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belumosudil

Rezurock · ATC code L04AA48

Key facts
Active substance
belumosudil
Drug class
Immunosuppressive drug
ATC code
L04AA48
Authorisation
centrally authorised across the EU (EMA)
Dosage forms
REZUROCK 200 mg film-coated tablets
Marketing authorisation holder
Sanofi Winthrop Industrie
Information as of
2026-10-29

Key facts

Belumosudil (Rezurock) is an oral kinase inhibitor used to treat chronic graft-versus-host disease (cGVHD) when other treatments are insufficient.

What it is used for

  • Chronic graft-versus-host disease in adults and paediatric patients 12 years and older weighing at least 40 kg, when other treatment options provide limited clinical benefit, are not suitable or have been exhausted.

Dosing

  • Usual dose: 200 mg orally once daily with a meal, until disease progression or unacceptable toxicity.
  • With strong CYP3A inducers or proton pump inhibitors: 200 mg twice daily with a meal.
  • Complete blood counts and liver function tests before starting; liver tests at least monthly during treatment.
  • Grade 3 hepatotoxicity (ALT/AST > 5 to 20 × ULN) or Grade 2 bilirubin: hold until ≤ Grade 1, then resume; Grade 4 or bilirubin ≥ Grade 3: discontinue permanently. Other Grade 3 reactions: hold; Grade 4: discontinue.
  • Missed dose: take the same day if missed ≤ 12 hours (once daily) or ≤ 6 hours (twice daily); otherwise skip.

Contraindications

  • Pregnancy and breast-feeding.
  • Severe hepatic impairment (Child-Pugh C) without liver GVHD.
  • Hypersensitivity to the active substance or any excipient.

Important warnings

  • Hepatotoxicity: monitor liver tests before and at least monthly during treatment; modify dose by severity.
  • Women of childbearing potential: verify pregnancy status before starting and use highly effective contraception during treatment and for at least one week after the last dose.
  • Men with female partners of childbearing potential must also use highly effective contraception; male fertility may be impaired.
  • Starting treatment with platelets < 50 × 10⁹/L or neutrophils < 1.5 × 10⁹/L requires close monitoring.

Side effects

  • Most common: fatigue (20.2%), diarrhoea (12.8%), nausea (11.7%), headache (10.6%), vomiting (8.5%), AST increased (7.4%), ALT increased (5.3%) and GGT increased (4.3%).
  • Most common Grade 3 or 4 reactions: pneumonia, hypoxia and diarrhoea (2.1% each).
  • Serious reactions included pneumonia (2.1%), cellulitis, pulmonary embolism and multiple organ dysfunction syndrome.

Interactions

  • Strong CYP3A4 inducers (e.g. carbamazepine, phenytoin, rifampicin, St John's wort) decrease belumosudil exposure (rifampicin reduced AUC by 72%); not recommended, otherwise increase to 200 mg twice daily.
  • Proton pump inhibitors decrease exposure; use 200 mg twice daily.

Pregnancy and breastfeeding

  • Contraindicated in pregnancy; animal studies showed reproductive toxicity.
  • Breast-feeding should be discontinued during treatment and for at least one week after the last dose.

Summary of the official product information, written with AI on 2026-10-29. Every number was checked automatically against the original text. Not reviewed by a physician – the full official text is authoritative.

Full official text →

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For patients

Package leaflet, verbatim

This product has no separate US patient information.

Authorisation and brand names by country

Medicines with exactly this active-substance composition, as listed in the national registers – alphabetical and without ranking. Whether a product is currently available is not shown here.

EU – centrally authorised (all member states)

  • RezurockSanofi Winthrop Industrie · EMEA/H/C/006421

Source: European Medicines Agency (EMA), product information

Turkey

  • RezurockSANOFİ SAĞLIK ÜRÜNLERİ LTD. ŞTİ. · 1 register entry

Source: TİTCK – Ruhsatlı Beşeri Tıbbi Ürünler Listesi, as of 2026-10-16

Brand names in 3 more European countries
Iceland
Rezurock
Liechtenstein
Rezurock
Norway
Rezurock

EMA – Article 57 product data (EU/EEA), 2026-10-29

Medelix receives no money from pharmaceutical companies. Brand names are listed alphabetically and without ranking.

Other substances in the same group

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Sources

  1. European Medicines Agency. Rezurock – EPAR, Product Information. 2026-10-29. https://www.ema.europa.eu/en/documents/product-information/rezurock-epar-product-information_en.pdf
  2. TİTCK – Ruhsatlı Beşeri Tıbbi Ürünler Listesi, 2026-10-16. https://www.titck.gov.tr/dinamikmodul/85
  3. Wikidata (CC0): ATC L04AA.

Editorial: Medelix editorial team · last updated 2026-10-29 · How these pages are made · Report an error

Source: European Medicines Agency (EMA), product information. Not advertising, not a treatment recommendation. For questions about your own treatment, ask your doctor or pharmacist.