Belzutifan, sold under the brand name Welireg, is an anti-cancer medication used for the treatment of von Hippel–Lindau disease-associated renal cell carcinoma.

Routes of administration By mouth

Pregnancy category AU: D

It is an hypoxia-inducible factor-2 alpha (HIF-2α) inhibitor.

Belzutifan has the capacity to reduce serum erythropoietin verified its clinically useful for the treatment of malignancies linked to von Hippel-Lindau (VHL), such as renal cell carcinoma (RCC) with clear cell histology (ccRCC), pancreatic lesions, neuroendocrine tumors, and CNS hemangioblastomas or pancreatic neuroendocrine tumors (pNET) but do not require immediate surgery. 

Belzutifan obtained a disease control rate of 80% in pretreated ccRCC during a phase I trial.

The most common side effects include decreased hemoglobin, anemia, fatigue, increased creatinine, headache, dizziness, increased glucose, and nausea.

Belzutifan is the first hypoxia-inducible factor-2 alpha inhibitor therapy approved.

Considers it to be a first-in-class medication.

Belzutifan is indicated for treatment of 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.

Belzutifan was well tolerated: Anemia, tiredness, headaches, vertigo, nausea, and dyspnea were the most typical side effects. 

All participants in the phase II trial reported a hemoglobin reduction of at least 1.9 g/dL; however, only a small number of individuals needed transfusions or erythropoietin-stimulating medications. 

Because of the downstream effect of HIF-2 inhibition, anemia was a predicted negative outcome of inhibiting the EPO gene. 

The majority of negative outcomes were grade 1 or 2, while 33% of patients experienced grade 3 to 5 occurrences. 

In 43% of patients treatment was discontinued, and in 15% of patients, the dosage was adjusted. 2% of patients stopped receiving therapy: as a result of fatigue, increased creatinine, headache, dizziness, elevated hyperglycemia, and nausea.

The most frequent side effects, including laboratory abnormalities, recorded in 20% or less of patients. 

Belzutifan has the potential to harm fetuses and embryos during pregnancy and can render some hormonal contraceptives ineffective.

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