Dosing & Uses
Dosage Forms & Strengths
tablet
- 200mg
Graft Versus Host Disease
Indicated for chronic graft versus host disease (GVHD) in adults and adolescents aged ≥12 years after failure of at least 2 prior lines of systemic therapy
200 mg PO qDay
Continue until progression of chronic GVHD requires new systemic therapy
Dosage Modifications
Hepatotoxicity
- Grade 3 AST or ALT (5-20x ULN) or Grade 2 bilirubin (1.5-3x ULN): Hold until recovery of bilirubin, AST, and ALT to Grade 0-1, then resume at recommended dose
- Grade 4 AST or ALT (>20x ULN) or Grade ≥3 bilirubin (>3x ULN): Permanently discontinue
Other adverse reactions
- Grade 3: Hold until recovery to Grade 0-1, then resume at recommended dose level
- Grade 4: Permanently discontinue
Renal impairment
- Mild-to-moderate (≥30 to <90 mL/min/1.72 m2): No dosage adjustment necessary
- Severe (<30 mL/min/1.72 m2): Not studied
- Patients with preexisting severe renal impairment: Not studied; consider risks and potential benefits before initiating treatment
Hepatic impairment
- Patients with preexisting severe hepatic impairment: Not studied; consider risks and potential benefits before initiating treatment
Strong CYP3A4 inducers
- If coadministered, increase to 200 mg PO BID
Proton pump inhibitors
- If coadministered, increase to 200 mg PO BID
Dosing Considerations
Monitoring parameters
- Monitor total bilirubin, AST, and ALT at least monthly
- Verify pregnancy status of females of reproductive potential before initiating
Dosage Forms & Strengths
tablet
- 200mg
Graft Versus Host Disease
Indicated for chronic graft versus host disease (GVHD) in adults and adolescents aged ≥12 years after failure of at least 2 prior lines of systemic therapy
<12 years: Safety and efficacy not established
≥12 years: 200 mg PO qDay
Continue until progression of chronic GVHD requires new systemic therapy
Dosage Modifications
Hepatotoxicity
- Grade 3 AST or ALT (5-20x ULN) or Grade 2 bilirubin (1.5-3x ULN): Hold until recovery of bilirubin, AST, and ALT to Grade 0-1, then resume at recommended dose
- Grade 4 AST or ALT (>20x ULN) or Grade ≥3 bilirubin (>3x ULN): Permanently discontinue
Other adverse reactions
- Grade 3: Hold until recovery to Grade 0-1, then resume at recommended dose level
- Grade 4: Permanently discontinue
Renal impairment
- Mild-to-moderate (≥30 to <90 mL/min/1.72 m2): No dosage adjustment necessary
- Severe (<30 mL/min/1.72 m2): Not studied
- Patients with pre-existing severe renal impairment: Not studied; consider risks and potential benefits before initiating treatment
Hepatic impairment
- Patients with pre-existing severe hepatic impairment: Not studied; consider risks and potential benefits before initiating treatment
Strong CYP3A4 inducers
- If coadministered, increase to 200 mg PO BID
Proton pump inhibitors
- If coadministered, increase to 200 mg PO BID
Dosing Considerations
Monitoring parameters
- Monitor total bilirubin, AST, and ALT at least monthly
- Verify pregnancy status of females of reproductive potential before initiating
Interactions
Interaction Checker
No Results

Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor

Contraindicated (0)
Serious - Use Alternative (1)
- fexinidazole
fexinidazole will increase the level or effect of belumosudil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Fexinidazole inhibits CYP3A4. Coadministration may increase risk for adverse effects of CYP3A4 substrates.
Monitor Closely (43)
- amobarbital
amobarbital will decrease the level or effect of belumosudil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase belumosudil dosage to 200 mg PO BID when coadministered with strong CYP3A inducers.
- apalutamide
apalutamide will decrease the level or effect of belumosudil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase belumosudil dosage to 200 mg PO BID when coadministered with strong CYP3A inducers.
