PT-2385

PT-2385 is an orally active, first-in-class small molecule inhibitor of hypoxia-inducible factor 2 alpha (HIF-2α). It acts by allosterically binding to HIF-2α, preventing its heterodimerization with HIF-1β and subsequent DNA binding. This inhibition disrupts the transcriptional activity of HIF-2α, which regulates genes involved in adaptation to hypoxia, including those promoting angiogenesis and metabolic adaptation. PT-2385 has demonstrated potent antineoplastic activity in preclinical models and has been investigated primarily for clear cell renal cell carcinoma (ccRCC), particularly in patients with Von Hippel-Lindau disease-associated tumors. The drug was developed as a targeted therapy for cancers driven by aberrant activation of the hypoxia pathway[1][3][4][5].

Other names

HIF-2alpha inhibitor PT2385HIF2alpha inhibitor PT2385HIF 2alpha inhibitor PT2385