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A Study to Evaluate Pharmacokinetics (PK) of Etrumadenant Tablet and Capsule Formulations in Healthy Adult Participants

Phase 1
Completed
Conditions
Healthy Participants
Interventions
Registration Number
NCT05277012
Lead Sponsor
Arcus Biosciences, Inc.
Brief Summary

This study will compare the pharmacokinetics (PK) effect of single-dose etrumadenant tablet and capsule formulations in fasted conditions. The effect of food on single-dose PK of tablet formulation will also be assessed.

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
24
Inclusion Criteria
  • Healthy, adult, male or female (non-childbearing potential), 19-55 years of age, inclusive, at the screening visit.
  • Body mass index (BMI) between 18.0 and 32.0 kilograms/m^2 inclusive, at screening.
  • Healthy as determined by medical history, physical examination, vital signs, and ECG assessed at the screening visit.
  • Clinical laboratory test results clinically acceptable at screening and check in.
  • Non-smokers or ex-smokers [must have ceased smoking and stopped using nicotine containing products greater than (>) 3 months prior to the first dosing] based on participant self-reporting.
  • Able to swallow multiple capsules or tablets.
Exclusion Criteria
  • Participants who have a clinically relevant history or presence of respiratory, gastrointestinal, renal, hepatic, hematological, lymphatic, neurological, cardiovascular, psychiatric, musculoskeletal, genitourinary, immunological, rheumatological, dermatological, endocrine, connective tissue diseases or disorders, in the opinion of the PI or designee.
  • Have a clinically relevant surgical history, in the opinion of the PI or designee.
  • History of relevant atopy or hypersensitivity to etrumadenant or related compounds.
  • History or presence of alcohol or drug abuse within the past 2 years prior to the first dosing.
  • History (within 3 months of screening visit) of alcohol consumption exceeding 2 standard drinks per day on average (1 standard drink = 10 g of alcohol [equivalent to approximately 8 oz of beer (5.5% alcohol); 1 oz of 45% alcohol; or 3.5 oz of wine (12% alcohol)] based on self-reporting.
  • Have a significant infection or known inflammatory process upon screening or check in, in the opinion of the PI or designee.
  • Have acute gastrointestinal symptoms (e.g., nausea, vomiting, diarrhea, heartburn) at the time of screening or check in.
  • Female participants of childbearing potential.
  • Positive results for hepatitis B, C, HIV-1 or HIV-2.
  • Clinically significant hypokalemia in the opinion of the PI or designee.
  • Have been on a diet incompatible with the on study diet, in the opinion of the PI or designee, within the 30 days prior to the first dosing.
  • Donation of blood or significant blood loss within 56 days prior to the first dosing.
  • Plasma donation within 7 days prior to the first dosing.
  • Participation in another clinical study within 30 days prior to the first dosing.

Study & Design

Study Type
INTERVENTIONAL
Study Design
CROSSOVER
Arm && Interventions
GroupInterventionDescription
Treatment sequence ABCEtrumadenantParticipants will be sequentially administered with Treatment A, B then C (Treatment A: etrumadenant capsule in fasted state; Treatment B: etrumadenant tablet in fasted state; Treatment C: etrumadenant tablet in fed state). Each treatment will be separated by a washout period of 7 days.
Treatment sequence BCAEtrumadenantParticipants will be sequentially administered with Treatment B, C then A. Each treatment will be separated by a washout period of 7 days.
Treatment sequence CABEtrumadenantParticipants will be sequentially administered with Treatment C, A then B. Each treatment will be separated by a washout period of 7 days.
Primary Outcome Measures
NameTimeMethod
Ratio of Etrumadenant metabolites to EtrumadenantMultiple timepoint evaluations from pre-dose to 24 hours post-dose at Days 1, 2, 3, 4, 5, and 6 during Treatment Period 1, 2 and 3
Maximum Observed Plasma Concentration (Cmax) of EtrumadenantMultiple timepoint evaluations from pre-dose to 24 hours post-dose at Days 1, 2, 3, 4, 5, and 6 during Treatment Period 1, 2 and 3
Time to Cmax (Tmax) of EtrumadenantMultiple timepoint evaluations from pre-dose to 24 hours post-dose at Days 1, 2, 3, 4, 5, and 6 during Treatment Period 1, 2 and 3
Apparent First-order Terminal Elimination Rate Constant (Kel) of EtrumadenantMultiple timepoint evaluations from pre-dose to 24 hours post-dose at Days 1, 2, 3, 4, 5, and 6 during Treatment Period 1, 2 and 3
Area Under the Plasma Concentration-time Curve From 0 to Last Observed Non-zero Concentration [AUC(0-t)] of EtrumadenantMultiple timepoint evaluations from pre-dose to 24 hours post-dose at Days 1, 2, 3, 4, 5, and 6 during Treatment Period 1, 2 and 3
Area Under the Plasma Concentration Time Curve From Time '0' Extrapolated to Infinity [AUC(0-inf)] of EtrumadenantMultiple timepoint evaluations from pre-dose to 24 hours post-dose at Days 1, 2, 3, 4, 5, and 6 during Treatment Period 1, 2 and 3
Percentage of AUC(0-inf) Extrapolation (AUC%extrap) of EtrumadenantMultiple timepoint evaluations from pre-dose to 24 hours post-dose at Days 1, 2, 3, 4, 5, and 6 during Treatment Period 1, 2 and 3
Apparent First Order Terminal Elimination Half-life (t1/2) of EtrumadenantMultiple timepoint evaluations from pre-dose to 24 hours post-dose at Days 1, 2, 3, 4, 5, and 6 during Treatment Period 1, 2 and 3
Apparent Total Plasma Clearance (CL/F) of EtrumadenantMultiple timepoint evaluations from pre-dose to 24 hours post-dose at Days 1, 2, 3, 4, 5, and 6 during Treatment Period 1, 2 and 3
Apparent Volume of Distribution During the Terminal Elimination Phase (Vz/F) of EtrumadenantMultiple timepoint evaluations from pre-dose to 24 hours post-dose at Days 1, 2, 3, 4, 5, and 6 during Treatment Period 1, 2 and 3
Ratio of Etrumadenant metabolites to Total Metabolite ConcentrationMultiple timepoint evaluations from pre-dose to 24 hours post-dose at Days 1, 2, 3, 4, 5, and 6 during Treatment Period 1, 2 and 3
Secondary Outcome Measures
NameTimeMethod
Number of Participants with Treatment Emergent Adverse Events (TEAEs)Up to 4 months

Safety will be assessed by monitoring adverse events and clinically significant changes in 12 lead Electrocardiogram, vital signs, and clinical laboratory tests results.

Trial Locations

Locations (1)

Investigational Site

🇺🇸

Lincoln, Nebraska, United States

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