orally Administered Radioactive Dose of [14C]PF-07081532
Urine
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4.7 Percentage of radioactive dose
Standard Deviation 0.6
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—
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Total Recovery of Radioactivity in Urine, Feces and Both Routes Combined, as Percentage of Orally Administered Radioactive Dose of [14C]PF-07081532
Feces
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78.6 Percentage of radioactive dose
Standard Deviation 6.7
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—
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Total Recovery of Radioactivity in Urine, Feces and Both Routes Combined, as Percentage of Orally Administered Radioactive Dose of [14C]PF-07081532
Urine + Feces
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83.4 Percentage of radioactive dose
Standard Deviation 6.9
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—
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PRIMARY outcome
Timeframe: Pre-dose (0 hours [hrs]) and 0.5 hrs, 1 hr, 2 hrs, 4 hrs, 6 hrs, 8 hrs, 10 hrs, 12 hrs, 24 hrs, 36 hrs, 48 hrs, and 72 hrs post Period 1 Day 1 dosingPopulation: The analysis population included all participants who received study intervention of \[14C\]PF-07081532 in Period 1.
Plasma samples collected after a single oral dose of \[14C\]PF-07081532 30 mg (\~250 nCi) were analyzed using Ultra Performance Liquid Chromatography coupled to High Resolution Mass Spectrometry (UPLC-HRMS). Relative abundance = (sum of radioactive content of fractions contributing to a particular peak/total circulating drug-related material \[total \[14C\] radioactivity in plasma\]) x 100%. Metabolites that were detected and identifiable (including coeluting metabolites reported together) are reported in this outcome measure (OM).
Outcome measures
| Measure |
Period 1: [14C]PF-07081532 30 mg Oral
n=6 Participants
In Period 1, participants received a single oral dose of \[14C\]PF-07081532 30 mg.
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Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV
In Period 2, participants received an oral dose of unlabeled PF-07081532 30 mg, followed by IV infusion of \[14C\]PF-07081532 100 µg.
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Relative Abundance of [14C]PF-07081532 and Its Metabolites in Plasma After A Single Oral Dose of [14]PF-07081532 in Period 1
Unassigned [14C]
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0.6 Percentage of circulating radioactivity
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—
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Relative Abundance of [14C]PF-07081532 and Its Metabolites in Plasma After A Single Oral Dose of [14]PF-07081532 in Period 1
767a (hydroxy glucuronide)
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1.2 Percentage of circulating radioactivity
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—
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Relative Abundance of [14C]PF-07081532 and Its Metabolites in Plasma After A Single Oral Dose of [14]PF-07081532 in Period 1
PF-07943285 (hydroxy glucuronide)
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8.8 Percentage of circulating radioactivity
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—
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Relative Abundance of [14C]PF-07081532 and Its Metabolites in Plasma After A Single Oral Dose of [14]PF-07081532 in Period 1
767c (hydroxy glucuronide)
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0.4 Percentage of circulating radioactivity
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—
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Relative Abundance of [14C]PF-07081532 and Its Metabolites in Plasma After A Single Oral Dose of [14]PF-07081532 in Period 1
671 (hydroxy sulfate)
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0.6 Percentage of circulating radioactivity
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—
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Relative Abundance of [14C]PF-07081532 and Its Metabolites in Plasma After A Single Oral Dose of [14]PF-07081532 in Period 1
Coeluting components: PF-07214855, PF-07260051, PF-07943284
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9.1 Percentage of circulating radioactivity
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—
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Relative Abundance of [14C]PF-07081532 and Its Metabolites in Plasma After A Single Oral Dose of [14]PF-07081532 in Period 1
PF-07081532
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79.3 Percentage of circulating radioactivity
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—
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PRIMARY outcome
Timeframe: 96 hours for urine samples and 144 hours for feces samplesPopulation: The analysis population included all participants who received study intervention of \[14C\]PF-07081532 in Period 1.
Urine and feces samples collected after a single oral dose of \[14C\]PF-07081532 30 mg (\~250 nCi) were analyzed using UPLC-HRMS. "Blank" pre-dose urine samples were collected within the 24 hours prior to dosing, "blank" fecal samples were collected from at least 1 bowel movement within the 48 hours prior to dosing. To obtain samples for evaluation of relative abundance in urine and feces, following oral dosing, each urine void was collected across intervals of 0-12 hours, 12-24 hours, and each subsequent 24 hour interval up to 96 hours post dose, and all feces excreted were collected across each 24 hour interval up to 144 hours post dose. Relative abundance was determined as sum of radioactive content of fractions contributing to a particular peak divided by total radioactive dose excreted in urine/feces respectively. Metabolites that were detected and identifiable (including coeluting metabolites reported together) are reported in this OM.
Outcome measures
| Measure |
Period 1: [14C]PF-07081532 30 mg Oral
n=6 Participants
In Period 1, participants received a single oral dose of \[14C\]PF-07081532 30 mg.
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Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV
In Period 2, participants received an oral dose of unlabeled PF-07081532 30 mg, followed by IV infusion of \[14C\]PF-07081532 100 µg.
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Relative Abundance of [14C]PF-07081532 and Its Metabolites in Urine and Feces After A Single Oral Dose of [14]PF-07081532 in Period 1
Urine: PF-07943285 (hydroxy glucuronide)
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0.1 Percentage of radioactive dose
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—
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Relative Abundance of [14C]PF-07081532 and Its Metabolites in Urine and Feces After A Single Oral Dose of [14]PF-07081532 in Period 1
Urine: 767c (hydroxy glucuronide)
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0.03 Percentage of radioactive dose
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—
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Relative Abundance of [14C]PF-07081532 and Its Metabolites in Urine and Feces After A Single Oral Dose of [14]PF-07081532 in Period 1
Urine: coeluting components PF-07214855 , PF-07260051 and PF-07943284
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0.2 Percentage of radioactive dose
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—
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Relative Abundance of [14C]PF-07081532 and Its Metabolites in Urine and Feces After A Single Oral Dose of [14]PF-07081532 in Period 1
Urine: PF-07081532
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0.04 Percentage of radioactive dose
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—
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Relative Abundance of [14C]PF-07081532 and Its Metabolites in Urine and Feces After A Single Oral Dose of [14]PF-07081532 in Period 1
Urine: Unassigned [14C]
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4.33 Percentage of radioactive dose
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—
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Relative Abundance of [14C]PF-07081532 and Its Metabolites in Urine and Feces After A Single Oral Dose of [14]PF-07081532 in Period 1
Feces: PF-07240437 (catechol)
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3.89 Percentage of radioactive dose
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—
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Relative Abundance of [14C]PF-07081532 and Its Metabolites in Urine and Feces After A Single Oral Dose of [14]PF-07081532 in Period 1
Feces: PF-07943283 (hydroxy)
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13.6 Percentage of radioactive dose
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—
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Relative Abundance of [14C]PF-07081532 and Its Metabolites in Urine and Feces After A Single Oral Dose of [14]PF-07081532 in Period 1
Feces: coeluting components PF-07260051 and PF-07943284
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24.7 Percentage of radioactive dose
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—
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Relative Abundance of [14C]PF-07081532 and Its Metabolites in Urine and Feces After A Single Oral Dose of [14]PF-07081532 in Period 1
Feces: PF-07081532
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13.2 Percentage of radioactive dose
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—
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Relative Abundance of [14C]PF-07081532 and Its Metabolites in Urine and Feces After A Single Oral Dose of [14]PF-07081532 in Period 1
Feces: Unassigned [14C]
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23.2 Percentage of radioactive dose
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—
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SECONDARY outcome
Timeframe: Pre-dose (0 hrs) and 0.5 hrs, 1 hr, 2 hrs, 4 hrs, 6 hrs, 8 hrs, 10 hrs, 12 hrs, 15 hrs, 24 hrs, 36 hrs, 48 hrs, 72 hrs, 96 hrs, 120 hrs and 144 hrs post Period 1 Day 1 dosingPopulation: The analysis population included all participants dosed with \[14C\]PF-07081532 in Period 1 who had at least one of the PF-07081532 or total \[14C\] PK parameters of interest.
