DelfaGLP-1 Atlas

← Trials/Trial dossier/NCT05652647

CompletedPhase 1Results posted

A Study to Understand How the Study Medicine (PF-07081532) is Processed and Eliminated in Healthy Men

A PHASE 1, OPEN-LABEL, 2-PERIOD, FIXED SEQUENCE STUDY TO INVESTIGATE THE ABSORPTION, DISTRIBUTION, METABOLISM AND EXCRETION OF [14C]PF-07081532 AND TO ASSESS THE ABSOLUTE BIOAVAILABILITY AND FRACTION ABSORBED OF PF-07081532 IN HEALTHY MALE PARTICIPANTS USING A [14C]-MICROTRACER APPROACH

Lead sponsor

Pfizer

Asset

Lotiglipron

Oral · GLP-1 agonist

Listed sites

1

Recruiting sites

—

Enrollment

6

actual

Study population

Healthy volunteers

Key I/E criteria

•BMI 17.5-30.5•Male•Healthy volunteers

Primary endpoints

•Total Recovery of Radioactivity in Urine, Feces and Both Routes Combined•Relative Abundance of [14C]PF-07081532•Relative Abundance of [14C]PF-07081532 and Its Metabolites in Urine

Footprint

Where this trial recruits

Site locations as reported to ClinicalTrials.gov. Site count is not enrollment count; per-site enrollment is not available from source.

Identifiers

Registered as

NCT IDNCT05652647
Org study IDC3991006

Timeline

Milestones

Study first posted2022-12-15actual
Study start2022-12-21actual
Primary completion2023-03-15actual
Study completion2023-03-15actual
Last update posted2024-09-24actual
Results first posted2024-09-24actual

Assets

Investigational agents

Lotiglipron

Study populations

Who this study enrolls

Healthy volunteers

Eligibility

Who can enroll

Minimum age18 Years
Maximum age60 Years
SexMale
Healthy volunteersAccepted

Inclusion 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.

Endpoints (60)

What's being measured

Protocol endpoints and posted registry outcome measures, grouped into outcome categories. Composite endpoints show their component event types. Standard codes (LOINC, SNOMED CT) are shown where available.

Safety / tolerability / PK

60 endpoints
Primary/registry result

Total Recovery of Radioactivity in Urine, Feces and Both Routes Combined, as Percentage of Orally Administered Radioactive Dose of [14C]PF-07081532

Time frame:360 hours

descriptive

Posted result

GroupValue (mean), Percentage of radioactive dose95% CI
Period 1: [14C]PF-07081532 30 mg OralUrine4.7—
Feces78.6—
Urine + Feces83.4—
Primary/registry result

Relative Abundance of [14C]PF-07081532 and Its Metabolites in Plasma After A Single Oral Dose of [14]PF-07081532 in Period 1

Time frame: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 dosing

concentration, descriptive

Posted result

GroupValue (number), Percentage of circulating radioactivity95% CI
Period 1: [14C]PF-07081532 30 mg Oral767a (hydroxy glucuronide)1.2—
PF-07943285 (hydroxy glucuronide)8.8—
767c (hydroxy glucuronide)0.4—
671 (hydroxy sulfate)0.6—
Coeluting components: PF-07214855, PF-07260051, PF-079432849.1—
PF-0708153279.3—
Unassigned [14C]0.6—
Primary/registry result

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

Time frame:96 hours for urine samples and 144 hours for feces samples

descriptive

Posted result

GroupValue (number), Percentage of radioactive dose95% CI
Period 1: [14C]PF-07081532 30 mg OralUrine: PF-07943285 (hydroxy glucuronide)0.1—
Urine: 767c (hydroxy glucuronide)0.03—
Urine: coeluting components PF-07214855 , PF-07260051 and PF-079432840.2—
Urine: PF-070815320.04—
Urine: Unassigned [14C]4.33—
Feces: PF-07240437 (catechol)3.89—
Feces: PF-07943283 (hydroxy)13.6—
Feces: coeluting components PF-07260051 and PF-0794328424.7—
Feces: PF-0708153213.2—
Feces: Unassigned [14C]23.2—
Primary/protocol endpoint/low confidence

