Belumosudil
Belumosudil is a ROCK (rho-associated, coiled-coil containing protein kinase) inhibitor used to treat inflammatory and immune-mediated conditions. It works by inhibiting ROCK2 and ROCK1 enzymes, which reduces proinflammatory responses through regulation of STAT3/STAT5 signaling pathways.
Belumosudil is an immunosuppressant that inhibits ROCK enzymes to reduce inflammatory responses in immune-mediated conditions.
Key facts at a glance
- ATC
- L04AA48
- RxNorm
- 2564025
- Generic
- Belumosudil
- Class
- atc-l04
- Brands
- Rezurock
- Availability
- rx
- Lactation
- unknown
- Routes
- oral
- Forms
- tablet
- Regions
- US, EU, CN, JP
- Monitoring
- —
This page is for informational purposes only.
Do not use this information to diagnose yourself or to replace a physician's advice. Always consult a qualified healthcare provider before starting, stopping, or changing any medication. If you believe you are experiencing a medical emergency, call your local emergency number immediately.
Dosage and administration
- Usual dose
- 500mg twice daily
- Maximum
- consult physician
- Frequency
- every 12 hours
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
- Usual dose
- 250mg twice daily
- Maximum
- consult physician
- Frequency
- every 12 hours
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
- Usual dose
- 400mg daily
- Maximum
- consult physician
- Frequency
- once daily
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
Overdose information
Special Populations
10 groupspregnancy
generalavoid if possible
avoid use during pregnancy unless benefits outweigh risks - animal studies show fetal toxicity
regular fetal monitoring if used
Use with caution and monitor for adverse effects.
pregnancy
first trimesteravoid
avoid use during first trimester unless absolutely necessary
close fetal monitoring
Use with caution and monitor for adverse effects.
pregnancy
third trimesteravoid
avoid use near term unless benefits outweigh risks
fetal monitoring
Use with caution and monitor for adverse effects.
lactation
breastfeedingavoid
breastfeeding not recommended during treatment - unknown if drug passes into breast milk
none established
pediatric_age
under 18 yearsnot recommended
safety and efficacy not established in pediatric patients
not applicable
geriatric
over 65 yearsno adjustment required
no dose adjustment required - use with standard dosing but monitor for adverse effects
standard monitoring for efficacy and adverse effects
Use with caution and monitor for adverse effects.
renal_impairment
mild moderateno adjustment required
no dose adjustment needed for mild to moderate renal impairment
standard monitoring
renal_impairment
severeuse with caution
limited data available for severe renal impairment - use with caution
close monitoring for adverse effects
Use with caution and monitor for adverse effects.
hepatic_impairment
mild moderateno adjustment required
no dose adjustment needed for mild to moderate hepatic impairment
standard monitoring
hepatic_impairment
severeuse with caution
limited data for severe hepatic impairment - use with caution
close monitoring for adverse effects
Use with caution and monitor for adverse effects.
Statistics and clinical data
Drug class
Molecular classification of Belumosudil
FDA approval year
FDA approval date for Rezurock
Primary indication
Approved therapeutic use
Brand name
Commercial brand name
Used for the treatment of chronic graft-versus-host disease (cGVHD) in adult and pediatric patients who have received at least two prior systemic therapies.
Belumosudil inhibits ROCK2 and ROCK1 kinases with IC50 values of approximately 100 nM and 3 µM respectively. By inhibiting these kinases, it down-regulates proinflammatory responses through regulation of STAT3/STAT5 phosphorylation pathways, modulating immune cell function.
As an immunosuppressant, it may increase the risk of infections. Liver function should be monitored during treatment. Common side effects may include fatigue, headache, and gastrointestinal symptoms. Drug interactions may occur with strong CYP3A inducers or inhibitors.
Contraindications
Conditions and patient states where this medication should be avoided or used with caution.
Do not use (1)
Known allergy to this medication or its components
Use caution (1)
Consult healthcare provider for benefits vs risks assessment
Official drug label
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This information is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment.
This content is for general informational and educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the guidance of a qualified healthcare provider with any questions you have about a medical condition, and never disregard professional medical advice or delay seeking it because of something you read here.
If you think you may have a medical emergency, call your local emergency number or go to the nearest emergency department immediately.
Medically reviewed by WellAlly Editorial Team Last reviewed July 26, 2026. · Read our editorial policy