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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.

Arcus is initially evaluating the safety, tolerability and efficacy of casdatifan, as a single agent and in combination with an anti-VEGF tyrosine kinase inhibitor (TKI) in ccRCC tumors.