Total Recovery of Radioactivity in Urine, Feces and Both Routes Combined, as Percentage of Orally Administered Radioactive Dose of [14C]PF-07081532

Time frame:360 hours

percent change from baseline, descriptive

componentsurine recovery radioactivity pct dose, feces recovery radioactivity pct dose, total recovery both routes pct dose

Primary/protocol endpoint

Relative Abundance of [14C]PF-07081532 and Its Metabolites in Plasma After A Single Oral Dose of [14]PF-07081532 in Period 1

Time frame: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 dosing

descriptive

Primary/protocol endpoint

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

Time frame:96 hours for urine samples and 144 hours for feces samples

descriptive

Secondary/registry result

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

Time frame: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 dosing

concentration, descriptive

Posted result

GroupValue (geometric_mean), ngEq*hr/mL95% CI
Period 1: [14C]PF-07081532 30 mg Oral74360—
Secondary/registry result

AUClast of PF-07081532 After A Single Oral Dose of [14]PF-07081532 in Period 1

Time frame: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 dosing

descriptive

Posted result

GroupValue (geometric_mean), nanogram*hr/milliliter (ng*hr/mL)95% CI
Period 1: [14C]PF-07081532 30 mg Oral49380—
Secondary/registry result

Plasma Maximum Observed Concentration (Cmax) of Total [14C] After A Single Oral Dose of [14C]PF-07081532 in Period 1

Time frame: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 dosing

concentration, descriptive

Posted result

GroupValue (geometric_mean), nanogram equivalent/milliliter (ngEq/mL)95% CI
Period 1: [14C]PF-07081532 30 mg Oral2934—
Secondary/registry result

Plasma Cmax of PF-07081532 After A Single Oral Dose of [14C]PF-07081532 in Period 1

Time frame: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 dosing

concentration, descriptive

Posted result

GroupValue (geometric_mean), nanogram/milliliter (ng/mL)95% CI
Period 1: [14C]PF-07081532 30 mg Oral2874—
Secondary/registry result

Plasma Time to Reach Cmax (Tmax) of Total [14C] and PF-07081532 After A Single Oral Dose of [14C]PF-07081532 in Period 1

Time frame: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 dosing

time to event, event

Posted result

GroupValue (median), hour95% CI
Period 1: [14C]PF-07081532 30 mg OralTotal [14C]4.932.00 – 6.00
PF-070815323.932.00 – 6.00
Secondary/registry result

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

Time frame: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 dosing

concentration, descriptive

Posted result

GroupValue (geometric_mean), ngEq*hr/mL95% CI
Period 1: [14C]PF-07081532 30 mg Oral76050—
Secondary/registry result

AUCinf of PF-07081532 After A Single Oral Dose of [14C]PF-07081532 in Period 1

Time frame: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 dosing

descriptive

Posted result

GroupValue (geometric_mean), ng*hr/mL95% CI
Period 1: [14C]PF-07081532 30 mg Oral51370—
Secondary/registry result

Plasma Elimination Half Life (t1/2) of Total [14C] and PF-07081532 After A Single Oral Dose of [14C]PF-07081532 in Period 1

Time frame: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 dosing

concentration, descriptive

Posted result

GroupValue (mean), hour95% CI
Period 1: [14C]PF-07081532 30 mg OralTotal [14C]65.20—
PF-0708153219.42—
Secondary/registry result

Apparent Clearance of Drug From Plasma (CL/F) of PF-07081532 After A Single Oral Dose of [14C]PF-07081532 in Period 1