Area under the plasma concentration versus time curve from time zero to the time of the last quantifiable concentration of total \[14C\] after the participant received a single oral dose of \[14C\]PF-07081532 30 mg (approximately 250 nCi \[14C\]) in Period 1. AUC for total \[14C\] is presented as nanogram equivalent \* hour/milliliter (ngEq\*hr/mL).
Outcome measures
| Measure |
Period 1: [14C]PF-07081532 30 mg Oral
n=6 Participants
In Period 1, participants received a single oral dose of \[14C\]PF-07081532 30 mg.
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Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV
In Period 2, participants received an oral dose of unlabeled PF-07081532 30 mg, followed by IV infusion of \[14C\]PF-07081532 100 µg.
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Area Under the Plasma Concentration-Time Profile From Time Zero to the Time of the Last Quantifiable Concentration (AUClast) of Total [14C] After A Single Oral Dose of [14C]PF-07081532 in Period 1
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74360 ngEq*hr/mL
Geometric Coefficient of Variation 17
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—
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SECONDARY outcome
Timeframe: Pre-dose (0 hrs) and 0.5 hrs, 1 hr, 2 hrs, 4 hrs, 6 hrs, 8 hrs, 10 hrs, 12 hrs, 15 hrs, 24 hrs, 36 hrs, 48 hrs, 72 hrs, 96 hrs, 120 hrs and 144 hrs post Period 1 Day 1 dosingPopulation: The analysis population included all participants dosed with \[14C\]PF-07081532 in Period 1 who had at least one of the PF-07081532 or total \[14C\] PK parameters of interest.
Area under the plasma concentration versus time curve from time zero to the time of the last quantifiable concentration of PF-07081532 after the participant received a single oral dose of \[14C\]PF-07081532 30 mg (approximately 250 nCi \[14C\]) in Period 1.
Outcome measures
| Measure |
Period 1: [14C]PF-07081532 30 mg Oral
n=6 Participants
In Period 1, participants received a single oral dose of \[14C\]PF-07081532 30 mg.
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Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV
In Period 2, participants received an oral dose of unlabeled PF-07081532 30 mg, followed by IV infusion of \[14C\]PF-07081532 100 µg.
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AUClast of PF-07081532 After A Single Oral Dose of [14]PF-07081532 in Period 1
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49380 nanogram*hr/milliliter (ng*hr/mL)
Geometric Coefficient of Variation 21
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—
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SECONDARY outcome
Timeframe: Pre-dose (0 hrs) and 0.5 hrs, 1 hr, 2 hrs, 4 hrs, 6 hrs, 8 hrs, 10 hrs, 12 hrs, 15 hrs, 24 hrs, 36 hrs, 48 hrs, 72 hrs, 96 hrs, 120 hrs and 144 hrs post Period 1 Day 1 dosingPopulation: The analysis population included all participants dosed with \[14C\]PF-07081532 in Period 1 who had at least one of the PF-07081532 or total \[14C\] PK parameters of interest.
Maximum plasma concentration of total \[14C\] after the participant received a single oral dose of \[14C\]PF-07081532 30 mg (approximately 250 nCi \[14C\]) in Period 1.
Outcome measures
| Measure |
Period 1: [14C]PF-07081532 30 mg Oral
n=6 Participants
In Period 1, participants received a single oral dose of \[14C\]PF-07081532 30 mg.
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Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV
In Period 2, participants received an oral dose of unlabeled PF-07081532 30 mg, followed by IV infusion of \[14C\]PF-07081532 100 µg.
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Plasma Maximum Observed Concentration (Cmax) of Total [14C] After A Single Oral Dose of [14C]PF-07081532 in Period 1
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2934 nanogram equivalent/milliliter (ngEq/mL)
Geometric Coefficient of Variation 10
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—
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SECONDARY outcome
Timeframe: Pre-dose (0 hrs) and 0.5 hrs, 1 hr, 2 hrs, 4 hrs, 6 hrs, 8 hrs, 10 hrs, 12 hrs, 15 hrs, 24 hrs, 36 hrs, 48 hrs, 72 hrs, 96 hrs, 120 hrs and 144 hrs post Period 1 Day 1 dosingPopulation: The analysis population included all participants dosed with \[14C\]PF-07081532 in Period 1 who had at least one of the PF-07081532 or total \[14C\] PK parameters of interest.
Maximum plasma concentration of PF-07081532 after the participant received a single oral dose of \[14C\]PF-07081532 30 mg (approximately 250 nCi \[14C\]) in Period 1.
Outcome measures
| Measure |
Period 1: [14C]PF-07081532 30 mg Oral
n=6 Participants
In Period 1, participants received a single oral dose of \[14C\]PF-07081532 30 mg.
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Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV
In Period 2, participants received an oral dose of unlabeled PF-07081532 30 mg, followed by IV infusion of \[14C\]PF-07081532 100 µg.
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|---|---|---|
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Plasma Cmax of PF-07081532 After A Single Oral Dose of [14C]PF-07081532 in Period 1
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2874 nanogram/milliliter (ng/mL)
Geometric Coefficient of Variation 10
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—
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SECONDARY outcome
Timeframe: Pre-dose (0 hrs) and 0.5 hrs, 1 hr, 2 hrs, 4 hrs, 6 hrs, 8 hrs, 10 hrs, 12 hrs, 15 hrs, 24 hrs, 36 hrs, 48 hrs, 72 hrs, 96 hrs, 120 hrs and 144 hrs post Period 1 Day 1 dosingPopulation: The analysis population included all participants dosed with \[14C\]PF-07081532 in Period 1 who had at least one of the PF-07081532 or total \[14C\] PK parameters of interest.