- armodafinil
armodafinil will decrease the level or effect of belumosudil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- belzutifan
belzutifan will decrease the level or effect of belumosudil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. If unable to avoid coadministration of belzutifan with sensitive CYP3A4 substrates, consider increasing the sensitive CYP3A4 substrate dose in accordance with its prescribing information.
- bexarotene
bexarotene will decrease the level or effect of belumosudil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- bosentan
bosentan will decrease the level or effect of belumosudil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase belumosudil dosage to 200 mg PO BID when coadministered with strong CYP3A inducers.
- brigatinib
brigatinib will decrease the level or effect of belumosudil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- butabarbital
butabarbital will decrease the level or effect of belumosudil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase belumosudil dosage to 200 mg PO BID when coadministered with strong CYP3A inducers.
- butalbital
butalbital will decrease the level or effect of belumosudil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase belumosudil dosage to 200 mg PO BID when coadministered with strong CYP3A inducers.
- carbamazepine
carbamazepine will decrease the level or effect of belumosudil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase belumosudil dosage to 200 mg PO BID when coadministered with strong CYP3A inducers.
- clobazam
clobazam will decrease the level or effect of belumosudil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- dabrafenib
dabrafenib will decrease the level or effect of belumosudil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase belumosudil dosage to 200 mg PO BID when coadministered with strong CYP3A inducers.
- dexlansoprazole
dexlansoprazole will decrease the level or effect of belumosudil by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Increase belumosudil dosage to 200 mg PO BID when coadministered with proton pump inhibitors.
- efavirenz
efavirenz will increase the level or effect of belumosudil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase belumosudil dosage to 200 mg PO BID when coadministered with strong CYP3A inducers.
- elagolix
elagolix will decrease the level or effect of belumosudil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- encorafenib
encorafenib will decrease the level or effect of belumosudil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- enzalutamide
enzalutamide will decrease the level or effect of belumosudil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase belumosudil dosage to 200 mg PO BID when coadministered with strong CYP3A inducers.
- eslicarbazepine acetate
eslicarbazepine acetate will decrease the level or effect of belumosudil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- esomeprazole
esomeprazole will decrease the level or effect of belumosudil by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Increase belumosudil dosage to 200 mg PO BID when coadministered with proton pump inhibitors.
- etravirine
etravirine will decrease the level or effect of belumosudil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase belumosudil dosage to 200 mg PO BID when coadministered with strong CYP3A inducers.
- fosphenytoin
fosphenytoin will decrease the level or effect of belumosudil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase belumosudil dosage to 200 mg PO BID when coadministered with strong CYP3A inducers.
- ivosidenib
ivosidenib will decrease the level or effect of belumosudil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase belumosudil dosage to 200 mg PO BID when coadministered with strong CYP3A inducers.
- lansoprazole
lansoprazole will decrease the level or effect of belumosudil by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Increase belumosudil dosage to 200 mg PO BID when coadministered with proton pump inhibitors.
- lorlatinib
lorlatinib will decrease the level or effect of belumosudil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- lumacaftor/ivacaftor
lumacaftor/ivacaftor will decrease the level or effect of belumosudil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase belumosudil dosage to 200 mg PO BID when coadministered with strong CYP3A inducers.
- mitotane
mitotane will decrease the level or effect of belumosudil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase belumosudil dosage to 200 mg PO BID when coadministered with strong CYP3A inducers.
- mobocertinib
mobocertinib will decrease the level or effect of belumosudil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- nafcillin
nafcillin will decrease the level or effect of belumosudil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase belumosudil dosage to 200 mg PO BID when coadministered with strong CYP3A inducers.
- omeprazole
omeprazole will decrease the level or effect of belumosudil by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Increase belumosudil dosage to 200 mg PO BID when coadministered with proton pump inhibitors.
- pantoprazole
pantoprazole will decrease the level or effect of belumosudil by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Increase belumosudil dosage to 200 mg PO BID when coadministered with proton pump inhibitors.
