ARTS-876

ARTS-876 is an orally bioavailable, potent, and highly selective small molecule inhibitor of Hypoxia-Inducible Factor 2-alpha (HIF-2α). It was originally developed by Anrui Biopharma (Guangzhou) and later licensed to Allist Pharmaceuticals for clinical development. HIF-2α is a critical transcription factor that drives the expression of genes involved in angiogenesis, cell proliferation, and survival, particularly in clear cell renal cell carcinoma (ccRCC) where the von Hippel-Lindau (VHL) tumor suppressor is frequently inactivated. By binding to the PAS-B domain of HIF-2α, ARTS-876 prevents its heterodimerization with HIF-1β, thereby inhibiting the transcriptional activity of the HIF-2 complex. It is currently being evaluated in Phase 1 clinical trials for the treatment of advanced solid tumors, with a primary focus on renal cell carcinoma.