Time to reach maximum plasma concentration of total \[14C\] and PF-07081532 after the participant received a single oral dose of \[14C\]PF-07081532 30 mg (approximately 250 nCi \[14C\]) in Period 1.
Outcome measures
| Measure |
Period 1: [14C]PF-07081532 30 mg Oral
n=6 Participants
In Period 1, participants received a single oral dose of \[14C\]PF-07081532 30 mg.
|
Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV
In Period 2, participants received an oral dose of unlabeled PF-07081532 30 mg, followed by IV infusion of \[14C\]PF-07081532 100 µg.
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Plasma Time to Reach Cmax (Tmax) of Total [14C] and PF-07081532 After A Single Oral Dose of [14C]PF-07081532 in Period 1
Total [14C]
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4.93 hour
Interval 2.0 to 6.0
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—
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Plasma Time to Reach Cmax (Tmax) of Total [14C] and PF-07081532 After A Single Oral Dose of [14C]PF-07081532 in Period 1
PF-07081532
|
3.93 hour
Interval 2.0 to 6.0
|
—
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SECONDARY outcome
Timeframe: Pre-dose (0 hrs) and 0.5 hrs, 1 hr, 2 hrs, 4 hrs, 6 hrs, 8 hrs, 10 hrs, 12 hrs, 15 hrs, 24 hrs, 36 hrs, 48 hrs, 72 hrs, 96 hrs, 120 hrs and 144 hrs post Period 1 Day 1 dosingPopulation: The analysis population included all participants dosed with \[14C\]PF-07081532 in Period 1 who had at least one of the PF-07081532 or total \[14C\] PK parameters of interest.
Area under the plasma concentration versus time curve from time zero to infinity of total \[14C\] after the participant received a single oral dose of \[14C\]PF-07081532 30 mg (approximately 250 nCi \[14C\]) in Period 1.
Outcome measures
| Measure |
Period 1: [14C]PF-07081532 30 mg Oral
n=6 Participants
In Period 1, participants received a single oral dose of \[14C\]PF-07081532 30 mg.
|
Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV
In Period 2, participants received an oral dose of unlabeled PF-07081532 30 mg, followed by IV infusion of \[14C\]PF-07081532 100 µg.
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|---|---|---|
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Area Under the Plasma Concentration-Time Curve to Infinity (AUCinf) of Total [14C] After A Single Oral Dose of [14C]PF-07081532 in Period 1
|
76050 ngEq*hr/mL
Geometric Coefficient of Variation 17
|
—
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SECONDARY outcome
Timeframe: Pre-dose (0 hrs) and 0.5 hrs, 1 hr, 2 hrs, 4 hrs, 6 hrs, 8 hrs, 10 hrs, 12 hrs, 15 hrs, 24 hrs, 36 hrs, 48 hrs, 72 hrs, 96 hrs, 120 hrs and 144 hrs post Period 1 Day 1 dosingPopulation: The analysis population included all participants dosed with \[14C\]PF-07081532 in Period 1 who had at least one of the PF-07081532 or total \[14C\] PK parameters of interest.
Area under the plasma concentration versus time curve from time zero to infinity of PF-07081532 after the participant received a single oral dose of \[14C\]PF-07081532 30 mg (approximately 250 nCi \[14C\]) in Period 1.
Outcome measures
| Measure |
Period 1: [14C]PF-07081532 30 mg Oral
n=6 Participants
In Period 1, participants received a single oral dose of \[14C\]PF-07081532 30 mg.
|
Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV
In Period 2, participants received an oral dose of unlabeled PF-07081532 30 mg, followed by IV infusion of \[14C\]PF-07081532 100 µg.
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|---|---|---|
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AUCinf of PF-07081532 After A Single Oral Dose of [14C]PF-07081532 in Period 1
|
51370 ng*hr/mL
Geometric Coefficient of Variation 21
|
—
|
SECONDARY outcome
Timeframe: Pre-dose (0 hrs) and 0.5 hrs, 1 hr, 2 hrs, 4 hrs, 6 hrs, 8 hrs, 10 hrs, 12 hrs, 15 hrs, 24 hrs, 36 hrs, 48 hrs, 72 hrs, 96 hrs, 120 hrs and 144 hrs post Period 1 Day 1 dosingPopulation: The analysis population included all participants dosed with \[14C\]PF-07081532 in Period 1 who had at least one of the PF-07081532 or total \[14C\] PK parameters of interest.
Plasma elimination half-life of total \[14C\] and PF-07081532 after the participant received a single oral dose of \[14C\]PF-07081532 30 mg (approximately 250 nCi \[14C\]) in Period 1.
Outcome measures
| Measure |
Period 1: [14C]PF-07081532 30 mg Oral
n=6 Participants
In Period 1, participants received a single oral dose of \[14C\]PF-07081532 30 mg.
|
Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV
In Period 2, participants received an oral dose of unlabeled PF-07081532 30 mg, followed by IV infusion of \[14C\]PF-07081532 100 µg.
|
|---|---|---|
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Plasma Elimination Half Life (t1/2) of Total [14C] and PF-07081532 After A Single Oral Dose of [14C]PF-07081532 in Period 1
Total [14C]
|
65.20 hour
Standard Deviation 6.7308
|
—
|
|
Plasma Elimination Half Life (t1/2) of Total [14C] and PF-07081532 After A Single Oral Dose of [14C]PF-07081532 in Period 1
PF-07081532
|
19.42 hour
Standard Deviation 3.5583
|
—
|
SECONDARY outcome
Timeframe: Pre-dose (0 hrs) and 0.5 hrs, 1 hr, 2 hrs, 4 hrs, 6 hrs, 8 hrs, 10 hrs, 12 hrs, 15 hrs, 24 hrs, 36 hrs, 48 hrs, 72 hrs, 96 hrs, 120 hrs and 144 hrs post Period 1 Day 1 dosingPopulation: The analysis population included all participants dosed with \[14C\]PF-07081532 in Period 1 who had at least one of the PF-07081532 or total \[14C\] PK parameters of interest.
Apparent clearance of PF-07081532 after the participant received a single oral dose of \[14C\]PF-07081532 30 mg (approximately 250 nCi \[14C\]) in Period 1. Clearance of a drug is a measure of the rate at which a drug is metabolized or eliminated by normal biological processes. Clearance obtained after oral dose (apparent oral clearance) is a quantitative measure of the rate at which a drug substance is removed from the blood. CL/F was calculated as dose/AUCinf, where AUCinf was area under the plasma concentration versus time curve from time zero to infinity.
