BPI-452080 is a selective HIF-2α inhibitor that prevents the dimerization of HIF-2α with HIF-1β, leading to lower transcription of hypoxia-responsive genes like GLUT1, CCND1, and CXCR4, and reducing VEGFA secretion in RCC preclinical models. This evidence concerns the gene EPAS1 and renal cell carcinoma.