Time frame: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 dosing

concentration, descriptive

Posted result

GroupValue (geometric_mean), Liter/hour (L/hr)95% CI
Period 1: [14C]PF-07081532 30 mg Oral0.5851—
Secondary/registry result

Plasma Apparent Volume of Distribution (Vz/F) of PF-07081532 After A Single Oral Dose of [14C]PF-07081532 in Period 1

Time frame: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 dosing

concentration, descriptive

Posted result

GroupValue (geometric_mean), L95% CI
Period 1: [14C]PF-07081532 30 mg Oral16.13—
Secondary/registry result

Plasma AUClast of [14C]PF-07081532 Following Intravenous (IV) Administration of [14C]PF-07081532 in Period 2

Time frame: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 1

concentration, descriptive

Posted result

GroupValue (geometric_mean), ng*hr/mL95% CI
Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV185.9—
Secondary/registry result

Dose-Normalized Plasma AUClast (AUClast(dn) of [14C]PF-07081532 Following IV Administration of [14C]PF-07081532 in Period 2

Time frame: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 1

concentration, descriptive

Posted result

GroupValue (geometric_mean), ng*hr/mL/mg95% CI
Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV1831—
Secondary/registry result

Plasma Cmax of [14C]PF-07081532 Following IV Administration of [14C]PF-07081532 in Period 2

Time frame: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 1

concentration, descriptive

Posted result

GroupValue (geometric_mean), ng/mL95% CI
Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV23.20—
Secondary/registry result

Dose-Normalized Plasma Cmax (Cmax (dn)) of [14C]PF-07081532 Following IV Administration of [14C]PF-07081532 in Period 2

Time frame: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 1

concentration, descriptive

Posted result

GroupValue (geometric_mean), ng/mL/mg95% CI
Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV228.5—
Secondary/registry result

Plasma Tmax of [14C]PF-07081532 Following IV Administration of [14C]PF-07081532 in Period 2

Time frame: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 1

concentration, descriptive

Posted result

GroupValue (median), hour95% CI
Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV0.2500.250 – 0.267
Secondary/registry result

Plasma AUCinf of [14C]PF-07081532 Following IV Administration of [14C]PF-07081532 in Period 2

Time frame: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 1

concentration, descriptive

Posted result

GroupValue (geometric_mean), ng*hr/mL95% CI
Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV186.9—
Secondary/registry result

Dose-Normalized Plasma AUCinf (AUCinf(dn)) of [14C]PF-07081532 Following IV Administration of [14C]PF-07081532 in Period 2

Time frame: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 1

concentration, descriptive

Posted result

GroupValue (geometric_mean), ng*hr/mL/mg95% CI
Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV1844—
Secondary/registry result

Plasma t1/2 of [14C]PF-07081532 Following IV Administration of [14C]PF-07081532 in Period 2

Time frame: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 1

concentration, descriptive

Posted result

GroupValue (mean), hour95% CI
Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV21.02—
Secondary/registry result

Plasma Clearance (CL) of [14C]PF-07081532 Following IV Administration of [14C]PF-07081532 in Period 2

Time frame: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 1

concentration, descriptive

Posted result

GroupValue (geometric_mean), L/hr95% CI
Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV0.5420—
Secondary/registry result

Plasma Steady-State Volume of Distribution (Vss) of [14C]PF-07081532 Following IV Administration of [14C]PF-07081532 in Period 2

Time frame: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 1

concentration, descriptive

Posted result

GroupValue (geometric_mean), L95% CI
Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV10.70—
Secondary/registry result

Plasma Mean Residence Time (MRT) of [14C]PF-07081532 Following IV Administration of [14C]PF-07081532 in Period 2

Time frame: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 1

concentration, descriptive

Posted result

GroupValue (geometric_mean), hour95% CI
Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV19.77—
Secondary/registry result

Absolute Oral Bioavailability (F) of PF-07081532 in Period 2

Time frame: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 1

descriptive

Posted result

GroupValue (geometric_mean), Percent95% CI
Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV90.7984.62 – 97.41
Secondary/registry result

