Casdatifan has shown promising clinical activity in the ARC-20 ccRCC platform study, both as monotherapy and in combination with the VEGFR tyrosine kinase inhibitor (TKI) cabozantinib. Currently, casdatifan is being evaluated in a Phase 3 trial in combination with cabozantinib (NCT07011719) in patients with advanced ccRCC.

7 days ago

Journal

EPAS1 (Endothelial PAS domain protein 1)

Cabometyx (cabozantinib tablet) • casdatifan (AB521)

Discovery of Casdatifan, Part I: Design and Characterization of Tetrahydroquinoline Inhibitors of Hypoxia-Inducible Factor-2α. (PubMed, J Med Chem)

These features translated into improved biochemical and cellular activity, including inhibition of hypoxia-regulated gene expression. Insights from this campaign ultimately informed the discovery of casdatifan, a clinical-stage HIF-2α inhibitor, underscoring the translational potential of this novel chemotype.

1 month ago

Journal

EPAS1 (Endothelial PAS domain protein 1)

casdatifan (AB521)

3ms

Pre-NEOSHIFT-RCC: Neoadjuvant HIF-Inhibitor Immunotherapy in RCC (clinicaltrials.gov)

P2, N=32, Recruiting, Dana-Farber Cancer Institute | Not yet recruiting --> Recruiting | Initiation date: Jul 2026 --> Mar 2026

3 months ago

Enrollment open • Trial initiation date

Yutuo (zimberelimab) • casdatifan (AB521)

3ms

ARC-20: A Phase 1 Study of AB521 Monotherapy and Combination Therapies in Renal Cell Carcinoma and Other Solid Tumors (clinicaltrials.gov)

P1, N=362, Recruiting, Arcus Biosciences, Inc. | Trial completion date: Jul 2027 --> Mar 2029 | Trial primary completion date: Jul 2027 --> Mar 2029

3 months ago

Trial completion date • Trial primary completion date

Yervoy (ipilimumab) • Cabometyx (cabozantinib tablet) • Yutuo (zimberelimab) • casdatifan (AB521)

4ms

PEAK-1: Randomized Phase 3 Trial of Casdatifan and Cabozantinib Versus Placebo and Cabozantinib in Patients With Advanced Clear Cell Renal Cell Carcinoma (2024-515023-11-00)

P2/3, N=308, Recruiting, Arcus Biosciences Inc.

4 months ago

New P2/3 trial

Cabometyx (cabozantinib tablet) • casdatifan (AB521)

4ms

Pre-NEOSHIFT-RCC: Neoadjuvant HIF-Inhibitor Immunotherapy in RCC (clinicaltrials.gov)

P2, N=32, Not yet recruiting, Dana-Farber Cancer Institute

4 months ago

New P2 trial

Yutuo (zimberelimab) • casdatifan (AB521)

7ms

eVOLVE-RCC02: A Study to Investigate the Efficacy and Safety of Volrustomig ± Casdatifan vs Nivolumab + Ipilimumab as 1L Treatment for Advanced ccRCC (clinicaltrials.gov)

P3, N=1116, Active, not recruiting, AstraZeneca | Recruiting --> Active, not recruiting

7 months ago

Enrollment closed

Opdivo (nivolumab) • Yervoy (ipilimumab) • volrustomig (MEDI5752) • casdatifan (AB521)

7ms

Drug-Drug Interaction Study of Casdatifan in Healthy Adult Participants (ARC-29) (clinicaltrials.gov)

P1, N=14, Completed, Arcus Biosciences, Inc. | Active, not recruiting --> Completed

7 months ago

Trial completion

itraconazole • casdatifan (AB521)

9ms

Study of Casdatifan and Cabozantinib Versus Placebo and Cabozantinib in Patients With Advanced Clear Cell Renal Cell Carcinoma (clinicaltrials.gov)

P3, N=720, Recruiting, Arcus Biosciences, Inc. | Not yet recruiting --> Recruiting

9 months ago

Enrollment open

Cabometyx (cabozantinib tablet) • casdatifan (AB521)

9ms

Drug-Drug Interaction Study of Casdatifan in Healthy Adult Participants (ARC-29) (clinicaltrials.gov)

P1, N=14, Active, not recruiting, Arcus Biosciences, Inc. | Recruiting --> Active, not recruiting

9 months ago

Enrollment closed

itraconazole • casdatifan (AB521)

10ms

eVOLVE-RCC02: A Study to Investigate the Efficacy and Safety of Volrustomig ± Casdatifan vs Nivolumab + Ipilimumab as 1L Treatment for Advanced ccRCC (clinicaltrials.gov)

P3, N=1116, Recruiting, AstraZeneca | Not yet recruiting --> Recruiting

10 months ago

Enrollment open

Opdivo (nivolumab) • Yervoy (ipilimumab) • volrustomig (MEDI5752) • casdatifan (AB521)