Outcome measures
| Measure |
Period 1: [14C]PF-07081532 30 mg Oral
n=6 Participants
In Period 1, participants received a single oral dose of \[14C\]PF-07081532 30 mg.
|
Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV
In Period 2, participants received an oral dose of unlabeled PF-07081532 30 mg, followed by IV infusion of \[14C\]PF-07081532 100 µg.
|
|---|---|---|
|
Apparent Clearance of Drug From Plasma (CL/F) of PF-07081532 After A Single Oral Dose of [14C]PF-07081532 in Period 1
|
0.5851 Liter/hour (L/hr)
Geometric Coefficient of Variation 22
|
—
|
SECONDARY outcome
Timeframe: Pre-dose (0 hrs) and 0.5 hrs, 1 hr, 2 hrs, 4 hrs, 6 hrs, 8 hrs, 10 hrs, 12 hrs, 15 hrs, 24 hrs, 36 hrs, 48 hrs, 72 hrs, 96 hrs, 120 hrs and 144 hrs post Period 1 Day 1 dosingPopulation: The analysis population included all participants dosed with \[14C\]PF-07081532 in Period 1 who had at least one of the PF-07081532 or total \[14C\] PK parameters of interest.
Apparent volume of distribution of PF-07081532 after the participant received a single oral dose of \[14C\]PF-07081532 30 mg (approximately 250 nCi \[14C\]) in Period 1. Vz/F is calculated as Dose/(AUCinf \* kel), where kel is the terminal phase rate constant calculated by a linear regression of the log-linear concentration-time curve, AUCinf is area under the plasma concentration versus time curve from time zero extrapolated to infinite time.
Outcome measures
| Measure |
Period 1: [14C]PF-07081532 30 mg Oral
n=6 Participants
In Period 1, participants received a single oral dose of \[14C\]PF-07081532 30 mg.
|
Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV
In Period 2, participants received an oral dose of unlabeled PF-07081532 30 mg, followed by IV infusion of \[14C\]PF-07081532 100 µg.
|
|---|---|---|
|
Plasma Apparent Volume of Distribution (Vz/F) of PF-07081532 After A Single Oral Dose of [14C]PF-07081532 in Period 1
|
16.13 L
Geometric Coefficient of Variation 21
|
—
|
SECONDARY outcome
Timeframe: Pre-dose (0 hrs) and 0.17 hrs, 0.25 hrs, 0.33 hrs, 0.5 hrs, 1 hr, 3 hrs, 5 hrs, 7 hrs, 9 hrs, 11 hrs, 14 hrs, 23 hrs, 35 hrs, 47 hrs, 71 hrs, 95 hrs, 119 hrs and 143 hrs post IV dosing of [14C]PF-07081532 on Period 2 Day 1Population: The analysis population included all participants dosed with \[14C\]PF-07081532 in Period 2 who had at least one of the \[14C\]PF-07081532 PK parameters of interest.
Area under the plasma concentration versus time curve from time zero to the time of the last quantifiable concentration of \[14C\]PF-07081532 after the participant received an oral (PO) dose of unlabeled PF-07081532 30 mg, followed by IV infusion of \[14C\]PF-07081532 100 µg (approximately 1 hour after the oral dose).
Outcome measures
| Measure |
Period 1: [14C]PF-07081532 30 mg Oral
n=6 Participants
In Period 1, participants received a single oral dose of \[14C\]PF-07081532 30 mg.
|
Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV
In Period 2, participants received an oral dose of unlabeled PF-07081532 30 mg, followed by IV infusion of \[14C\]PF-07081532 100 µg.
|
|---|---|---|
|
Plasma AUClast of [14C]PF-07081532 Following Intravenous (IV) Administration of [14C]PF-07081532 in Period 2
|
185.9 ng*hr/mL
Geometric Coefficient of Variation 32
|
—
|
SECONDARY outcome
Timeframe: Pre-dose (0 hrs) and 0.17 hrs, 0.25 hrs, 0.33 hrs, 0.5 hrs, 1 hr, 3 hrs, 5 hrs, 7 hrs, 9 hrs, 11 hrs, 14 hrs, 23 hrs, 35 hrs, 47 hrs, 71 hrs, 95 hrs, 119 hrs and 143 hrs post IV dosing of [14C]PF-07081532 on Period 2 Day 1Population: The analysis population included all participants dosed with \[14C\]PF-07081532 in Period 2 who had at least one of the \[14C\]PF-07081532 PK parameters of interest.
Dose-normalized plasma AUClast of \[14C\]PF-07081532 after the participant received an oral dose of unlabeled PF-07081532 30 mg, followed by IV infusion of \[14C\]PF-07081532 100 µg (equivalent to 0.1 mg; approximately 1 hour after the oral dose). AUClast(dn) = AUClast/Dose, where AUClast = area under the plasma concentration versus time curve from time zero to the time of the last quantifiable concentration, dose = IV dose of \[14C\]PF-07081532 (expressed in mg).
Outcome measures
| Measure |
Period 1: [14C]PF-07081532 30 mg Oral
n=6 Participants
In Period 1, participants received a single oral dose of \[14C\]PF-07081532 30 mg.
|
Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV
In Period 2, participants received an oral dose of unlabeled PF-07081532 30 mg, followed by IV infusion of \[14C\]PF-07081532 100 µg.
|
|---|---|---|
|
Dose-Normalized Plasma AUClast (AUClast(dn) of [14C]PF-07081532 Following IV Administration of [14C]PF-07081532 in Period 2
|
1831 ng*hr/mL/mg
Geometric Coefficient of Variation 28
|
—
|
SECONDARY outcome
Timeframe: Pre-dose (0 hrs) and 0.17 hrs, 0.25 hrs, 0.33 hrs, 0.5 hrs, 1 hr, 3 hrs, 5 hrs, 7 hrs, 9 hrs, 11 hrs, 14 hrs, 23 hrs, 35 hrs, 47 hrs, 71 hrs, 95 hrs, 119 hrs and 143 hrs post IV dosing of [14C]PF-07081532 on Period 2 Day 1Population: The analysis population included all participants dosed with \[14C\]PF-07081532 in Period 2 who had at least one of the \[14C\]PF-07081532 PK parameters of interest.
Maximum plasma concentration of \[14C\]PF-07081532 after the participant received an oral dose of unlabeled PF-07081532 30 mg, followed by IV infusion of \[14C\]PF-07081532 100 µg (approximately 1 hour after the oral dose).
