Belzutifan(Welireg)

Belzutifan is a prescription drug that received its first marketing approval from the U.S. Food and Drug Administration (FDA) on August 13, 2021. It targets hypoxia-inducible factor-2α (HIF-2α), and must be used strictly in accordance with medical advice.

Target

Hypoxia-Inducible Factor-2α (HIF-2α)

Mechanism of Action

Belzutifan is a hypoxia-inducible factor 2α (HIF-2α) inhibitor. It binds to HIF-2α and, under hypoxic conditions or in the presence of impaired von Hippel-Lindau (VHL) protein function, blocks the interaction between HIF-2α and HIF-1β, thereby reducing the transcription and expression of HIF-2α target genes.

Dosage and Administration

Route and Frequency of Administration: Oral, once daily, 120 mg per dose.

Dosage adjustments of Belzutifan should be made based on the patient’s actual condition. For specific circumstances, please consult a doctor and strictly follow medical advice.

Recommended Reading: Dosage and Administration of Belzutifan

Adverse Reactions

Major Risks and Warnings: Anemia, hypoxia, embryo-fetal toxicity.

Common Adverse Reactions: Laboratory abnormalities, fatigue, musculoskeletal pain, etc.

Severe Adverse Reactions: Anemia, hypoxia, anaphylactic shock reactions, etc.

Reference Article: Adverse Reactions of Belzutifan

Use in Special Populations

Pregnancy

Belzutifan may cause harm to the fetus when administered to pregnant women. The pregnancy status of women of childbearing potential must be verified prior to initiating treatment with Belzutifan.

Lactation

Due to the potential risk of severe adverse reactions in breastfed infants, it is recommended that women refrain from breastfeeding during treatment with Belzutifan and for 1 week after the last dose.

General Precautions

1.Instruct patients to read the U.S. Food and Drug Administration (FDA)-approved medication guide.

2.Advise patients to take Belzutifan at the same time every day (once daily). Inform patients that Belzutifan may be taken with or without food. The tablets should be swallowed whole.

3.Inform patients that Belzutifan may cause severe anemia, which may require blood transfusion treatment, and therefore red blood cell levels will be monitored regularly during treatment. Advise patients to contact their healthcare provider if they experience any symptoms suggestive of anemia.

FDA，2021.08