belumosudil 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| Rho protein kinase inhibitors | 5467 | 911417-87-3 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
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.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
None
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| 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)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Graft versus host disease in skin | 42.08 | 37.81 | 9 | 402 | 6064 | 79737913 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| 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|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| 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 strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent 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 strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 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:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA 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:
| ID | Source |
|---|---|
| 834YJF89WO | UNII |
| 2109704-99-4 | SECONDARY_CAS_RN |
| C5418179 | UMLSCUI |
| ICQ | PDB_CHEM_ID |
| CHEMBL2005186 | ChEMBL_ID |
| D11815 | KEGG_DRUG |
| 11950170 | PUBCHEM_CID |
| DB16703 | DRUGBANK_ID |
| CHEMBL4802130 | ChEMBL_ID |
| 11343 | INN_ID |
| C000619755 | MESH_SUPPLEMENTAL_RECORD_UI |
| 9558 | IUPHAR_LIGAND_ID |
| 018817 | NDDF |
| 018818 | NDDF |
| 1163566003 | SNOMEDCT_US |
| 1163567007 | SNOMEDCT_US |
| 1163571005 | SNOMEDCT_US |
| 4040727 | VANDF |
| 2564025 | RXNORM |
| 348524 | MMSL |
| 39721 | MMSL |
| d09774 | MMSL |
| C000718240 | MESH_SUPPLEMENTAL_RECORD_UI |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Rezurock | HUMAN PRESCRIPTION DRUG LABEL | 1 | 75929-174 | TABLET | 200 mg | ORAL | NDA | 28 sections |
| Rezurock | HUMAN PRESCRIPTION DRUG LABEL | 1 | 79802-200 | TABLET | 200 mg | ORAL | NDA | 29 sections |
| Rezurock | HUMAN PRESCRIPTION DRUG LABEL | 1 | 79802-200 | TABLET | 200 mg | ORAL | NDA | 29 sections |
| Rezurock | HUMAN PRESCRIPTION DRUG LABEL | 1 | 79802-200 | TABLET | 200 mg | ORAL | NDA | 29 sections |