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Belzutifan is an oral small molecule hypoxia-inducible factor-2α (HIF-2α) inhibitor that targets and inhibits the activity of HIF-2α and blocks its interaction with HIF-1β, thereby reducing the transcriptional expression of downstream genes related to angiogenesis, cell proliferation and tumor growth.
1. Generic name: Belzutifan;
2. Trade name: WELIREG™.
Bestivan is a hypoxia-inducible factor inhibitor, suitable for the treatment of adult patients with von Hippel-Lindau (VHL) disease-related renal cell carcinoma (RCC), central nervous system (CNS) hemangioblastoma, or pancreatic neuroendocrine tumors (pNET) who do not require immediate surgery.
1. Specifications: 40mg
2. Properties: Tablets
Active ingredients:Bestivan
1. Recommended dosage: 120 mg orally, once a day, before or after a meal.
2. How to take the medicine: Swallow the tablet whole. Do not chew, crush or cut.
3. Treatment of missed doses: If you remember to take a missed dose on the same day, you can take it again at the original time the next day.
4. Treatment of vomiting: If you vomit after taking the medicine, there is no need to take a supplement. You can continue taking the medicine at the original dose the next day.
1. Anemia : Suspend the administration when the hemoglobin is <9g/dL. After recovery to ≥9g/dL, reduce the dose to 80mg or 40mg once a day, or permanently discontinue the drug.
2. Hypoxia : Suspension of medication when resting blood oxygen saturation is <88% or emergency intervention is required, and reduction or permanent discontinuation of medication after recovery.
3. Other adverse reactions : For grade ≥ 3 toxic reactions, the drug needs to be suspended, and after remission to ≤ grade 2, the dose needs to be reduced by 40 mg; for grade 4 or recurrent grade 3 toxicity, the drug needs to be permanently discontinued.
1. Pregnancy risk : Pregnancy status needs to be confirmed before treatment. Women of childbearing age need to use non-hormonal contraceptive measures (because they may reduce the effect of hormonal contraceptives), and avoid pregnancy during treatment and within 1 week after stopping the drug.
2. Anemia monitoring : Check hemoglobin regularly before and during treatment. Severe anemia requires blood transfusion.
3. Blood oxygen monitoring : Monitor blood oxygen saturation before and during treatment. If symptoms such as difficulty breathing occur, seek medical attention promptly.
1. Pregnant women : Contraindicated, it may cause fetal malformation.
2. Lactation : Avoid breastfeeding during treatment and within 1 week after the last dose.
3. Liver and renal insufficiency : No dose adjustment is required for mild to moderate liver damage or renal insufficiency; it is contraindicated for severe liver damage.
1. Common (≥25%): Anemia (90%), fatigue (64%), headache (39%), dizziness (38%), nausea (31%), increased creatinine (64%), increased blood sugar (34%).
2. Severe reactions: Anemia (7% grade 3), hypoxia (1.6%), allergic reaction, retinal detachment, etc.
There are no clear contraindications.
1. UGT2B17 or CYP2C19 inhibitor : It may increase the exposure of besetifan. It is necessary to monitor the symptoms of anemia and hypoxia and reduce the dose.
2. Hormonal contraceptive : It may reduce the contraceptive effect. It is recommended to use non-hormonal contraceptive.
1. Storage temperature: 20-25°C (short-term 15-30°C allowed).
2. Store in the original packaging. The bottle contains desiccant and is not edible.