Fraction Absorbed (Fa) of PF-07081532

Time frame:Day 1 to Day 7 for both Period 1 and Period 2

descriptive

Posted result

GroupValue (geometric_mean), Percent95% CI
Period 1: [14C]PF-07081532 30 mg Oral; Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV79.9173.53 – 86.85
Secondary/registry result

Number of Participants With Treatment-Emergent Adverse Events (TEAEs)

Time frame:Maximum of 11 weeks

event count, event

Posted result

GroupValue (count_of_participants), Participants95% CI
Period 1: [14C]PF-07081532 30 mg OralAll-causality TEAE4—
Treatment-related TEAE2—
All-causality SAE0—
Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IVAll-causality TEAE2—
Treatment-related TEAE1—
All-causality SAE0—
Secondary/registry result

Number of Participants With Laboratory Test Abnormality (Without Regard to Baseline Abnormality)

Time frame:Maximum of 11 weeks

event count, event

Posted result

GroupValue (count_of_participants), Participants95% CI
Period 1: [14C]PF-07081532 30 mg Oral1—
Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV0—
Secondary/registry result

Number of Participants With Post-Baseline Vital Signs Data Meeting Pre-Defined Criteria

Time frame:Maximum of 11 weeks

event count, event

Posted result

GroupValue (count_of_participants), Participants95% CI
Period 1: [14C]PF-07081532 30 mg Oral0—
Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV1—
Secondary/registry result

Number of Participants With Electrocardiogram (ECG) Data Meeting Pre-Defined Criteria

Time frame:Maximum of 11 weeks

event count, event

Posted result

GroupValue (count_of_participants), Participants95% CI
Period 1: [14C]PF-07081532 30 mg Oral0—
Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV0—
Secondary/protocol endpoint/low confidence

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

Time frame: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 dosing

concentration, descriptive

Secondary/protocol endpoint

AUClast of PF-07081532 After A Single Oral Dose of [14]PF-07081532 in Period 1

Time frame: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 dosing

concentration, descriptive

Secondary/protocol endpoint

Plasma Maximum Observed Concentration (Cmax) of Total [14C] After A Single Oral Dose of [14C]PF-07081532 in Period 1

Time frame: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 dosing

Cmax

concentration, descriptive

Secondary/protocol endpoint

Plasma Cmax of PF-07081532 After A Single Oral Dose of [14C]PF-07081532 in Period 1

Time frame: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 dosing

Cmax

concentration, descriptive

Secondary/protocol endpoint

Plasma Time to Reach Cmax (Tmax) of Total [14C] and PF-07081532 After A Single Oral Dose of [14C]PF-07081532 in Period 1

Time frame: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 dosing

Tmax

descriptive

Secondary/protocol endpoint

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

Time frame: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 dosing

AUC₀–∞

concentration, descriptive

Secondary/protocol endpoint

AUCinf of PF-07081532 After A Single Oral Dose of [14C]PF-07081532 in Period 1

Time frame: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 dosing

AUC₀–∞

concentration, descriptive

Secondary/protocol endpoint

Plasma Elimination Half Life (t1/2) of Total [14C] and PF-07081532 After A Single Oral Dose of [14C]PF-07081532 in Period 1

Time frame: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 dosing

Half-life

descriptive

Secondary/protocol endpoint

Apparent Clearance of Drug From Plasma (CL/F) of PF-07081532 After A Single Oral Dose of [14C]PF-07081532 in Period 1

Time frame: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 dosing

descriptive

Secondary/protocol endpoint

Plasma Apparent Volume of Distribution (Vz/F) of PF-07081532 After A Single Oral Dose of [14C]PF-07081532 in Period 1

Time frame: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 dosing

descriptive

Secondary/protocol endpoint

Plasma AUClast of [14C]PF-07081532 Following Intravenous (IV) Administration of [14C]PF-07081532 in Period 2