Outcome measures
| Measure |
Period 1: [14C]PF-07081532 30 mg Oral
n=6 Participants
In Period 1, participants received a single oral dose of \[14C\]PF-07081532 30 mg.
|
Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV
In Period 2, participants received an oral dose of unlabeled PF-07081532 30 mg, followed by IV infusion of \[14C\]PF-07081532 100 µg.
|
|---|---|---|
|
Plasma Cmax of [14C]PF-07081532 Following IV Administration of [14C]PF-07081532 in Period 2
|
23.20 ng/mL
Geometric Coefficient of Variation 16
|
—
|
SECONDARY outcome
Timeframe: Pre-dose (0 hrs) and 0.17 hrs, 0.25 hrs, 0.33 hrs, 0.5 hrs, 1 hr, 3 hrs, 5 hrs, 7 hrs, 9 hrs, 11 hrs, 14 hrs, 23 hrs, 35 hrs, 47 hrs, 71 hrs, 95 hrs, 119 hrs and 143 hrs post IV dosing of [14C]PF-07081532 on Period 2 Day 1Population: The analysis population included all participants dosed with \[14C\]PF-07081532 in Period 2 who had at least one of the \[14C\]PF-07081532 PK parameters of interest.
Dose-normalized plasma Cmax of \[14C\]PF-07081532 after the participant received an oral dose of unlabeled PF-07081532 30 mg, followed by IV infusion of \[14C\]PF-07081532 100 µg (equivalent to 0.1 mg; approximately 1 hour after the oral dose). Cmax(dn) = Cmax/Dose, where Cmax = maximum concentration, dose = IV dose of \[14C\]PF-07081532 (expressed in mg).
Outcome measures
| Measure |
Period 1: [14C]PF-07081532 30 mg Oral
n=6 Participants
In Period 1, participants received a single oral dose of \[14C\]PF-07081532 30 mg.
|
Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV
In Period 2, participants received an oral dose of unlabeled PF-07081532 30 mg, followed by IV infusion of \[14C\]PF-07081532 100 µg.
|
|---|---|---|
|
Dose-Normalized Plasma Cmax (Cmax (dn)) of [14C]PF-07081532 Following IV Administration of [14C]PF-07081532 in Period 2
|
228.5 ng/mL/mg
Geometric Coefficient of Variation 13
|
—
|
SECONDARY outcome
Timeframe: Pre-dose (0 hrs) and 0.17 hrs, 0.25 hrs, 0.33 hrs, 0.5 hrs, 1 hr, 3 hrs, 5 hrs, 7 hrs, 9 hrs, 11 hrs, 14 hrs, 23 hrs, 35 hrs, 47 hrs, 71 hrs, 95 hrs, 119 hrs and 143 hrs post IV dosing of [14C]PF-07081532 on Period 2 Day 1Population: The analysis population included all participants dosed with \[14C\]PF-07081532 in Period 2 who had at least one of the \[14C\]PF-07081532 PK parameters of interest.
Time to reach maximum plasma concentration of \[14C\]PF-07081532 after the participant received an oral dose of unlabeled PF-07081532 30 mg, followed by IV infusion of \[14C\]PF-07081532 100 µg (approximately 1 hour after the oral dose).
Outcome measures
| Measure |
Period 1: [14C]PF-07081532 30 mg Oral
n=6 Participants
In Period 1, participants received a single oral dose of \[14C\]PF-07081532 30 mg.
|
Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV
In Period 2, participants received an oral dose of unlabeled PF-07081532 30 mg, followed by IV infusion of \[14C\]PF-07081532 100 µg.
|
|---|---|---|
|
Plasma Tmax of [14C]PF-07081532 Following IV Administration of [14C]PF-07081532 in Period 2
|
0.250 hour
Interval 0.25 to 0.267
|
—
|
SECONDARY outcome
Timeframe: Pre-dose (0 hrs) and 0.17 hrs, 0.25 hrs, 0.33 hrs, 0.5 hrs, 1 hr, 3 hrs, 5 hrs, 7 hrs, 9 hrs, 11 hrs, 14 hrs, 23 hrs, 35 hrs, 47 hrs, 71 hrs, 95 hrs, 119 hrs and 143 hrs post IV dosing of [14C]PF-07081532 on Period 2 Day 1Population: The analysis population included all participants dosed with \[14C\]PF-07081532 in Period 2 who had at least one of the \[14C\]PF-07081532 PK parameters of interest.
Area under the plasma concentration versus time curve from time zero to infinity of \[14C\]PF-07081532 after the participant received an oral dose of unlabeled PF-07081532 30 mg, followed by IV infusion of \[14C\]PF-07081532 100 µg (approximately 1 hour after the oral dose).
Outcome measures
| Measure |
Period 1: [14C]PF-07081532 30 mg Oral
n=6 Participants
In Period 1, participants received a single oral dose of \[14C\]PF-07081532 30 mg.
|
Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV
In Period 2, participants received an oral dose of unlabeled PF-07081532 30 mg, followed by IV infusion of \[14C\]PF-07081532 100 µg.
|
|---|---|---|
|
Plasma AUCinf of [14C]PF-07081532 Following IV Administration of [14C]PF-07081532 in Period 2
|
186.9 ng*hr/mL
Geometric Coefficient of Variation 32
|
—
|
SECONDARY outcome
Timeframe: Pre-dose (0 hrs) and 0.17 hrs, 0.25 hrs, 0.33 hrs, 0.5 hrs, 1 hr, 3 hrs, 5 hrs, 7 hrs, 9 hrs, 11 hrs, 14 hrs, 23 hrs, 35 hrs, 47 hrs, 71 hrs, 95 hrs, 119 hrs and 143 hrs post IV dosing of [14C]PF-07081532 on Period 2 Day 1Population: The analysis population included all participants dosed with \[14C\]PF-07081532 in Period 2 who had at least one of the \[14C\]PF-07081532 PK parameters of interest.
Dose-normalized plasma AUCinf of \[14C\]PF-07081532 after the participant received an oral dose of unlabeled PF-07081532 30 mg, followed by IV infusion of \[14C\]PF-07081532 100 µg (equivalent to 0.1 mg; approximately 1 hour after the oral dose). AUCinf(dn) = AUCinf/Dose, where AUCinf = area under the plasma concentration versus time curve from time zero to infinity, dose = IV dose of \[14C\]PF-07081532 (expressed in mg).
Outcome measures
| Measure |
Period 1: [14C]PF-07081532 30 mg Oral
n=6 Participants
In Period 1, participants received a single oral dose of \[14C\]PF-07081532 30 mg.
|
Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV
In Period 2, participants received an oral dose of unlabeled PF-07081532 30 mg, followed by IV infusion of \[14C\]PF-07081532 100 µg.
|
|---|---|---|
|
Dose-Normalized Plasma AUCinf (AUCinf(dn)) of [14C]PF-07081532 Following IV Administration of [14C]PF-07081532 in Period 2
|
1844 ng*hr/mL/mg
Geometric Coefficient of Variation 29
|
—
|
SECONDARY outcome
Timeframe: Pre-dose (0 hrs) and 0.17 hrs, 0.25 hrs, 0.33 hrs, 0.5 hrs, 1 hr, 3 hrs, 5 hrs, 7 hrs, 9 hrs, 11 hrs, 14 hrs, 23 hrs, 35 hrs, 47 hrs, 71 hrs, 95 hrs, 119 hrs and 143 hrs post IV dosing of [14C]PF-07081532 on Period 2 Day 1Population: The analysis population included all participants dosed with \[14C\]PF-07081532 in Period 2 who had at least one of the \[14C\]PF-07081532 PK parameters of interest.
