belumosudil 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
Rho protein kinase inhibitors 5467 911417-87-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • belumosudil
  • belumosudil mesylate
  • rezurock
  • KD025
  • SLx-2119
Belumosudil is an inhibitor of rho-associated, coiled-coil containing protein kinase (ROCK) which inhibits ROCK2 and ROCK1 with IC50 values of approximately 100 nanoM and 3 microM, respectively. Belumosudil downregulated proinflammatory responses via regulation of STAT3/STAT5 phosphorylation and shifting Th17/Treg balance in ex-vivo or in vitro-human T cell assays. Belumosudil also inhibited aberrant pro-fibrotic signaling, in vitro. In vivo, belumosudil demonstrated activity in animal models of chronic GVHD.
  • Molecular weight: 452.52
  • Formula: C26H24N6O2
  • CLOGP: 5.02
  • LIPINSKI: 0
  • HAC: 8
  • HDO: 3
  • TPSA: 104.82
  • ALOGS: -5.19
  • ROTB: 7

  • Status: ONP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
July 16, 2021 FDA KADMON PHARMA LLC

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L04AA48 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
IMMUNOSUPPRESSANTS
IMMUNOSUPPRESSANTS
Selective immunosuppressants
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D047428 Protein Kinase Inhibitors

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Chronic graft-versus-host disease (chronic GVHD) indication 402356004




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 200MG BASE REZUROCK KADMON PHARMS LLC N214783 July 16, 2021 RX TABLET ORAL 8357693 Oct. 30, 2029 FOR THE TREATMENT OF CHRONIC GRAFT VERSUS HOLD DISEASE
EQ 200MG BASE REZUROCK KADMON PHARMS LLC N214783 July 16, 2021 RX TABLET ORAL 10183931 Oct. 7, 2033 FOR THE TREATMENT OF CHRONIC GRAFT VERSUS HOST DISEASE
EQ 200MG BASE REZUROCK KADMON PHARMS LLC N214783 July 16, 2021 RX TABLET ORAL 10696660 Oct. 7, 2033 FOR THE TREATMENT OF CHRONIC GRAFT VERSUS HOST DISEASE
EQ 200MG BASE REZUROCK KADMON PHARMS LLC N214783 July 16, 2021 RX TABLET ORAL 9815820 Oct. 7, 2033 FOR THE TREATMENT OF CHRONIC GRAFT VERSUS HOLD DISEASE
EQ 200MG BASE REZUROCK KADMON PHARMS LLC N214783 July 16, 2021 RX TABLET ORAL 11311541 April 9, 2035 TREATMENT OF ADULTS AND PEDIATRIC PATIENTS 12 AND OLDER WITH SCLERODERMATOUS FORM OF CHRONIC GRAFT-VERSUS-HOST DISEASE ( CGVHD) AFTER FAILURE OF AT LEAST TWO PRIOR LINES OF SYSTEMIC THERAPY

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 200MG BASE REZUROCK KADMON PHARMS LLC N214783 July 16, 2021 RX TABLET ORAL July 16, 2026 NEW CHEMICAL ENTITY
EQ 200MG BASE REZUROCK KADMON PHARMS LLC N214783 July 16, 2021 RX TABLET ORAL July 16, 2028 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

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Rho-associated protein kinase 1 Kinase INHIBITOR IC50 5.52 DRUG LABEL DRUG LABEL
Rho-associated protein kinase 2 Kinase INHIBITOR IC50 5.52 DRUG LABEL DRUG LABEL

External reference:

IDSource
834YJF89WO UNII
C5418179 UMLSCUI
CHEMBL4594302 ChEMBL_ID
D11815 KEGG_DRUG
11950170 PUBCHEM_CID
DB16703 DRUGBANK_ID
CHEMBL4594303 ChEMBL_ID
CHEMBL2005186 ChEMBL_ID
C000619755 MESH_SUPPLEMENTAL_RECORD_UI
9558 IUPHAR_LIGAND_ID
2564025 RXNORM
348524 MMSL
39721 MMSL
d09774 MMSL
1163566003 SNOMEDCT_US
1163567007 SNOMEDCT_US
1163571005 SNOMEDCT_US
4040727 VANDF
018817 NDDF
018818 NDDF
C000718240 MESH_SUPPLEMENTAL_RECORD_UI
11343 INN_ID
2109704-99-4 SECONDARY_CAS_RN

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Rezurock HUMAN PRESCRIPTION DRUG LABEL 1 79802-200 TABLET 200 mg ORAL NDA 27 sections