Time frame: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 1

concentration, descriptive

Secondary/protocol endpoint

Dose-Normalized Plasma AUClast (AUClast(dn) of [14C]PF-07081532 Following IV Administration of [14C]PF-07081532 in Period 2

Time frame: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 1

concentration, descriptive

Secondary/protocol endpoint

Plasma Cmax of [14C]PF-07081532 Following IV Administration of [14C]PF-07081532 in Period 2

Time frame: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 1

Cmax

concentration, descriptive

Secondary/protocol endpoint

Dose-Normalized Plasma Cmax (Cmax (dn)) of [14C]PF-07081532 Following IV Administration of [14C]PF-07081532 in Period 2

Time frame: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 1

Cmax

concentration, descriptive

Secondary/protocol endpoint

Plasma Tmax of [14C]PF-07081532 Following IV Administration of [14C]PF-07081532 in Period 2

Time frame: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 1

Tmax

descriptive

Secondary/protocol endpoint

Plasma AUCinf of [14C]PF-07081532 Following IV Administration of [14C]PF-07081532 in Period 2

Time frame: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 1

AUC₀–∞

concentration, descriptive

Secondary/protocol endpoint

Dose-Normalized Plasma AUCinf (AUCinf(dn)) of [14C]PF-07081532 Following IV Administration of [14C]PF-07081532 in Period 2

Time frame: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 1

AUC₀–∞

concentration, descriptive

Secondary/protocol endpoint

Plasma t1/2 of [14C]PF-07081532 Following IV Administration of [14C]PF-07081532 in Period 2

Time frame: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 1

Half-life

descriptive

Secondary/protocol endpoint

Plasma Clearance (CL) of [14C]PF-07081532 Following IV Administration of [14C]PF-07081532 in Period 2

Time frame: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 1

descriptive

Secondary/protocol endpoint

Plasma Steady-State Volume of Distribution (Vss) of [14C]PF-07081532 Following IV Administration of [14C]PF-07081532 in Period 2

Time frame: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 1

descriptive

Secondary/protocol endpoint

Plasma Mean Residence Time (MRT) of [14C]PF-07081532 Following IV Administration of [14C]PF-07081532 in Period 2

Time frame: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 1

descriptive

Secondary/protocol endpoint

Absolute Oral Bioavailability (F) of PF-07081532 in Period 2

Time frame: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 1

ratio, descriptive

Secondary/protocol endpoint

Fraction Absorbed (Fa) of PF-07081532

Time frame:Day 1 to Day 7 for both Period 1 and Period 2

ratio, descriptive

Secondary/protocol endpoint

Number of Participants With Treatment-Emergent Adverse Events (TEAEs)

Time frame:Maximum of 11 weeks

Treatment-emergent AEs (any)

event count, event

Secondary/protocol endpoint

Number of Participants With Laboratory Test Abnormality (Without Regard to Baseline Abnormality)

Time frame:Maximum of 11 weeks

event count, event

Secondary/protocol endpoint

Number of Participants With Post-Baseline Vital Signs Data Meeting Pre-Defined Criteria

Time frame:Maximum of 11 weeks

threshold achievement, event

componentsSystolic BP, change, Diastolic BP, change, Heart rate, change

Secondary/protocol endpoint

Number of Participants With Electrocardiogram (ECG) Data Meeting Pre-Defined Criteria

Time frame:Maximum of 11 weeks

threshold achievement, event

Provenance

Sources

Trial identity, design, statusClinicalTrials.gov API v2
Snapshot dateJuly 1, 2026
Endpoint classificationDelfa endpoint taxonomy v2 (May 13, 2026)
Results tableClinicalTrials.gov results section

Trial facts come from public ClinicalTrials.gov records. Endpoint categories are Delfa's classification of those records, not a ClinicalTrials.gov field. All figures reflect the July 1, 2026 snapshot.