Plasma terminal half life of \[14C\]PF-07081532 after the participant received an oral dose of unlabeled PF-07081532 30 mg, followed by IV infusion of \[14C\]PF-07081532 100 µg (approximately 1 hour after the oral dose).
Outcome measures
| Measure |
Period 1: [14C]PF-07081532 30 mg Oral
n=6 Participants
In Period 1, participants received a single oral dose of \[14C\]PF-07081532 30 mg.
|
Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV
In Period 2, participants received an oral dose of unlabeled PF-07081532 30 mg, followed by IV infusion of \[14C\]PF-07081532 100 µg.
|
|---|---|---|
|
Plasma t1/2 of [14C]PF-07081532 Following IV Administration of [14C]PF-07081532 in Period 2
|
21.02 hour
Standard Deviation 2.9027
|
—
|
SECONDARY outcome
Timeframe: Pre-dose (0 hrs) and 0.17 hrs, 0.25 hrs, 0.33 hrs, 0.5 hrs, 1 hr, 3 hrs, 5 hrs, 7 hrs, 9 hrs, 11 hrs, 14 hrs, 23 hrs, 35 hrs, 47 hrs, 71 hrs, 95 hrs, 119 hrs and 143 hrs post IV dosing of [14C]PF-07081532 on Period 2 Day 1Population: The analysis population included all participants dosed with \[14C\]PF-07081532 in Period 2 who had at least one of the \[14C\]PF-07081532 PK parameters of interest.
Plasma clearance of \[14C\]PF-07081532 after the participant received an oral dose of unlabeled PF-07081532 30 mg, followed by IV infusion of \[14C\]PF-07081532 100 µg (approximately 1 hour after the oral dose). Clearance of a drug is a measure of the rate at which a drug is metabolized or eliminated by normal biological processes. CL was calculated as (IV dose of \[14C\]PF-07081532) divided by (AUCinf of \[14C\]PF-07081532), where AUCinf = Area under the plasma concentration versus time curve from time zero to infinity.
Outcome measures
| Measure |
Period 1: [14C]PF-07081532 30 mg Oral
n=6 Participants
In Period 1, participants received a single oral dose of \[14C\]PF-07081532 30 mg.
|
Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV
In Period 2, participants received an oral dose of unlabeled PF-07081532 30 mg, followed by IV infusion of \[14C\]PF-07081532 100 µg.
|
|---|---|---|
|
Plasma Clearance (CL) of [14C]PF-07081532 Following IV Administration of [14C]PF-07081532 in Period 2
|
0.5420 L/hr
Geometric Coefficient of Variation 29
|
—
|
SECONDARY outcome
Timeframe: Pre-dose (0 hrs) and 0.17 hrs, 0.25 hrs, 0.33 hrs, 0.5 hrs, 1 hr, 3 hrs, 5 hrs, 7 hrs, 9 hrs, 11 hrs, 14 hrs, 23 hrs, 35 hrs, 47 hrs, 71 hrs, 95 hrs, 119 hrs and 143 hrs post IV dosing of [14C]PF-07081532 on Period 2 Day 1Population: The analysis population included all participants dosed with \[14C\]PF-07081532 in Period 2 who had at least one of the \[14C\]PF-07081532 PK parameters of interest.
Plasma steady-state volume of distribution of \[14C\]PF-07081532 after the participant received an oral dose of unlabeled PF-07081532 30 mg, followed by IV infusion of \[14C\]PF-07081532 100 µg (approximately 1 hour after the oral dose). Vss was calculated as CL \* MRT, where CL was the plasma clearance of \[14C\]PF-07081532, and MRT was the Mean Residence Time of \[14C\]PF-07081532. MRT = AUMCinf/AUCinf - (Infusion time/2), where AUMCinf was the area under the first moment curve from time zero to infinity, AUCinf = area under the plasma concentration versus time curve from time zero to infinity.
Outcome measures
| Measure |
Period 1: [14C]PF-07081532 30 mg Oral
n=6 Participants
In Period 1, participants received a single oral dose of \[14C\]PF-07081532 30 mg.
|
Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV
In Period 2, participants received an oral dose of unlabeled PF-07081532 30 mg, followed by IV infusion of \[14C\]PF-07081532 100 µg.
|
|---|---|---|
|
Plasma Steady-State Volume of Distribution (Vss) of [14C]PF-07081532 Following IV Administration of [14C]PF-07081532 in Period 2
|
10.70 L
Geometric Coefficient of Variation 15
|
—
|
SECONDARY outcome
Timeframe: Pre-dose (0 hrs) and 0.17 hrs, 0.25 hrs, 0.33 hrs, 0.5 hrs, 1 hr, 3 hrs, 5 hrs, 7 hrs, 9 hrs, 11 hrs, 14 hrs, 23 hrs, 35 hrs, 47 hrs, 71 hrs, 95 hrs, 119 hrs and 143 hrs post IV dosing of [14C]PF-07081532 on Period 2 Day 1Population: The analysis population included all participants dosed with \[14C\]PF-07081532 in Period 2 who had at least one of the \[14C\]PF-07081532 PK parameters of interest.
Plasma mean residence time of \[14C\]PF-07081532 after the participant received an oral dose of unlabeled PF-07081532 30 mg, followed by IV infusion of \[14C\]PF-07081532 100 µg (approximately 1 hour after the oral dose). MRT = AUMCinf/AUCinf - (Infusion time/2), where AUMCinf was the area under the first moment curve from time zero to infinity, AUCinf = area under the plasma concentration versus time curve from time zero to infinity.
Outcome measures
| Measure |
Period 1: [14C]PF-07081532 30 mg Oral
n=6 Participants
In Period 1, participants received a single oral dose of \[14C\]PF-07081532 30 mg.
|
Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV
In Period 2, participants received an oral dose of unlabeled PF-07081532 30 mg, followed by IV infusion of \[14C\]PF-07081532 100 µg.
|
|---|---|---|
|
Plasma Mean Residence Time (MRT) of [14C]PF-07081532 Following IV Administration of [14C]PF-07081532 in Period 2
|
19.77 hour
Geometric Coefficient of Variation 21
|
—
|
SECONDARY outcome
Timeframe: Pre-dose (0 hrs) and 0.5 hrs, 1 hr, 2 hrs, 4 hrs, 6 hrs, 8 hrs, 10 hrs, 12 hrs, 15 hrs, 24 hrs, 36 hrs, 48 hrs, 72hrs, 96 hrs, 120 hrs and 144 hrs post oral dosing of unlabeled PF-07081532 on Period 2 Day 1Population: The analysis population included all participants dosed with PF-07081532 and \[14C\]PF-07081532 in Period 2 who had at least one of the PK parameters of interest.
