A Bioequivalence Study Between Two Casdatifan Tablet Strengths and Food Effect Study of Casdatifan in Healthy Adult Participants

A Phase 1, Open-Label, Randomized, Single-Dose, Three-Treatment, Three-Period, Six-Sequence Crossover Pharmacokinetic Study to Evaluate the Bioequivalence of Two Casdatifan (AB521) Tablet Strengths and Food Effect in Healthy Adult Participants

The purpose of this study is to compare the single-dose pharmacokinetics (PK) of casdatifan 100 mg versus four 25 mg tablets under fasting conditions in healthy adult participants, and to evaluate the effect of food on the single-dose PK of casdatifan 100 mg administered as four 25 mg tablets in healthy adult participants.

Study Overview

• Status: Not yet recruiting
• Conditions: Healthy Participants
• Intervention / Treatment: Drug: Casdatifan

• Study Type: Interventional
• Enrollment (Estimated): 24
• Phase: Phase 1

Contacts and Locations

• Study Contact: Name: Medical Director; Phone Number: +1-510-462-3330; Email: ClinicalTrialInquiry@arcusbio.com

Study Locations

• United States
  • Arizona
    • Tempe, Arizona, United States, 85283
      • Research Site

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: Adult
• Accepts Healthy Volunteers: Yes

Description

Inclusion Criteria:

• Continuous non-smoker who has not used nicotine- and tobacco-containing products for at least 3 months prior to the first dosing based on participant self-reporting.
• BMI ≥ 18.0 and ≤ 32.0 kg/m2 and body weight ≥ 45 kg at the screening visit.
• Medically healthy with no clinically significant medical history, physical examination, clinical laboratory profiles, standard vital signs, and ECGs, as deemed by the PI or designee.
• Able to swallow multiple tablets.
• Has adequate peripheral venous access.

Exclusion Criteria:

• Is mentally or legally incapacitated or has significant emotional problems at the time of the screening visit or expected during the conduct of the study.
• History of any illness that, in the opinion of the PI or designee, might confound the results of the study or poses an additional risk to the participant by their participation in the study.
• History of asthma or chronic obstructive pulmonary disease (including childhood), clinically significant food allergies or anaphylaxis, as deemed by PI or designee.
• Current or chronic history of liver disease or known hepatic or biliary abnormalities (with the exception of asymptomatic gallstones).
• Seizure (excluding simple febrile seizure), epilepsy, severe head injury, multiple sclerosis, or other known neurological conditions which the PI or designee considers to be clinically significant.

NOTE: Other protocol defined Inclusion/Exclusion criteria may apply

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Basic Science
• Allocation: Randomized
• Interventional Model: Crossover Assignment
• Masking: None (Open Label)

Number of Arms

3

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Treatment A; Participants will receive 4 X 25 mg tablets of casdatifan.	Drug: Casdatifan; Administered as specified in the treatment arm; Other Names: AB521
Experimental: Treatment B; Participants will receive 1 X 100 mg tablets of casdatifan.	Drug: Casdatifan; Administered as specified in the treatment arm; Other Names: AB521
Experimental: Treatment C; Participants will receive 4 X 25 mg tablets of casdatifan under fed conditions.	Drug: Casdatifan; Administered as specified in the treatment arm; Other Names: AB521

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
Maximum observed concentration for casdatifan	Up to 168 hours post each dose
Area under the concentration-time curve for casdatifan	Up to 168 hours post each dose

Secondary Outcome Measures

Outcome Measure	Time Frame
Time to reach Cmax (Tmax) for casdatifan	Up to 168 hours post each dose
Lag time (Tlag) for casdatifan	Up to 168 hours post each dose
Apparent first-order terminal elimination rate constant (Kel) for casdatifan	Up to 168 hours post each dose
Percent of AUC0-inf extrapolated for casdatifan	Up to 168 hours post each dose
Apparent first-order terminal elimination half-life (t½) for casdatifan	Up to 168 hours post each dose
Apparent total clearance after extravascular (oral) administration (CL/F) for casdatifan	Up to 168 hours post each dose
Apparent total clearance after extravascular (oral) administration (Vz/F) for casdatifan	Up to 168 hours post each dose
Number of participants experiencing Adverse Events (AEs)	Up to 43 days

Collaborators and Investigators

• Sponsor: Arcus Biosciences, Inc.
• Collaborators: Taiho Pharmaceutical Co., Ltd.
• Investigators: Study Director: Medical Director, Arcus Biosciences

Study record dates

Study Major Dates

• Study Start (Estimated): June 1, 2026
• Primary Completion (Estimated): July 1, 2026
• Study Completion (Estimated): July 1, 2026

Study Registration Dates

• First Submitted: June 8, 2026
• First Submitted That Met QC Criteria: June 8, 2026
• First Posted (Actual): June 11, 2026

Study Record Updates

• Last Update Posted (Actual): June 12, 2026
• Last Update Submitted That Met QC Criteria: June 11, 2026
• Last Verified: May 1, 2026

More Information

Terms related to this study

• Keywords: Pharmacokinetics; AB521; HIF-2α; Casdatifan
• Other Study ID Numbers: ARC-30

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: YES

IPD Plan Description

Arcus will provide access to individual de-identified participant data and related study documents (e.g., protocol, Statistical Analysis Plan [SAP], Clinical Study Report [CSR]) upon request from qualified researchers, and subject to certain criteria, conditions, and exceptions.

For more information, please visit our website.

• IPD Sharing Supporting Information Type: STUDY_PROTOCOL; SAP; CSR

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: Yes
• Studies a U.S. FDA-regulated device product: No