Casdatifan

Casdatifan (AB521) is a small molecule inhibitor of the oxygen-sensing transcription factor HIF-2⍺ that has demonstrated potent antitumor activity in xenograft models of renal cell cancer (RCC). Under normal physiological conditions, HIF-2⍺ is involved in sensing oxygen availability in multiple organs. In certain tumors, particularly clear cell RCC (ccRCC), HIF-2⍺ activity is highly dysregulated as a result of genetic abnormalities in the VHL pathway. This creates a situation of pseudohypoxia and the abnormal increase in HIF-2⍺-mediated expression of a wide array of proteins involved in cancer cell proliferation and survival, treatment resistance and angiogenesis.
Chemenu has been working to develop more compounds for drug discovery. Here are the building blocks we can provide.