BPI-452080 is a selective small-molecule HIF-2α inhibitor that disrupts HIF-2α heterodimerization with HIF-1β, leading to decreased transcription of downstream hypoxia-responsive genes (e.g., GLUT1, CCND1, and CXCR4) and VEGFA secretion in pre-clinical RCC models [61]. The gene discussed is EPAS1; the disease is renal cell carcinoma.