F is a measure of the rate and extent of a drug reaching the systemic circulation in its unchanged form. F was estimated as the ratio of adjusted geometric means of dose-normalized plasma AUCinf following oral unlabeled PF-07081532 and IV \[14C\]PF-07081532 in Period 2, which is equivalent to the following equation: F = (AUCpo/\[14C\]\_AUCiv)\*(\[14C\]\_Doseiv/Dosepo). AUCpo and \[14C\]\_AUCiv were the AUCinf values of unlabeled PF-07081532 and \[14C\]PF-07081532, respectively in Period 2; Dosepo and \[14C\]\_Doseiv were the 30 mg oral dose of unlabeled PF-07081532 and each participant's individual IV dose of \[14C\]PF-07081532, respectively.
Outcome measures
| Measure |
Period 1: [14C]PF-07081532 30 mg Oral
n=6 Participants
In Period 1, participants received a single oral dose of \[14C\]PF-07081532 30 mg.
|
Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV
In Period 2, participants received an oral dose of unlabeled PF-07081532 30 mg, followed by IV infusion of \[14C\]PF-07081532 100 µg.
|
|---|---|---|
|
Absolute Oral Bioavailability (F) of PF-07081532 in Period 2
|
90.79 Percent
Interval 84.62 to 97.41
|
—
|
SECONDARY outcome
Timeframe: Day 1 to Day 7 for both Period 1 and Period 2Population: The analysis population included all participants who received at least 1 dose of study intervention and had at least 1 of the PF-07081532 or \[14C\]PF-07081532 parameters of interest.
Fa was estimated as the ratio of adjusted geometric means of the % of administered radioactive dose excreted into urine following oral (Period 1) and IV (Period 2) dosing of \[14C\]PF-07081532. Urine radioactivity up to Day 7 in Period 1 was used to match the duration of Period 2 urine collection. Fa = (Total \[14C\]\_Urine\_PO\_Trunc/Total \[14C\]\_Urine\_IV) × (\[14C\] Doseiv/\[14C\] Dosepo). Total \[14C\]\_Urine\_PO\_Trunc = Total cumulative radioactivity excreted into urine from time zero up to Day 7 following Period 1 oral dosing, calculated as sum of (\[14C\] urine concentration × sample volume) for each collection interval. Total \[14C\]\_Urine\_IV = Total cumulative radioactivity excreted into urine from time zero to the time of last measurable concentration following Period 2 IV dosing, calculated as sum of (\[14C\] concentration × urine collection volume) for each collection interval (= sum of collection intervals). \[14C\] Dose = radioactivity dose (PO in Period 1, IV in Period 2) for each participant.
Outcome measures
| Measure |
Period 1: [14C]PF-07081532 30 mg Oral
n=6 Participants
In Period 1, participants received a single oral dose of \[14C\]PF-07081532 30 mg.
|
Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV
In Period 2, participants received an oral dose of unlabeled PF-07081532 30 mg, followed by IV infusion of \[14C\]PF-07081532 100 µg.
|
|---|---|---|
|
Fraction Absorbed (Fa) of PF-07081532
|
79.91 Percent
Interval 73.53 to 86.85
|
—
|
SECONDARY outcome
Timeframe: Maximum of 11 weeksPopulation: The safety analysis population included all participants who received at least 1 dose of any study treatment.
An adverse event (AE) was any untoward medical occurrence in a participant who received study drug without regard to possibility of causal relationship with the study treatment. TEAEs were AEs that occurred after initiation of treatment or AEs increasing in severity during treatment. Treatment-related TEAEs were determined by the investigator. A serious adverse event (SAE) was any untoward medical occurrence at any dose that resulted in death; was life threatening; required inpatient hospitalization or prolongation of existing hospitalization; resulted in persistent or significant disability/incapacity; resulted in congenital anomaly/birth defect.
Outcome measures
| Measure |
Period 1: [14C]PF-07081532 30 mg Oral
n=6 Participants
In Period 1, participants received a single oral dose of \[14C\]PF-07081532 30 mg.
|
Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV
n=6 Participants
In Period 2, participants received an oral dose of unlabeled PF-07081532 30 mg, followed by IV infusion of \[14C\]PF-07081532 100 µg.
|
|---|---|---|
|
Number of Participants With Treatment-Emergent Adverse Events (TEAEs)
All-causality TEAE
|
4 Participants
|
2 Participants
|
|
Number of Participants With Treatment-Emergent Adverse Events (TEAEs)
Treatment-related TEAE
|
2 Participants
|
1 Participants
|
|
Number of Participants With Treatment-Emergent Adverse Events (TEAEs)
All-causality SAE
|
0 Participants
|
0 Participants
|
SECONDARY outcome
Timeframe: Maximum of 11 weeksPopulation: The safety analysis population included all participants who received at least 1 dose of any study treatment.
Laboratory tests included hematology, clinical chemistry and urinalysis. Laboratory abnormalities reported in at least 1 participant are reported in this OM.
Outcome measures
| Measure |
Period 1: [14C]PF-07081532 30 mg Oral
n=6 Participants
In Period 1, participants received a single oral dose of \[14C\]PF-07081532 30 mg.
|
Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV
n=6 Participants
In Period 2, participants received an oral dose of unlabeled PF-07081532 30 mg, followed by IV infusion of \[14C\]PF-07081532 100 µg.
|
|---|---|---|
|
Number of Participants With Laboratory Test Abnormality (Without Regard to Baseline Abnormality)
|
1 Participants
|
0 Participants
|
SECONDARY outcome
Timeframe: Maximum of 11 weeksPopulation: The safety analysis population included all participants who received at least 1 dose of any study treatment.
Vital signs data included supine systolic and diastolic blood pressure (BP) and pulse rate. Potentially clinically significant vital signs abnormalities are defined as: systolic BP - minimum (min) absolute result \<90 mmHg, maximum (max) increase or decrease from baseline ≥30 mmHg; diastolic BP - min absolute result \<50 mmHg, max increase or decrease from baseline ≥20 mmHg; supine pulse rate - min absolute result \<40 beat per minute (bpm), max absolute result \>120 bpm. Participants with vital signs data meeting any criteria above are reported in this OM.
Outcome measures
| Measure |
Period 1: [14C]PF-07081532 30 mg Oral
n=6 Participants
In Period 1, participants received a single oral dose of \[14C\]PF-07081532 30 mg.
|
Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV
n=6 Participants
In Period 2, participants received an oral dose of unlabeled PF-07081532 30 mg, followed by IV infusion of \[14C\]PF-07081532 100 µg.
|
|---|---|---|
|
Number of Participants With Post-Baseline Vital Signs Data Meeting Pre-Defined Criteria
|
0 Participants
|
1 Participants
|
SECONDARY outcome
Timeframe: Maximum of 11 weeksPopulation: The safety analysis population included all participants who received at least 1 dose of any study treatment.
