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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 (Belzutifan)
2. Trade name: WELIREG™
For the treatment of adult patients with von Hippel-Lindau (VHL) disease who require treatment of associated renal cell carcinoma (RCC), central nervous system (CNS) hemangioblastoma, or pancreatic neuroendocrine tumors (pNET) and who do not require immediate surgery.
Bestivan tablets are 40 mg oval film-coated tablets.
1. Each tablet contains 40 mg of besetifan.
2. Excipients include: Crosscarmellose sodium, hypromellose acetate succinate, magnesium stearate, mannitol, microcrystalline cellulose, and silicon dioxide.
3. Film coating contains: FD&C blue No. 2 aluminum lake, polyethylene glycol, polyvinyl alcohol, talc, titanium dioxide.
1. The recommended dose is 120mg taken orally once a day, which can be taken with food or on an empty stomach.
2. The tablet should be swallowed whole and should not be chewed, crushed or broken.
3. If you miss a dose, you can take it as soon as possible on the same day, and take the medicine at the original planned time the next day. No additional dose is required.
4. If you vomit after taking the medicine, there is no need to take a supplement, and you can take the medicine the next day as originally planned.
Adjust the dose according to the severity of adverse reactions:
1. Reduce the dose to 80 mg once a day for the first time, reduce it to 40 mg once a day for the second time, and permanently discontinue the drug for the third time.
2. Anemia (hemoglobin <9g/dL or blood transfusion required): Suspend medication until hemoglobin ≥9g/dL. Reduce dose or discontinue medication when recovery occurs.
3. Hypoxia (blood oxygen saturation <88% during exercise or <88% at rest): Suspend the medication according to the severity, and reduce the dose or discontinue the medication after recovery.
4. Other grade 3 adverse reactions: suspend until recovery to ≤ grade 2 and then reduce the dose; grade 4 adverse reactions require permanent discontinuation.
1. Medication time: Take the medication at a fixed time every day, not affected by food.
2. Swallowing requirements: Swallow the whole tablet without damaging the tablet structure.
3. Treatment of missed doses: Take the dose as soon as possible within the same day, and take the medicine as originally planned the next day.
4. Treatment of vomiting: There is no need to take additional doses after vomiting. Take the medicine as originally planned the next day.
5. Hemoglobin and blood oxygen saturation need to be monitored regularly before and during treatment.
6. Avoid combined use with UGT2B17 or CYP2C19 inhibitors, which may increase the risk of adverse reactions.
1. Pregnant women: It has embryo-fetal toxicity and needs to use effective non-hormonal contraceptive measures.
2. Breastfeeding women: Breastfeeding is prohibited during treatment and within 1 week after the last dose.
3. Children: Safety and effectiveness have not been established.
4. Elderly people: The data is limited and should be used with caution.
5. Renal insufficiency: No dose adjustment is required for mild to moderate patients, and there is insufficient data for severe patients.
6. Hepatic insufficiency: No dose adjustment is required for mild cases, and there is insufficient data for moderate to severe patients.
7. Slow metabolizers of UGT2B17 and CYP2C19: Exposure increases and adverse reactions need to be closely monitored.
1. Common adverse reactions (incidence ≥25%) include: Decreased hemoglobin, anemia, fatigue, increased creatinine, headache, dizziness, increased blood sugar, and nausea.
2. Serious adverse reactions include: Severe anemia (requiring blood transfusion), severe hypoxia (requiring oxygen or hospitalization), allergic reaction, retinal detachment, and central retinal vein occlusion.
No clear contraindications.
1. UGT2B17 or CYP2C19 inhibitors: May increase the exposure of besetifan, so symptoms of anemia and hypoxia need to be monitored and the dosage adjusted.
2. Sensitive CYP3A4 substrates: Bestifan may reduce its concentration, resulting in a decrease in efficacy, so combined use should be avoided or the dosage of the substrate should be adjusted.
3. Hormonal contraceptives: May be ineffective or cause breakthrough bleeding, so non-hormonal contraceptive measures need to be used.
1. Store at 20°C to 25°C (68°F to 77°F). Short-term storage is allowed at 15°C to 30°C (59°F to 86°F).
2. The medicine bottle contains desiccant and is not edible.