- pentobarbital
pentobarbital will decrease the level or effect of belumosudil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase belumosudil dosage to 200 mg PO BID when coadministered with strong CYP3A inducers.
- pexidartinib
pexidartinib will decrease the level or effect of belumosudil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- phenobarbital
phenobarbital will decrease the level or effect of belumosudil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase belumosudil dosage to 200 mg PO BID when coadministered with strong CYP3A inducers.
- phenytoin
phenytoin will decrease the level or effect of belumosudil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase belumosudil dosage to 200 mg PO BID when coadministered with strong CYP3A inducers.
- primidone
primidone will decrease the level or effect of belumosudil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase belumosudil dosage to 200 mg PO BID when coadministered with strong CYP3A inducers.
- rabeprazole
rabeprazole will decrease the level or effect of belumosudil by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Increase belumosudil dosage to 200 mg PO BID when coadministered with proton pump inhibitors.
- rifabutin
rifabutin will decrease the level or effect of belumosudil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase belumosudil dosage to 200 mg PO BID when coadministered with strong CYP3A inducers.
- rifampin
rifampin will decrease the level or effect of belumosudil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase belumosudil dosage to 200 mg PO BID when coadministered with strong CYP3A inducers.
- rifapentine
rifapentine will decrease the level or effect of belumosudil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase belumosudil dosage to 200 mg PO BID when coadministered with strong CYP3A inducers.
- secobarbital
secobarbital will decrease the level or effect of belumosudil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase belumosudil dosage to 200 mg PO BID when coadministered with strong CYP3A inducers.
- sotorasib
sotorasib will decrease the level or effect of belumosudil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- St John's Wort
St John's Wort will decrease the level or effect of belumosudil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase belumosudil dosage to 200 mg PO BID when coadministered with strong CYP3A inducers.
- telotristat ethyl
telotristat ethyl will decrease the level or effect of belumosudil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
Minor (0)
Adverse Effects
>10%
All grades
- Infection (unspecified pathogen) (53%)
- Asthenia (46%)
- Nausea (42%)
- Diarrhea (35%)
- Dyspnea (33%)
- Cough (30%)
- Edema (27%)
- Hemorrhage (23%)
- Abdominal pain (22%)
- Musculoskeletal pain (22%)
- Hypertension (21%)
- Headache (21%)
- Viral infection (19%)
- Pyrexia (18%)
- Muscle spasm (17%)
- Decreased appetite (17%)
- Bacterial infection (16%)
- Dysphagia (16%)
- Arthralgia (15%)
- Nasal congestion (12%)
- Rash (12%)
- Pruritus (11%)
Grade 0-1 (baseline)
- ALT increased (83%)
- Creatinine increased (83%)
- Neutrophil count decreased (83%)
- Calcium decreased (82%)
- Potassium increased (82%)
- Platelets decreased (82%)
- Alkaline phosphatase increased (80%)
- Hemoglobin decreased (79%)
- Phosphate decreased (76%)
- Lymphocytes decreased (62%)
- Gamma glutamyl transferase (GGT) increased (47%)
Grade 2-4 max post
- Lymphocytes decreased (29%)
- Phosphate decreased (28%)
- GGT increased (21%)
- Calcium decreased (12%)
- Hemoglobin decreased (11%)
Grade 3-4
- Infection (unspecified pathogen) (16%)
-
Max post
- Lymphocytes decreased (13%)
- GGT increased (11%)
1-10%
Grade 2-4 max post
- Platelets decreased (10%)
- Alkaline phosphate increased (9%)
- Neutrophil count decreased (8%)
- Potassium increased (7%)
- ALT increased (7%)
- Creatinine increased (4%)
Grade 3-4
- Hypertension (7%)
- Diarrhea (5%)
- Dyspnea (5%)
- Hemorrhage (5%)
- Viral infection (4%)
- Bacterial infection (4%)
- Asthenia (4%)
- Nausea (4%)
- Musculoskeletal pain (4%)
