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AboutPricing
Drug ReportsBelumosudil
Belumosudil
Rezurock (belumosudil) is a small molecule pharmaceutical. Belumosudil was first approved as Rezurock on 2021-07-16. It is used to treat graft vs host disease in the USA. The pharmaceutical is active against rho-associated protein kinase 1 and rho-associated protein kinase 2.
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FDA Novel Drug Approvals 2021
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Events Timeline
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FDA approval date
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Results first post date
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Commercial
Therapeutic Areas
Therapeutic Area
MeSH
immune system diseasesD007154
Trade Name
FDA
EMA
Rezurock
Drug Products
FDA
EMA
New Drug Application (NDA)
New Drug Application (NDA)
Abbreviated New Drug Application (ANDA)
Abbreviated New Drug Application (ANDA)
Belumosudil mesylate
Tradename
Company
Number
Date
Products
REZUROCKSanofiN-214783 RX2021-07-16
1 products, RLD, RS
Labels
FDA
EMA
Brand Name
Status
Last Update
rezurockNew Drug Application2025-04-29
Indications
FDA
EMA
Indication
Ontology
MeSH
ICD-10
graft vs host disease—D006086D89.81
Agency Specific
FDA
EMA
Expiration
Code
BELUMOSUDIL MESYLATE, REZUROCK, KADMON PHARMS LLC
2028-07-16ODE-362
2026-07-16NCE
Patent Expiration
Patent
Expires
Flag
FDA Information
Belumosudil Mesylate, Rezurock, Kadmon Pharms Llc
113115412035-04-09U-3369
98158202033-10-07U-3247
101839312033-10-07U-3246
106966602033-10-07U-3246
83576932029-10-30DS, DPU-3247
ATC Codes
L: Antineoplastic and immunomodulating agents
— L04: Immunosuppressants
— L04A: Immunosuppressants
— L04AA: Selective immunosuppressants
— L04AA48: Belumosudil
HCPCS
No data
Clinical
Clinical Trials
37 clinical trials
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Indications Phases 4
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Graft vs host diseaseD006086—D89.81—711—9
Bronchiolitis obliterans syndromeD000092122—D89.811—711—9
Indications Phases 3
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Graft rejectionD006084————1——1
Indications Phases 2
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
PsoriasisD011565EFO_0000676L40—3———3
Systemic sclerodermaD012595EFO_0000717M34—2———2
Diffuse sclerodermaD045743EFO_0000404——2———2
SclerosisD012598———2———2
FibrosisD005355——11———2
Multiple myelomaD009101—C90.011———1
Plasma cell neoplasmsD054219——11———1
Idiopathic pulmonary fibrosisD054990—J84.112—1———1
Pulmonary fibrosisD011658—J84.10—1———1
Lung diseasesD008171EFO_0003818J98.4—1———1
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Indications Phases 1
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Immune system diseasesD007154—D89.94————4
Autoimmune diseasesD001327EFO_0000540M30-M362————2
Drug interactionsD004347——1————1
Healthy volunteers/patients———1————1
Liver diseasesD008107EFO_0001421K70-K771————1
Hepatic insufficiencyD048550——1————1
Biological availabilityD001682——1————1
Indications Without Phase
No data
Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
Drug common nameBelumosudil
INNbelumosudil
Description
Belumosudil, sold under the brand name Rezurock among others, is a medication used for the treatment of chronic graft versus host disease (cGvHD). It is in the class of drugs known as serine/threonine kinase inhibitors. Specifically, it is an inhibitor of Rho-associated coiled-coil kinase 2 (ROCK2; ROCK-II). Belumosudil binds to and inhibits the serine/threonine kinase activity of ROCK2. This inhibits ROCK2-mediated signaling pathways which play major roles in pro- and anti-inflammatory immune cell responses. A genomic study in human primary cells demonstrated that the drug also has effects on oxidative phosphorylation, WNT signaling, angiogenesis, and KRAS signaling.
Classification
Small molecule
Drug classvasodilators (undefined group): Rho protein kinase (ROCK) inhibitors
Image (chem structure or protein)Loading
Structure (InChI/SMILES or Protein Sequence)
CC(C)NC(=O)COc1cccc(-c2nc(Nc3ccc4[nH]ncc4c3)c3ccccc3n2)c1
Identifiers
PDB—
CAS-ID911417-87-3
RxCUI—
ChEMBL IDCHEMBL2005186
ChEBI ID—
PubChem CID11950170
DrugBankDB16703
UNII ID834YJF89WO (ChemIDplus, GSRS)
Target
Agency Approved
ROCK1
ROCK1
ROCK2
ROCK2
Organism
Homo sapiens
Gene name
ROCK1
Gene synonyms
NCBI Gene ID
Protein name
rho-associated protein kinase 1
Protein synonyms
p160 ROCK-1, p160ROCK, Renal carcinoma antigen NY-REN-35, Rho-associated, coiled-coil-containing protein kinase 1, Rho-associated, coiled-coil-containing protein kinase I, ROCK-I
Uniprot ID
Mouse ortholog
Rock1 (19877)
rho-associated protein kinase 1 (Q8C7H0)
Alternate
No data
Variants
No data
Financial
Revenue by drug
$
€
£
â‚£
Rezurock – Sanofi
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Rezurock – Sanofi
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Estimated US medical usage
No data
Trends
PubMed Central
Top Terms for Disease or Syndrome:
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Additional graphs summarizing 489 documents
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Safety
Black-box Warning
No Black-box warning
Adverse Events
Top Adverse Reactions
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2,507 adverse events reported
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