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Phase 1 N=6 Treatment

A Study To Evaluate The Pharmacokinetics, Excretion, Mass Balance and Metabolism of PF-07265803

Healthy

Enrolled (actual)
6
Serious AEs
0.0%
Results posted
Mar 2024
Primary outcome: Primary: Total Recovery of Radioactivity in Urine, Expressed as Percentage of Total Radioactive Dose Administered — 13.98 Percentage of total radioactive dose

Study Design & Population

Study type
Interventional
Phase
Phase 1
Interventions
PF-07265803 (Drug)
Age
Adult, Older Adult · 18+ yrs
Sex
Male
Sponsor
Pfizer
Primary completion
May 2022

Outcome Measures

OutcomeResultp-value
PRIMARY
Total Recovery of Radioactivity in Urine, Expressed as Percentage of Total Radioactive Dose Administered
13.98
PRIMARY
Total Recovery of Radioactivity in Feces, Expressed as Percentage of Total Radioactive Dose Administered
74.65
PRIMARY
Total Recovery of Radioactivity in Total Excretion (Urine + Feces), Expressed as Percentage of Total Radioactive Dose Administered
88.64
PRIMARY
Relative Abundance of PF-07265803 and Its Metabolites in Plasma, Expressed as Percentage of Radioactivity
8.49; 68.27; 12.73; 2.58; 2.58
PRIMARY
Relative Abundance of PF-07265803 and Its Metabolites in Urine, Expressed as Percentage of Radioactivity
6.86; 63.9; 11.9; 0.888; 1.61
PRIMARY
Relative Abundance of PF-07265803 and Its Metabolites in Feces, Expressed as Percentage of Radioactivity
1.53; 78.1; 6.79; 6.45; 1.90
SECONDARY
Area Under the Plasma Concentration-Time Profile From Time 0 to Time of the Last Quantifiable Concentration (AUClast) of Total Radioactivity of [14C]PF-07265803 in Plasma
5345
SECONDARY
Area Under the Plasma Concentration-Time Profile From Time 0 Extrapolated to Infinite Time (AUCinf) of Total Radioactivity of [14C]PF-07265803 in Plasma
6430
SECONDARY
Maximum Plasma Concentration (Cmax) of Total Radioactivity of [14C]PF-07265803 in Plasma
1183
SECONDARY
Time for Cmax (Tmax) of Total Radioactivity of [14C]PF-07265803 in Plasma
1.000
SECONDARY
Terminal Elimination Half-life (t1/2) of Total Radioactivity of [14C]PF-07265803 in Plasma
3.24
SECONDARY
AUClast of PF-07265803, PF-07327859, PF-07327860 and PF-07327890 in Plasma
313.2; 3661; 828.3; 855.5
SECONDARY
AUCinf of PF-07265803, PF-07327859, PF-07327860 and PF-07327890 in Plasma
315.1; 3451; 1018; 871.7
SECONDARY
Apparent Clearance (CL/F) of PF-07265803 in Plasma
1280
SECONDARY
Apparent Volume (Vz/F) of PF-07265803 in Plasma
3158
SECONDARY
Cmax of PF-07265803, PF-07327859, PF-07327860 and PF-07327890 in Plasma
258.6; 741.2; 22.38; 117.3
SECONDARY
Tmax of PF-07265803, PF-07327859, PF-07327860 and PF-07327890 in Plasma
0.5000; 1.000; 24.00; 2.500
SECONDARY
t1/2 of PF-07265803, PF-07327859, PF-07327860 and PF-07327890 in Plasma
1.713; 4.985; 14.79; 11.97
SECONDARY
Number of Participants With All-Causality and Treatment-Related Treatment-Emergent Adverse Events (TEAEs)
0; 0; 0; 0
SECONDARY
Number of Participants With Laboratory Abnormalities Without Regard to Baseline Abnormality
1; 1
SECONDARY
Number of Participants With Clinically Significant Vital Signs Values
SECONDARY
Number of Participants With Clinically Significant Electrocardiogram (ECG) Values

Summary

The purpose of this study is to assess the pharmacokinetics, excretion, mass balance and metabolism of PF-07265803 (formerly known as ARRY-371797) in approximately 6 healthy adult male participants.

