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Casdatifan · AB-521

Small molecule · Inhibitor of HIF-2alpha (EPAS1) · developed by Arcus Biosciences

Phase 1/2 Most advanced trial
1 Registered trials

What is Casdatifan?

Casdatifan is an orally bioavailable allosteric inhibitor of HIF-2alpha that prevents its heterodimerization with HIF-1beta and DNA binding, reducing transcription of HIF-2alpha target genes that promote tumor cell growth and survival. It is studied in advanced renal cell carcinoma.

Summary written with AI from the sources listed at the end of this page.

At a glance

Also known as
AB-521
Drug type
Small molecule
Targets
HIF-2alpha (EPAS1)
Mechanism
Inhibitor of HIF-2alpha (EPAS1)
Pathways
HIF-2alpha transcriptional activity, tumor cell proliferation and survival
Therapy area
Oncology
Developer
Arcus Biosciences, Inc.
In trials of
BMY
FDA status
Investigational, not approved in the US. Most advanced trial: Phase 1/2
UNII
DP73UWL6LE

🧪 Clinical trials

TrialPhaseConditionStatusSponsor
NCT07293351 Phase 1/2 Advanced Renal Cell Carcinoma (RCC) Recruiting BMY

Trials of the companies BioRadar tracks, from ClinicalTrials.gov, most advanced phase first.

Conditions studied

Advanced Renal Cell Carcinoma (RCC)

Other drugs acting on EPAS1

Belzutifan FDA approved Imdatifan Phase 1/2 Zifcasiran Phase 1

Sources

Updated Oct 3, 2026.

Data: FDA (Drugs@FDA, Purple Book, DailyMed), NIH (NCI Thesaurus, GSRS, RxNorm), ClinicalTrials.gov • Informational purposes only, not medical or investment advice. • All drugs A–Z

This data is for informational purposes only, not investment advice. BioRadar does not provide buy/sell recommendations. Past performance does not guarantee future results. Always do your own due diligence.