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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: Belumosudil (Belumosudil)
2. Trade name: REZUROCK™
It is used to treat chronic graft-versus-host disease (chronic GVHD) in adults and children aged 12 years and above, and it needs to be used after the failure of at least two systemic treatments.
200mg tablet : film-coated oval tablet.
Active ingredient: Besudil mesylate (chemical name: 2-{3-[4-(1H-indazol-5-ylamino)-2-quinazolinyl]phenoxy}-N-(propan-2-yl)acetamide methanesulfonate).
1. Standard dose : 200mg once a day, take with food, swallow the tablet whole, do not cut, crush or chew.
2. Treatment course : Continue medication until chronic GVHD progresses and requires new systemic treatment.
3. Treatment of missed doses : There is no need to take a missed dose on the same day. Next time, take the medicine according to the original plan.
1. Hepatotoxicity : Suspend administration when grade 3 AST/ALT elevation or grade 2 bilirubin elevation occurs, and continue with the original dose after recovery; permanently discontinue medication when grade 4 AST/ALT or grade ≥3 bilirubin elevation occurs.
2. Other adverse reactions : for grade 3, suspend until restored to grade 0-1 and continue; for grade 4, discontinue permanently.
3. Drug interactions : When used in combination with strong CYP3A inducers or proton pump inhibitors, the dose is increased to 200 mg twice daily.
1. Dietary requirements : must be taken with food and avoid grapefruit and its products.
2. How to take the medicine : Swallow the whole tablet without damaging the tablet structure.
3. Monitoring requirements : Test liver function (bilirubin, AST, ALT) at least once a month.
1. Pregnancy/breastfeeding : It may cause fetal malformation. Contraception is required during treatment and within 1 week of stopping the drug; it is contraindicated during breastfeeding.
2. Children : safe and effective for 12 years old and above, but insufficient data for children under 12 years old.
3. Liver and renal insufficiency : People with severe liver/renal insufficiency need to weigh the risks and benefits.
Common (≥20%) include: infection, fatigue, nausea, diarrhea, dyspnea, cough, edema, bleeding, abdominal pain, musculoskeletal pain, headache, hypophosphatemia, lymphopenia, and hypertension.
There are no absolute contraindications.
1. Strong CYP3A inducer (such as rifampicin): the dose needs to be increased to 200 mg twice a day.
2. Proton pump inhibitor (such as omeprazole): the dose needs to be increased to 200 mg twice a day.
3. CYP3A substrate : may increase its plasma concentration (such as midazolam).
Store at room temperature 20°C-25°C. The original bottle should be sealed to prevent moisture and the desiccant should be retained.