Source: European Medicines Agency (EU) Revision Year: 2026 Publisher: Sanofi Winthrop Industrie, 82 Avenue Raspail, 94250 Gentilly, France
REZUROCK is indicated for the treatment of adults and paediatric patients (12 years and older with a body weight of at least 40 kg) with chronic graft-versus-host disease (cGVHD) when other treatment options provide limited clinical benefit, are not suitable or have been exhausted.
Treatment should be initiated and supervised by physicians experienced in the management of cGVHD.
The recommended dose is 200 mg given orally once daily with a meal.
Treatment is recommended until disease progression or unacceptable toxicity.
A complete blood cell counts and liver function tests must be performed before initiating therapy (see section 4.4). Initiation of belumosudil in patients with platelets <50 × 109/L or absolute neutrophil count <1.5 × 109/L should be based on close monitoring of laboratory values and clinical assessment.
Liver function tests must be performed at least monthly throughout treatment (see section 4.4).
The recommended dose modifications in case of adverse reactions are provided in Table 1.
Table 1. Recommended dose modifications in case of adverse reactions:
| Adverse reaction | Severity* | Dose modification |
| Hepatotoxicity | Grade 3 ALT or AST (>5 to 20 × ULN) or Grade 2 bilirubin (>1.5 to 3 × ULN) | Hold treatment until recovery to ≤ Grade 1, then resume belumosudil recommended dose and monitor laboratory tests for toxicity. |
| Grade 4 ALT or AST (>20 × ULN) or Grade ≥3 bilirubin (>3 × ULN) | Permanently discontinue treatment. | |
| Other adverse reactions (see section 4.8) | Grade 3 | Hold treatment until recovery to ≤ Grade 1, then resume belumosudil recommended dose and monitor for toxicity. |
| Grade 4 | Permanently discontinue treatment. |
ALT = alanine aminotransferase; AST = aspartate aminotransferase; ULN = upper limit of normal
* Grade 1 is mild, Grade2 is moderate, Grade 3 is severe, Grade 4 is life-threatening. Toxicity grades are in accordance with National Cancer Institute Common Terminology Criteria for Adverse Events Version 4.03 (NCI-CTCAE v4.03)
Strong CYP3A4 inducers and proton pump inhibitors decrease the exposure of belumosudil (see section 4.5).
The recommended dose is 200 mg twice daily with a meal when co-administered with strong CYP3A inducers.
The recommended dose is 200 mg twice daily with a meal when co-administered with proton pump inhibitors.
In the event of a delayed or missed dose:
A dose should be taken as soon as possible on the same day if:
For the next dose, the usual schedule should be resumed.
A dose should not be taken if:
For the next dose, the usual schedule should be resumed.
If a patient vomits following the intake of a dose, the next dose should be taken at the usual time.
In case of missed dose, the patient should be instructed not to take extra doses to make up the missed dose.
Use in patients with severe hepatic impairment (Child-Pugh C) without liver GVHD is contraindicated (see section 4.3). Use in patients with moderate hepatic impairment (Child-Pugh B) without liver GVHD is not recommended (see section 5.2).
No dose adjustment is recommended when administering belumosudil to patients with mild hepatic impairment (Child-Pugh A) (see section 5.2).
No dose adjustment is recommended in patients with mild or moderate renal impairment (creatinine clearance ≥30 mL/min).
No data are available for patients with severe renal impairment (creatinine clearance <30 mL/min) or for patients with end-stage renal disease on dialysis (see section 5.2). Patients should be carefully monitored with regard to safety and efficacy during belumosudil treatment.
No additional dose adjustments are recommended for elderly patients (see sections 5.1 and 5.2).
The safety and efficacy of REZUROCK in paediatric patients aged less than 12 years and with a bodyweight of less than 40 kg have not been established. No data are available.
For oral use.
Film-coated tablets are to be swallowed whole with water at approximately the same time every day with a meal (see section 5.2).
There is no known antidote for overdoses with belumosudil. Single doses up to 1 000 mg have been administered with acceptable tolerability in healthy volunteers. In the event of an overdose, the patient must be monitored for signs or symptoms of adverse reactions and all appropriate supportive measures must be taken immediately.
3 years.
This medicinal product does not require any special storage conditions.
High-density polyethylene (HDPE) bottle with polypropylene child-resistant closure and a silica gel desiccant.
Pack size: 28 or 30 film-coated tablets.
Not all pack sizes may be marketed.
Any unused medicinal product or waste material should be disposed of in accordance with local requirements.
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