ECG data included heart rate, PR interval, QT interval, QT Interval (Fridericia's Correction) (QTcF) and QRS complex. Potentially clinically significant ECG abnormalities are categorized as follows: Uncorrected QT value \>500 millisecond (msec). QTcF - absolute value \>450 and ≤480 msec; absolute value \>480 and ≤500 msec; absolute value \>500 msec; increase from baseline \>30 and ≤60 msec; increase from baseline \>60 msec. PR interval - max absolute value ≥300 msec; baseline value \>200 msec and ≥25% increase from baseline; baseline value ≤200 msec and ≥50% increase from baseline. QRS complex - max absolute value ≥140 msec; ≥50% increase from baseline. Participants with ECG data meeting any criteria above are reported in this OM, if any.
Outcome measures
| Measure |
Period 1: [14C]PF-07081532 30 mg Oral
n=6 Participants
In Period 1, participants received a single oral dose of \[14C\]PF-07081532 30 mg.
|
Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV
n=6 Participants
In Period 2, participants received an oral dose of unlabeled PF-07081532 30 mg, followed by IV infusion of \[14C\]PF-07081532 100 µg.
|
|---|---|---|
|
Number of Participants With Electrocardiogram (ECG) Data Meeting Pre-Defined Criteria
|
0 Participants
|
0 Participants
|
Adverse Events
Period 1: [14C]PF-07081532 30 mg Oral
Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV
Serious adverse events
Adverse event data not reported
Other adverse events
| Measure |
Period 1: [14C]PF-07081532 30 mg Oral
n=6 participants at risk
In Period 1, participants received a single oral dose of \[14C\]PF-07081532 30 mg.
|
Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV
n=6 participants at risk
In Period 2, participants received an oral dose of unlabeled PF-07081532 30 mg, followed by IV infusion of \[14C\]PF-07081532 100 µg.
|
|---|---|---|
|
Gastrointestinal disorders
Abdominal pain
|
16.7%
1/6 • Maximum of 11 weeks
All TEAEs, without regard to possibility of causal relationship with the study treatment, are summarized.
|
0.00%
0/6 • Maximum of 11 weeks
All TEAEs, without regard to possibility of causal relationship with the study treatment, are summarized.
|
|
Gastrointestinal disorders
Dyspepsia
|
0.00%
0/6 • Maximum of 11 weeks
All TEAEs, without regard to possibility of causal relationship with the study treatment, are summarized.
|
16.7%
1/6 • Maximum of 11 weeks
All TEAEs, without regard to possibility of causal relationship with the study treatment, are summarized.
|
|
Gastrointestinal disorders
Frequent bowel movements
|
0.00%
0/6 • Maximum of 11 weeks
All TEAEs, without regard to possibility of causal relationship with the study treatment, are summarized.
|
16.7%
1/6 • Maximum of 11 weeks
All TEAEs, without regard to possibility of causal relationship with the study treatment, are summarized.
|
|
Gastrointestinal disorders
Nausea
|
33.3%
2/6 • Maximum of 11 weeks
All TEAEs, without regard to possibility of causal relationship with the study treatment, are summarized.
|
0.00%
0/6 • Maximum of 11 weeks
All TEAEs, without regard to possibility of causal relationship with the study treatment, are summarized.
|
|
Gastrointestinal disorders
Noninfective gingivitis
|
0.00%
0/6 • Maximum of 11 weeks
All TEAEs, without regard to possibility of causal relationship with the study treatment, are summarized.
|
16.7%
1/6 • Maximum of 11 weeks
All TEAEs, without regard to possibility of causal relationship with the study treatment, are summarized.
|
|
General disorders
Fatigue
|
16.7%
1/6 • Maximum of 11 weeks
All TEAEs, without regard to possibility of causal relationship with the study treatment, are summarized.
|
0.00%
0/6 • Maximum of 11 weeks
All TEAEs, without regard to possibility of causal relationship with the study treatment, are summarized.
|
|
General disorders
Hunger
|
16.7%
1/6 • Maximum of 11 weeks
All TEAEs, without regard to possibility of causal relationship with the study treatment, are summarized.
|
0.00%
0/6 • Maximum of 11 weeks
All TEAEs, without regard to possibility of causal relationship with the study treatment, are summarized.
|
|
General disorders
Malaise
|
0.00%
0/6 • Maximum of 11 weeks
All TEAEs, without regard to possibility of causal relationship with the study treatment, are summarized.
|
16.7%
1/6 • Maximum of 11 weeks
All TEAEs, without regard to possibility of causal relationship with the study treatment, are summarized.
|
|
Infections and infestations
Nasopharyngitis
|
16.7%
1/6 • Maximum of 11 weeks
All TEAEs, without regard to possibility of causal relationship with the study treatment, are summarized.
|
0.00%
0/6 • Maximum of 11 weeks
All TEAEs, without regard to possibility of causal relationship with the study treatment, are summarized.
|
|
Musculoskeletal and connective tissue disorders
Back pain
|
16.7%
1/6 • Maximum of 11 weeks
All TEAEs, without regard to possibility of causal relationship with the study treatment, are summarized.
|
0.00%
0/6 • Maximum of 11 weeks
All TEAEs, without regard to possibility of causal relationship with the study treatment, are summarized.
|
|
Nervous system disorders
Dizziness
|
16.7%
1/6 • Maximum of 11 weeks
All TEAEs, without regard to possibility of causal relationship with the study treatment, are summarized.
|
0.00%
0/6 • Maximum of 11 weeks
All TEAEs, without regard to possibility of causal relationship with the study treatment, are summarized.
|
|
Nervous system disorders
Headache
|
33.3%
2/6 • Maximum of 11 weeks
All TEAEs, without regard to possibility of causal relationship with the study treatment, are summarized.
|
16.7%
1/6 • Maximum of 11 weeks
All TEAEs, without regard to possibility of causal relationship with the study treatment, are summarized.
|
|
Skin and subcutaneous tissue disorders
Rash macular
|
16.7%
1/6 • Maximum of 11 weeks
All TEAEs, without regard to possibility of causal relationship with the study treatment, are summarized.
|
0.00%
0/6 • Maximum of 11 weeks
All TEAEs, without regard to possibility of causal relationship with the study treatment, are summarized.
|
Additional Information
Results disclosure agreements
- Principal investigator is a sponsor employee Pfizer has the right to review disclosures, requesting a delay of less than 60 days. Investigator will postpone single center publications until after disclosure of pooled data (all sites), less than 12 months from study completion/termination at all participating sites. Investigator may not disclose previously undisclosed confidential information other than study results.
- Publication restrictions are in place
Restriction type: OTHER