Belumosudil is a kinase inhibitor that regulates immune response and fibrosis signaling pathways by inhibiting the activity of ROCK2 and ROCK1, and is used to treat chronic graft-versus-host disease (chronic graft-versus-host disease).

1、 Drug name

1. Common name: Belumosudil

2. Product Name: REZUROCK ™

2、 Indications

Used for the treatment of chronic graft-versus-host disease (chronic GVHD) in adults and children aged 12 and above, and must be used after at least two systemic treatment failures.

3、 Specifications and characteristics

200mg tablets: film coated oval tablets.

4、 Main components

Active ingredient: Besudil methanesulfonate (chemical name: 2- {3- [4- (1H-indazol-5-ylamino) -2-quinazolinyl] phenoxy} - N - (prop-2-yl) acetamide methanesulfonate).

5、 Usage and dosage

1. Standard dose: 200mg once daily, taken with food, whole tablet swallowed, not cut, crushed or chewed.

2. Course of treatment: Continue medication until chronic GVHD progresses and requires new systemic treatment.

3. Omission treatment: No need to supplement on the same day, take the medication according to the original plan next time.

6、 Dose adjustment

1. Hepatotoxicity: Suspend administration when there is a level 3 AST/ALT elevation or a level 2 bilirubin elevation, and continue with the original dose after recovery; Permanently discontinue medication when AST/ALT level 4 or bilirubin level ≥ 3 is elevated.

2. Other adverse reactions: pause at level 3 and resume after recovering to level 0-1; Level 4 permanent discontinuation of medication.

3. Drug interactions: When combined with strong CYP3A inducers or proton pump inhibitors, the dose is increased to 200mg twice daily.

7、 Medication precautions

1. Dietary requirements: Must be taken with food and avoid grapefruit and related products.

2. Medication method: Swallow the entire tablet without damaging its structure.

3. Monitoring requirements: Liver function (bilirubin, AST, ALT) should be tested at least once a month.

8、 Medication for special populations

1. Pregnancy/lactation: may cause fetal malformation, contraception is necessary during treatment and 1 week after discontinuation of medication; Prohibited during lactation.

2. Children: Safe and effective for children aged 12 and above, data for children under 12 years old is insufficient.

3. Liver and kidney dysfunction: Those with severe liver/kidney dysfunction need to weigh the risks and benefits.

9、 Adverse reactions

Common (≥ 20%) symptoms include: infection, fatigue, nausea, diarrhea, difficulty breathing, cough, edema, bleeding, abdominal pain, musculoskeletal pain, headache, hypophosphatemia, lymphopenia, and hypertension.

10、 Contraindications

There are no absolute contraindications.

11、 Drug interactions

1. Strong CYP3A inducers (such as rifampicin): The dosage needs to be increased to 200mg twice daily.

2. Proton pump inhibitors (such as omeprazole): The dosage needs to be increased to 200mg twice a day.

3. CYP3A substrate: may increase its blood drug concentration (such as midazolam).

12、 Storage method

Store at room temperature of 20 ° C-25 ° C, seal the original bottle to prevent moisture, and retain the desiccant.

Belumosudilinformation