BPI-452080

BPI-452080 is an orally available, highly selective small molecule inhibitor of hypoxia-inducible factor 2 alpha (HIF-2α). It is designed to prevent the dimerization of HIF-2α with HIF-1β, thereby inhibiting the transcriptional activation of hypoxia-responsive genes involved in tumor growth and survival. The drug is being developed by Betta Pharmaceuticals for the treatment of advanced solid tumors, including clear cell renal cell carcinoma (ccRCC), von Hippel-Lindau (VHL) disease-associated tumors, and other solid malignancies. Preclinical studies have demonstrated potent in vitro and in vivo antitumor activity as well as favorable pharmacokinetic properties and safety profiles. As of 2023–2024, BPI-452080 has entered Phase 1 clinical trials in China for these indications[1][2][3][4][5][7][8].