Belzutifan is an oral small molecule hypoxia inducible factor-2 alpha (HIF-2 alpha) inhibitor that targets and inhibits the activity of HIF-2 alpha, blocking its interaction with HIF-1 β and reducing the transcriptional expression of downstream angiogenic, cell proliferation, and tumor growth related factors.

1、 Drug name

1. Common name: Belzutifan;

2. Product Name: WELIREG ™。

2、 Indications

Betamethasone is a hypoxia inducible factor inhibitor suitable for the treatment of adult von Hippel Lindau (VHL) disease-related renal cell carcinoma (RCC), central nervous system (CNS) hemangioblastoma, or pancreatic neuroendocrine tumor (pNET) in patients who do not require immediate surgery.

3、 Specifications and characteristics

1. Specification: 40mg

2. Appearance: Tablets

4、 Main components

Active ingredient: Beizu Tifan

5、 Usage and dosage

1. Recommended dosage: 120mg orally, once daily, before or after meals.

2. Medication method: Swallow the whole tablet, do not chew, crush or cut.

3. Omission treatment: If remembered on the same day, take the medication as scheduled the next day.

4. Vomiting treatment: Vomiting after taking medication does not require supplementation, and should be continued at the original dose the next day.

6、 Dose adjustment

1. Anemia: Suspend administration when hemoglobin<9g/dL, reduce to 80mg or 40mg once daily after recovery to ≥ 9g/dL, or permanently discontinue medication.

2. Hypoxia: When the resting blood oxygen saturation is less than 88% or emergency intervention is needed, the medication should be suspended, and reduced or permanently discontinued after recovery.

3. Other adverse reactions: For toxicity reactions of grade ≥ 3, medication should be suspended and reduced by 40mg after remission to grade ≤ 2; for grade 4 or recurrent grade 3 toxicity, medication should be permanently discontinued.

7、 Medication precautions

1. Pregnancy risk: Before treatment, it is necessary to confirm the pregnancy status. Women of childbearing age should use non hormonal contraceptive measures (as they may reduce the effectiveness of hormonal contraceptives), and avoid pregnancy during treatment and within one week after discontinuation.

2. Anemia monitoring: Regular check of hemoglobin before and during treatment, severe anemia requires blood transfusion.

3. Blood oxygen monitoring: Monitor blood oxygen saturation before and during treatment, and seek medical attention promptly if symptoms such as difficulty breathing occur.

8、 Medication for special populations

1. Pregnant women: Prohibited, may cause fetal malformation.

2. Breastfeeding period: Avoid breastfeeding during treatment and within one week after the last dose.

3. Liver and kidney dysfunction: mild to moderate liver injury or complete renal dysfunction requiring dose adjustment; Prohibited for severe liver injury.

9、 Adverse reactions

1. Common (≥ 25%): Anemia (90%), fatigue (64%), headache (39%), dizziness (38%), nausea (31%), elevated creatinine (64%), elevated blood sugar (34%).

2. Serious reactions: anemia (7% grade 3), hypoxia (1.6%), allergic reactions, retinal detachment, etc.

10、 Contraindications

There are no clear contraindications.

11、 Drug interactions

1. UGT2B17 or CYP2C19 inhibitors: may increase exposure to bevacizumab, and anemia and hypoxia symptoms need to be monitored and reduced.

2. Hormonal contraceptive pills: may reduce contraceptive effectiveness, it is recommended to switch to non hormonal contraception.

12、 Storage method

1. Storage temperature: 20-25 ° C (short-term 15-30 ° C allowed).

2. Store in original packaging, the bottle contains desiccants that are not edible.

Belzutifaninformation