Belumosudil

Belumosudil is an inhibitor of rho-associated, coiled-coil containing protein kinase (ROCK) which inhibits ROCK2 and ROCK1 with IC 50 values of approximately 100 nM and 3 µM, respectively. Belumosudil down-regulated proinflammatory responses via regulation of STAT3/STAT5 phosphorylation and shifting Th17/Treg balance in ex-vivo or in vitro -human T cell assays.

• REZUROCK is indicated for the treatment of adult and pediatric patients 12 years and older with chronic graft-versus-host disease (chronic GVHD) after failure of at least two prior lines of systemic therapy. REZUROCK is a kinase inhibitor indicated for the treatment of adult and pediatric patients 12 years and older with chronic graft-versus-host disease (chronic GVHD) after failure of at least two prior lines of systemic therapy.

• None. None.contraindicated

Recommended Dosage : 200 mg taken orally once daily with food. ( 2.1 ) 2.1 Recommended Dosage The recommended dose of REZUROCK is 200 mg given orally once daily until progression of chronic GVHD that requires new systemic therapy. Instruct the patient on the following: Swallow REZUROCK tablets whole. Do not cut, crush, or chew tablets. Take REZUROCK with a meal at approximately the same time each day [see Clinical Pharmacology (12.3) ] . If a dose of REZUROCK is missed, instruct the patient to not take extra doses to make up the missed dose. Treatment with REZUROCK has not been studied in patients with pre-existing severe renal impairment. For patients with pre-existing severe renal impairment, consider the risks and potential benefits before initiating treatment with REZUROCK [see Clinical Pharmacology (12.3) ] . 2.2 Dosage Modifications for Adverse Reactions Monitor total bilirubin, aspartate aminotransferase (AST), and alanine aminotransferase (ALT) at least monthly. Modify the REZUROCK dosage for adverse reactions as per Table 1. Table 1: Recommended Dosage Modifications for REZUROCK for Adverse Reactions Adverse Reaction Severity Based on CTCAE v 4.03 REZUROCK Dosage Modifications Hepatotoxicity [see Adverse Reactions (6.1) ] Grade 3 AST or ALT (5× to 20× ULN) or Grade 2 bilirubin (1.5× to 3× ULN) Hold REZUROCK until recovery of bilirubin, AST and ALT to Grade 0–1, then resume REZUROCK at the recommended dose. Grade 4 AST or ALT (more than 20× ULN) or Grade ≥3 bilirubin (more than 3× ULN) Discontinue REZUROCK permanently.

Embryo-Fetal Toxicity : Can cause fetal harm. Advise females of reproductive potential of the potential risk to a fetus and to use effective contraception. ( 5.1 , 8.1 , 8.3 ) 5.1 Embryo-Fetal Toxicity Based on findings in animals and its mechanism of action, REZUROCK can cause fetal harm when administered to a pregnant woman. In animal reproduction studies, administration of belumosudil to pregnant rats and rabbits during the period of organogenesis caused adverse developmental outcomes including embryo-fetal mortality and malformations at maternal exposures (AUC) less than those in patients at the recommended dose. Advise pregnant women of the potential risk to a fetus. Advise females of reproductive potential and males with female partners of reproductive potential to use effective contraception during treatment with REZUROCK and for one week after the last dose [see Use in Specific Populations (8.1 , 8.3) , Nonclinical Toxicology (13.1) ] .

The most common (≥20%) adverse reactions, including laboratory abnormalities, are infections, asthenia, nausea, diarrhea, dyspnea, cough, edema, hemorrhage, abdominal pain, musculoskeletal pain, headache, phosphate decreased, gamma glutamyl transferase increased, lymphocytes decreased, and hypertension. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Kadmon Pharmaceuticals, LLC at 1-800-633-1610 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trial Experience Because clinical trials are conducted under widely variable conditions, adverse reaction rates observed in clinical trials of a drug cannot be directly compared with rates of clinical trials of another drug and may not reflect the rates observed in practice. Chronic Graft versus Host Disease In two clinical trials (Study KD025-213 and Study KD025-208), 83 adult patients with chronic GVHD were treated with REZUROCK 200 mg once daily [see Clinical Studies (14.1) ] . The median duration of treatment was 9.2 months (range 0.5 to 44.7 months). Fatal adverse reaction was reported in one patient with severe nausea, vomiting, diarrhea and multi-organ failure. Permanent discontinuation of REZUROCK due to adverse reactions occurred in 18% of patients. The adverse reactions which resulted in permanent discontinuation of REZUROCK in >3% of patients included nausea (4%). Adverse reactions leading to dose interruption occurred in 29% of patients.

Lactation : Advise not to breastfeed. ( 8.2 ) Moderate or Severe Hepatic Impairment: Avoid use of REZUROCK in patients with moderate or severe hepatic impairment. ( 2.4 , 8.7 ) 8.1 Pregnancy Risk Summary Based on findings from animal studies and the mechanism of action [see Clinical Pharmacology (12.1) ] , REZUROCK can cause fetal harm when administered to pregnant women. There are no available human data on REZUROCK use in pregnant women to evaluate for a drug-associated risk. In animal reproduction studies, administration of belumosudil to pregnant rats and rabbits during the period of organogenesis resulted in adverse developmental outcomes, including alterations to growth, embryo-fetal mortality, and embryo-fetal malformations at maternal exposures (AUC) approximately ≥1.4 (rat) and ≥0.08 (rabbit) times the human exposure (AUC) at the recommended dose (see Data ) . Advise pregnant women and females of reproductive potential of the potential risk to the fetus. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively.

