Chemistry:Casdatifan
From HandWiki
Casdatifan is an investigational new drug that is being evaluated by Arcus Biosciences and AstraZeneca for the treatment of renal cell carcinoma.[1] It is an inhibitor of endothelial PAS domain-containing protein 1 (HIF‑2α).[2][3][4]
Pharmacology
Casdatifan is allosteric HIF‑2α inhibitor with low-nanomolar potency in cell-based reporter assays.[3]
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.[4][5]
References
- ↑ "Casdatifan - Arcus Biosciences". AdisInsight. Springer Nature Switzerland AG. https://adisinsight.springer.com/drugs/800063239.
- ↑ "Discovery of Casdatifan, Part I: Design and Characterization of Tetrahydroquinoline Inhibitors of Hypoxia-Inducible Factor-2α". Journal of Medicinal Chemistry 69 (12): 14921–14951. June 2026. doi:10.1021/acs.jmedchem.5c03647. PMID 42053090.
- ↑ 3.0 3.1 "Discovery of Casdatifan, Part II: A Potent and Orally Bioavailable Inhibitor of Hypoxia Inducible Factor-2α". Journal of Medicinal Chemistry 69 (12): 14952–14988. June 2026. doi:10.1021/acs.jmedchem.5c03724. PMID 42246926.
- ↑ 4.0 4.1 "Hypoxia Inducible Factor-2α (HIF-2α) Pathway Inhibitors". Journal of Kidney Cancer and VHL 12 (3): 1–15. 2025. doi:10.15586/jkc.v12i3.413. PMID 40620865.
- ↑ Clinical trial number NCT07011719 for "Study of Casdatifan and Cabozantinib Versus Placebo and Cabozantinib in Patients With Advanced Clear Cell Renal Cell Carcinoma" at ClinicalTrials.gov
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