casdatifan

Casdatifan is an orally bioavailable, highly specific small molecule inhibitor of hypoxia-inducible factor 2 alpha (HIF-2α). It allosterically binds to a hydrophobic pocket on HIF-2α, preventing its heterodimerization with HIF-1β and subsequent binding to the hypoxia response element (HRE) on DNA. This action blocks the transcription of genes that promote tumor cell survival, proliferation, angiogenesis, and immune evasion in hypoxic tumor microenvironments. Casdatifan is under clinical development primarily for metastatic clear cell renal cell carcinoma (ccRCC), a cancer type strongly associated with dysregulation of HIF pathways. The drug has demonstrated promising clinical activity and tolerability in early-phase trials involving heavily pretreated ccRCC patients[1][2][3][4][5][7].

Other names

casdatifan [INN]