Metabolism

The following pharmacokinetic parameters are presented for chronic GVHD patients administered belumosudil 200 mg once daily, unless otherwise specified. The mean (% coefficient of variation, %CV) steady-state AUC and C max of belumosudil was 22,700 (48%) h∙ng/mL and 2390 (44%) ng/mL, respectively.

• Jul 16, 2021NDANDA214783Kadmon Pharms Llc

1. 1Product Use In Unapproved Indication42214%
2. 2Inappropriate Schedule Of Product Administration40714%
3. 3Fatigue2378.0%
4. 4Off Label Use2087.0%
5. 5Death1615.4%
6. 6Product Dose Omission Issue1555.2%
7. 7Drug Ineffective1535.2%
8. 8Nausea1404.7%
9. 9Pneumonia1384.6%
10. 10Hospitalisation1324.4%
11. 11Diarrhoea1314.4%
12. 12Condition Aggravated1304.4%
13. 13Dyspnoea1194.0%
14. 14Asthenia893.0%
15. 15Pain883.0%

The 10 most recently updated of 38 ClinicalTrials.gov registrations naming Belumosudil as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• IL6-receptor Inhibitor Iwith Belumosudil for the Treatment of Belumosudil-refractory cGVHD
  Not yet recruiting · Phase 1 · Interventional · 10 enrolled · Stanford University
  NCT07484113updated 2026-06-12
• Belumosudil With Ruxolitnib as Second Line Therapy for Chronic Graft Versus Host Disease (cGvHD) After Steroid Failure
  Not yet recruiting · Phase 2 · Interventional · 63 enrolled · Dennis Kim
  NCT07643025updated 2026-06-11
• BElumosudil for Bronchiolitis Obliterans Prevention/Therapy (BEBOP)
  Recruiting · Phase 2 · Interventional · 45 enrolled · Dana-Farber Cancer Institute
  NCT05922761updated 2026-06-10
• A Study of Belumosudil in Children With Chronic Graft Versus Host Disease (schoolROCK)
  Recruiting · Phase 2 · Interventional · 37 enrolled · Sanofi
  NCT07116031updated 2026-06-05
• Belumosudil for the Pre-emptive Treatment of Patients With Chronic Graft Versus Host Disease
  Recruiting · Phase 2 · Interventional · 82 enrolled · Fred Hutchinson Cancer Center
  NCT05996627updated 2026-06-04
• A Study to Test How Effective Belumosudil Tablets Are for Treating Adult Participants With Chronic Lung Allograft Dysfunction
  Recruiting · Phase 3 · Interventional · 180 enrolled · Sanofi
  NCT06082037updated 2026-06-02
• A Clinical Study to Evaluate the Pharmacokinetics, Efficacy, and Safety of Belumosudil in Chinese Adolescents With cGVHD Who Have Had an Inadequate Response to Glucocorticoids or Other Systemic Therapies
  Completed · Phase 4 · Interventional · 6 enrolled · Sanofi
  NCT06616415updated 2026-05-27
• A Prospective Study of Madecassoside Tablets in Sclerotic Chronic Graft-versus-Host Disease After Allo-HSCT
  Recruiting · Phase 2 · Interventional · 30 enrolled · WeiShi
  NCT07606703updated 2026-05-26
• A Study to Investigate Safety of Belumosudil in Participants Aged 12 Years and Above, With Chronic Graft-versus-host Disease (cGVHD)
  Not yet recruiting · Phase 4 · Interventional · 26 enrolled · Sanofi
  NCT07135973updated 2026-05-12
• Belumosudil to Block Chronic Lung Allograft Dysfunction (CLAD) in High Risk Lung Transplant Recipients
  Recruiting · Phase 2 · Interventional · 234 enrolled · National Institute of Allergy and Infectious Diseases (NIAID)
  NCT06476132updated 2026-05-12

Frequently asked questions

How does Belumosudil work?

Belumosudil is an inhibitor of rho-associated, coiled-coil containing protein kinase (ROCK) which inhibits ROCK2 and ROCK1 with IC 50 values of approximately 100 nM and 3 µM, respectively. Belumosudil down-regulated proinflammatory responses via regulation of STAT3/STAT5 phosphorylation and shifting Th17/Treg balance in ex-vivo or in vitro -human T cell assays.

What is Belumosudil used for?

According to FDA labeling, Belumosudil carries indications including: REZUROCK is indicated for the treatment of adult and pediatric patients 12 years and older with chronic graft-versus-host disease (chronic GVHD) after failure of at least two prior lines of systemic therapy. REZUROCK is a kinase inhibitor indicated for the treatment of adult and pediatric patients 12 years and older with chronic graft-versus-host disease (chronic GVHD) after failure of at least two prior lines of systemic therapy.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Belumosudil?

Belumosudil is classified as Selective immunosuppressants, Rho Kinase Inhibitors.

What are the brand names for Belumosudil?

Belumosudil is marketed under brand names including Rezurock.

What are the contraindications for Belumosudil?

Belumosudil labeling lists contraindications including: None. None.. Always consult the full prescribing information and a clinician.