Eligibility Criteria

Inclusion Criteria

  • Participants must be male and ≥18 years of age at the time of signing the informed consent.
  • Male participants who are overtly healthy as determined by medical evaluation including medical history, physical examination, laboratory tests, and electrocardiogram (ECG) monitoring.
  • Participants who are willing and able to comply with all scheduled visits, treatment plan, laboratory tests , lifestyle considerations , and other study procedures.
  • Body Mass Index of 18.0 to 32 kg/m2; and a total body weight >50 kg (110 lb).
  • Capable of giving signed informed consent, which includes compliance with the requirements and restrictions listed in the ICD and in this protocol.

Exclusion Criteria

  • Evidence or history of clinically significant hematological, renal, endocrine, pulmonary, gastrointestinal, cardiovascular, hepatic, psychiatric, neurological, or allergic disease (including drug allergies, but excluding untreated, asymptomatic, seasonal allergies at the time of dosing).
  • Any condition possibly affecting drug absorption (eg, gastrectomy, cholecystectomy, gastric bypass, duodenotomy, colectomy, history of inflammatory bowel disease).
  • History of HIV infection, hepatitis B, or hepatitis C; positive testing for HIV, HBsAg, or HCVAb. Hepatitis B vaccination is allowed.
  • Participants with a history of irregular bowel movements; e.g., less than 1 bowel movement per day, regular episodes of diarrhea or constipation, irritable bowel syndrome (IBS) or lactose intolerance.
  • Other medical or psychiatric condition including recent (within the past year) or active suicidal ideation/behavior or laboratory abnormality or other conditions or situations related to COVID-19 pandemic (eg. Contact with positive case)] that may increase the risk of study participation or, in the investigator's judgment, make the participant inappropriate for the study.
  • Use of prescription or nonprescription drugs and dietary and herbal supplements within 7 days or 5 half lives (whichever is longer) prior to the first dose of study intervention with the exception of moderate/potent CYP3A inducers which are prohibited within 14 days plus 5 half-lives prior to the first dose of study intervention.
  • Current use of any prohibited concomitant medication(s) or those unwilling/unable to use a permitted concomitant medication(s).
  • Previous administration with an investigational drug within 30 days (or as determined by the local requirement) or 5 half lives preceding the first dose of study intervention used in this study (whichever is longer).
  • A positive urine drug test.
  • Screening and baseline supine blood pressure (BP) >140 mm Hg (systolic) or >90 mm Hg (diastolic), following at least 5 minutes of supine rest. If BP is >140 mm Hg (systolic) or >90 mm Hg (diastolic), the BP should be repeated 2 more times and the average of the 3 BP values should be used to determine the participant's eligibility.
  • Screening and baseline standard 12 lead ECG that demonstrates clinically relevant abnormalities that may affect participant safety or interpretation of study results (eg, baseline QTcF interval >450 msec, atrial fibrillation, complete left bundle branch block (LBBB), signs of an acute or indeterminate age myocardial infarction, ST T interval changes suggestive of myocardial ischemia, second or third degree AV block, or serious bradyarrhythmias or tachyarrhythmias). If the baseline uncorrected QT interval is >450 msec, this interval should be rate corrected using the Fridericia method and the resulting QTcF should be used for decision making and reporting. If QTcF exceeds 450 msec, or QRS exceeds 120 msec, the ECG should be repeated 2 more times and the average of the 3 QTcF or QRS values should be used to determine the participant's eligibility. Computer interpreted ECGs should be overread by a physician experienced in reading ECGs before excluding a participant.
  • Participants with ANY of the following abnormalities in
View full record on ClinicalTrials.gov →

Data sourced from ClinicalTrials.gov (NCT05286281). 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.

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