What is Rezurock used for?

Rezurock is used to treat adults and children 12 years or older with chronic graft-versus-host disease (GVHD) who have not responded to at least two other treatments.

Can Rezurock cause birth defects?

Yes, Rezurock can cause fetal harm and should not be used during pregnancy.

What should I do if I miss a dose of Rezurock?

Take the missed dose as soon as possible on the same day, but do not take two doses at once to catch up.

Should I take Rezurock with food?

Yes, it is recommended to take Rezurock once daily with a meal.

Can I breastfeed while taking Rezurock?

No, you should not breastfeed during treatment and for one week after your last dose.

What are the most common side effects of Rezurock?

Common side effects include infections, fatigue, nausea, diarrhea, and cough.

Does Rezurock affect liver function?

Yes, it can affect liver enzymes and bilirubin, so monthly blood tests are necessary.

Can Rezurock be used in children?

Yes, it is approved for children and adolescents 12 years of age and older.

BELUMOSUDIL | CAS 911417-87-3 | GKHIVNAUVKXIIY

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Kinase inhibitor

Rezurock (belumosudil) is a kinase inhibitor used to treat adults and children (aged 12 and older) who have chronic graft-versus-host disease (GVHD) and have already failed at least two other systemic treatments. It works by inhibiting specific proteins involved in inflammation and fibrosis.

How it worksRezurock works by blocking a protein called ROCK (specifically ROCK1 and ROCK2). This helps reduce harmful inflammation and prevents excessive scarring in the body.

Brand names:Rezurock

Used for

Chronic graft-versus-host disease (GVHD) in adults and children 12 years or older after failing two or more previous systemic therapies.

Conditions

Chronic graft-versus-host disease

Class

Kinase inhibitorImmune System

How to take

FormsOral tablet

RoutesOral

The standard dose is 200 mg taken once daily with food.

Swallow tablets whole; do not cut, crush, or chew them. Take the dose at approximately the same time each day. If you miss a dose, take it as soon as possible on the same day, but do not take an extra dose to make up for it.

Missed dose: Take the missed dose as soon as possible on the same day. Do not take an extra dose to make up for a missed dose.

Key warnings

·Embryo-Fetal Toxicity: Rezurock can cause harm to an unborn baby. Females of reproductive potential and males with female partners should use effective contraception during treatment and for one week after the last dose.
·Liver Health: Monthly monitoring of liver function (AST, ALT, and bilirubin) is required.

Do not use if

·None listed

Side effects

Common

InfectionsFatigue (asthenia)NauseaDiarrheaShortness of breath (dyspnea)CoughSwelling (edema)Bleeding (hemorrhage)Abdominal painMuscle or bone painHeadacheLow phosphate levelsHigh liver enzymes (gamma glutamyl transferase)Low lymphocyte countsHigh blood pressure (hypertension)

Serious

·Fetal harm/birth defects
·Severe infections
·Liver toxicity (hepatotoxicity)
·Severe nausea, vomiting, and diarrhea leading to organ failure
·Kidney failure

Seek help if

·pregnancy
·liver_function
·infections

Interactions

·Strong CYP3A inducers (e.g., certain antibiotics or seizure meds): May require increasing the Rezurock dose to 200 mg twice daily.
·Proton Pump Inhibitors (acid reducers): May require increasing the Rezurock dose to 200 mg twice daily.
·UGT1A1 substrates: Avoid using Rezurock with drugs that rely on this pathway to avoid serious toxicity.
·P-gp, OATP1B1, and BCRP substrates: Rezurock may increase the levels of these drugs in your body, increasing their risk of side effects.

FoodTaking Rezurock with a high-fat, high-calorie meal increases the amount of medicine your body absorbs.

Special populations

PregnancyRezurock can cause fetal harm. Animal studies showed developmental issues and death in unborn rats and rabbits. Pregnant women should be informed of these risks, and effective contraception is required during and for one week after treatment.

BreastfeedingDo not breastfeed while taking Rezurock. You should also wait at least one week after your last dose before breastfeeding.

PediatricRezurock is approved for use in children and adolescents aged 12 years and older. Safety and effectiveness have not been established for children under 12.

GeriatricRezurock has been used in patients aged 65 and older, and no significant differences in safety or effectiveness were noted compared to younger patients.

Talk to your doctor

Monitor

·Total bilirubin
·Aspartate aminotransferase (AST)
·Alanine aminotransferase (ALT)
·Lymphocytes
·Phosphate levels
·Blood pressure

Questions to ask

·What are the risks of Rezurock for my liver?
·How often will I need blood tests while on Rezurock?
·Are there specific foods I should avoid with Rezurock?
·How should I manage my other medications while taking Rezurock?

Pharmacokinetics

Half-life19 hours

Bioavailability64%

Protein binding99.9% to human serum albumin; 98.6% to human α 1-acid glycoprotein

MetabolismPrimarily metabolized by CYP3A4; also by CYP2C8, CYP2D6, and UGT1A9.

Excretion85% recovered in feces (30% as unchanged); less than 5% in urine.

Ingredients

Inactive

colloidal silicon dioxidecroscarmellose sodiumhypromellosemagnesium stearatemicrocrystalline cellulosepolyethylene glycolpolyvinyl alcoholtalctitanium dioxideyellow iron oxide

Educational summary derived from FDA labeling, AI-assisted. Not medical advice — consult a healthcare professional. Updated 2026-04-26.