belumosudil mesilate at a glance
Medicine class
Selective ROCK2 inhibitor and immunosuppressant
Licensed role
Chronic graft-versus-host disease after at least two previous systemic treatment lines
Administration
Take with a meal and swallow the film-coated tablet whole
Key monitoring
Blood count and liver tests before treatment, with continued liver testing during treatment
What is belumosudil mesilate used for?
The UK-licensed use is:
Chronic graft-versus-host disease in adults and adolescents aged 12 years and over who have received at least two previous lines of systemic therapy.
How does belumosudil mesilate work?
Belumosudil selectively inhibits ROCK2, modifying pathways involved in immune-cell activity and tissue fibrosis that contribute to chronic graft-versus-host disease.
belumosudil mesilate preparations and strengths
Tablet
Route: Oral
Strengths: 200 mg
How to take belumosudil mesilate
Follow the specialist team’s instructions and the dispensing label.
Take the tablet with a meal.
Swallow it whole; do not break, crush or chew it.
Tell the specialist team about all other medicines, particularly acid-reducing treatments.
belumosudil mesilate side effects
Common or expected effects
- Tiredness or weakness
- Nausea, diarrhoea, vomiting, abdominal pain or constipation
- Headache or dizziness
- Muscle, joint or other musculoskeletal pain
- Reduced appetite
- Cough, breathlessness or respiratory infection
- Swelling
- Changes in liver tests or blood-cell counts
Get urgent medical advice
- Serious infection, including pneumonia or bloodstream infection
- Significant liver injury
- Severe gastrointestinal symptoms causing dehydration or inability to keep fluids down
- Marked falls in white cells, red cells or platelets
- Severe or rapidly worsening breathlessness
belumosudil mesilate in pregnancy
Belumosudil is contraindicated during pregnancy because animal studies indicate potential harm to the developing baby and human pregnancy data are unavailable. Pregnancy status should be checked before treatment. Highly effective contraception is required for patients who could become pregnant and for male patients whose partners could become pregnant during treatment and for at least one week afterwards. Contact the specialist team promptly if pregnancy occurs; do not change treatment without advice.
belumosudil mesilate while breastfeeding
It is unknown whether belumosudil enters human milk. Because serious effects in a breastfed child cannot be excluded, breastfeeding should stop during treatment and for at least one week afterwards. Discuss feeding plans with the specialist team.
belumosudil mesilate interactions
A full interaction review is important before starting or stopping any prescribed, over-the-counter or herbal product.
Strong CYP3A4 inducers, such as rifampicin
They can substantially reduce belumosudil exposure, so specialist review is required.
Proton-pump inhibitors, including omeprazole and rabeprazole
They can markedly reduce belumosudil absorption and require specialist management.
Other gastric acid-reducing treatments
They may reduce belumosudil exposure. Confirm management with the specialist team.
Common questions about belumosudil mesilate
Answers are fully visible for fast scanning and source review.
Why is belumosudil mesilate used after a stem-cell transplant?
It treats chronic graft-versus-host disease, in which donor immune cells attack the recipient’s tissues after transplantation.
Does it need to be taken with food?
Yes. Take it with a meal because food substantially increases its absorption.
Can the tablet be crushed or split?
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.