- Arthralgia (2%)
- Edema (1%)
- Pyrexia (1%)
- Abdominal pain (1%)
- Decreased appetite (1%)
-
Max post
- Phosphate decreased (7%)
- Platelets decreased (5%)
- Neutrophil count decreased (4%)
- ALT increased (2%)
- Calcium decreased (1%)
- Potassium increased (1%)
- Hemoglobin decreased (1%)
Warnings
Contraindications
None
Cautions
Can cause fetal harm
Drug interaction overview
- Substrate of CYP3A4 and P-gp (in vitro)
-
In vitro studies
- Inhibits BCRP, P-gp, and OATP1B1 at clinically relevant concentrations
- Inhibits CYP1A2, CYP2C19, CYP2D6, UGT1A1, and UGT1A9
-
Strong CYP3A4 inducers
- Increase to 200 mg PO BID
- Strong CYP3A inducers decrease exposure and effects of belumosudil
-
Proton pump inhibitors
- Increase to 200 mg PO BID
- Proton pump inhibitors decrease exposure and effects of belumosudil
Pregnancy & Lactation
Pregnancy
Based on animal studies and mechanism of action, fetal harm may occur
No human data are available on use in pregnant females to evaluate for drug-associated risks
Verify pregnancy status of females of reproductive potential before initiating
Contraception
-
Females of reproductive potential
- Use effective contraception during treatment and for at least 1 week after last dose
- If used during pregnancy or if patient becomes pregnant during treatment, inform patient of potential hazard to fetus
-
Males with female partners of reproductive potential
- Use effective contraception during treatment and for at least 1 week after last dose
Infertility
- Based on animal findings, male or female fertility may be impaired; effects on fertility are reversible
Animal data
- Administration of belumosudil to pregnant rats and rabbits during organogenesis resulted in adverse developmental outcomes, including alterations to growth, embryofetal mortality, and embryofetal malformations at maternal exposures approximately ≥3x (rat) and ≥0.07x (rabbit) the human exposure (AUC) at the recommended dose
Lactation
There are no data available on drug presence or its metabolites in human milk or effects on breastfed children, or milk production
Advise lactating females not to breastfeed during treatment and for at least 1 week after last dose
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Inhibitor of rho-associated, coiled-coil–containing protein kinase (ROCK), which inhibits ROCK2 and ROCK1
Down-regulates proinflammatory responses via regulation of STAT3/STAT5 phosphorylation and shifting Th17/Treg balance in ex vivo or in vitro human T-cell assays
Also, it inhibits aberrant profibrotic signaling, in vitro
In vivo, belumosudil demonstrated activity in animal models of chronic GVHD
Absorption
Peak plasma concentration: 2,390 ng/mL
Peak plasma time: 1.26-2.53 hr
AUC: 22,700 ng⋅hr/mL
Accumulation ratio: 1.4
Bioavailability: 64% (single-dose)
Effect of food
- Single-dose administration with a high-fat and high-calorie meal (800-1,000 calories with ~50% of total caloric content of the meal from fat): Peak plasma concentration and AUC increased 2.2x and 2x; median peak plasma time was delayed 0.5 hr
Distribution
Vd: 184 L
Protein bound: 99.9% (human serum albumin); 98.6% (human alpha1-acid glycoprotein)
Metabolism
Primarily metabolized by CYP3A4 and to a lesser extent by CYP2C8, CYP2D6, and UGT1A9, in vitro
Elimination
Half-life: 19 hr
Clearance: 9.83 L/hr
Excretion: Feces (85% [30% unchanged]); urine (<5%)
Administration
Oral Administration
Take with a meal at approximately the same time each day
Swallow tablets whole; do not cut, crush, or chew
Missed dose: Do not take extra doses to make up missed dose
Patients should inform their health care providers of all concomitant medications, including prescription medicines, over-the-counter drugs, vitamins, and herbal products
Storage
Store at room temperature, 20-25ºC (68-77ºF); excursions permitted to 15-30ºC (59-86ºF)
Dispense in original container only
Store in original container to protect from moisture
Replace cap securely each time after opening; do not discard desiccant
Images
Formulary
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