Medical Uses
Welireg (belzutifan) is a first-in-class, oral HIF-2α (hypoxia-inducible factor-2 alpha) inhibitor from Merck. It is approved for adults with Von Hippel-Lindau (VHL) disease who require therapy for associated renal cell carcinoma (RCC), central nervous system (CNS) hemangioblastomas, or pancreatic neuroendocrine tumors (pNET) not requiring immediate surgery.
Welireg is also approved for adults with advanced RCC with a clear cell component, following a PD-1/PD-L1 inhibitor and a VEGF tyrosine kinase inhibitor (VEGF-TKI), and for adults and pediatric patients 12 years and older with locally advanced, unresectable, or metastatic pheochromocytoma or paraganglioma (PPGL).
Certain tumors accumulate abnormally high levels of HIF-2α, which drives angiogenesis and tumor growth. Belzutifan binds HIF-2α and blocks this pathway, slowing tumor progression.
