Casdatifan is an investigational new drug that is being evaluated by Arcus Biosciences and AstraZeneca for the treatment of renal cell carcinoma. It is an inhibitor of endothelial PAS domain-containing protein 1 (HIF‑2α).

Pharmacology

Casdatifan is allosteric HIF‑2α inhibitor with low-nanomolar potency in cell-based reporter assays.

Clinical trials

Casdatifan in combination with cabozantinib (a tyrosine-kinase inhibitor) is currently in phase 3 clinical trials for the treatment of advanced clear cell renal cell carcinoma.

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