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Belumosudil is a kinase inhibitor that regulates immune response and fibrosis signaling pathways by inhibiting the activities of ROCK2 and ROCK1, and is used to treat chronic graft-versus-host disease (chronicGVHD).
1. Generic name: Besudil
2. Trade name: REZUROCK
3. English name: Belumosudil
This product is suitable for the treatment of chronic graft-versus-host disease (chronic GVHD) in adults and pediatric patients 12 years old and above, and these patients have previously received at least two systemic treatments but failed.
This product is a 200 mg tablet. It is a film-coated special-shaped tablet.
1. Active ingredient: Besudil mesylate (each tablet contains 200 mg of Besudil, equivalent to 242.5 mg of Besudil mesylate).
2. Excipients: The tablet core contains microcrystalline cellulose, hypromellose, croscarmellose sodium, colloidal silicon dioxide and magnesium stearate. The film coat contains polyvinyl alcohol, polyethylene glycol, talc, titanium dioxide and iron oxide yellow.
1. Recommended dose: 200 mg, once a day, orally with food.
2. How to take: Swallow the tablet whole and do not cut, crush or chew it. Take it at about the same time every day.
3. Treatment duration: Medication should be continued until the progression of chronic GVHD requires new systemic treatment.
1. Adverse reaction dose adjustment: For grade 3 liver toxicity (AST or ALT increased to 5-20 times the upper limit of normal) or grade 2 bilirubin increase (1.5-3 times the upper limit of normal), administration should be suspended and resumed at the original dose after recovery to grade 0-1. For grade 4 hepatotoxicity (AST or ALT more than 20 times the upper limit of normal) or grade 3 and above bilirubin elevation (more than 3 times the upper limit of normal), the drug should be permanently discontinued. For other grade 3 non-hematological adverse reactions, suspend administration until recovery to grade 0-1 and then resume treatment; for grade 4, discontinue treatment permanently.
2. Drug interaction dose adjustment: When used in combination with strong CYP3A inducers or proton pump inhibitors, the dose of this product should be increased to 200 mg twice a day.
1. Medication time: It must be taken with meals to increase drug absorption.
2. Missed dose: If you miss a dose, you should take it as soon as you remember on the same day, and take the medicine at the normal time the next day. Extra doses should not be taken to make up for a missed dose.
3. Vomiting: The instructions do not clearly mention the treatment after vomiting. It is recommended to consult a doctor.
1. Pregnant women: Based on animal data and mechanism of action, this product can cause fetal harm and is contraindicated in pregnant women. Women of childbearing potential need to use effective contraceptive measures during treatment and for at least one week after the last dose. Pregnancy status should be verified before starting treatment.
2. Breastfeeding women: It is recommended that women stop breastfeeding during treatment and at least one week after the last dose.
3. Men and women of childbearing age: It may damage male and female fertility, but the effects are considered reversible. Men and their female partners of childbearing potential should use effective contraception during treatment and for at least one week after the last dose.
4. Children: The safety and effectiveness in pediatric patients 12 years old and above have been established. Safety and effectiveness in pediatric patients under 12 years of age have not been established.
5. Elderly patients: No clinically significant differences in safety or efficacy were observed compared with younger patients.
6. Hepatic/renal insufficiency: Studies have not yet been conducted in patients with severe hepatic or renal impairment. Risks and benefits should be weighed when initiating treatment in such patients.
1. The most common adverse reactions (≥20%) include: infection, fatigue, nausea, diarrhea, dyspnea, cough, edema, bleeding, abdominal pain, musculoskeletal pain, headache, decreased blood phosphate, increased gamma-glutamyl transferase, lymphopenia and hypertension.
2. Adverse reactions that may lead to permanent discontinuation: nausea (>3% of patients).
3. Adverse reactions that may lead to dose interruption: infection (11%), diarrhea (4%).
There are currently no clear contraindications.
1. Strong CYP3A inducers: combined use will reduce the exposure of besudil and may reduce the efficacy. The dose of this product needs to be increased.
2. Proton pump inhibitors: Combined use will significantly reduce the exposure of besudil and may reduce the efficacy. The dose of this product needs to be increased.
3. This product is an inhibitor of CYP3A, CYP2C8, CYP2D6 and UGT1A9, and may inhibit certain transporters (such as BCRP, P-gp, OATP1B1). Caution should be used when combined with drugs with narrow therapeutic windows metabolized by these enzymes.
Storage at 20℃ to 25℃ (68℉ to 77℉); short-distance transportation allowed between 15℃ to 30℃ (59℉ to 86℉). It needs to be stored in the original bottle to prevent moisture. The desiccant in the bottle should be retained. The bottle cap must be tightly closed after each opening.