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belumosudil 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 4.281 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 11.588 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 28.379 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 20.091 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 0.490 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 2.040 | % | High | 1 |
| herg | hERG pIC50 | 5.364 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 17.498 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 43.954 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 0.480 | % | High | 1 |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 36.813 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 46.238 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 0.470 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 34.754 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 1.910 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 59.979 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 3.850 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 0.600 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 0.828 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| July 16, 2021 | FDA | KADMON PHARMA LLC |
FDA Adverse Event Reporting System (Female)
| 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 |
|---|---|---|---|---|---|---|
| Inappropriate schedule of product administration | 313.22 | 30.10 | 119 | 1895 | 149814 | 90476619 |
| Product use in unapproved indication | 241.01 | 30.10 | 126 | 1888 | 336110 | 90290323 |
| Hospitalisation | 55.93 | 30.10 | 35 | 1979 | 128065 | 90498368 |
| Bronchopulmonary aspergillosis | 38.49 | 30.10 | 13 | 2001 | 11385 | 90615048 |
| Phaeohyphomycosis | 31.98 | 30.10 | 6 | 2008 | 477 | 90625956 |
| Fatigue | 31.75 | 30.10 | 75 | 1939 | 1153948 | 89472485 |
FDA Adverse Event Reporting System (Male)
| 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 |
|---|---|---|---|---|---|---|
| Inappropriate schedule of product administration | 495.80 | 37.56 | 180 | 1827 | 95722 | 42523606 |
| Product use in unapproved indication | 381.88 | 37.56 | 180 | 1827 | 184276 | 42435052 |
| Hospitalisation | 79.05 | 37.56 | 47 | 1960 | 74283 | 42545045 |
| Alveolar proteinosis | 70.22 | 37.56 | 14 | 1993 | 716 | 42618612 |
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 |
|---|---|---|---|---|---|---|
| Inappropriate schedule of product administration | 785.91 | 26.84 | 297 | 4171 | 203340 | 110381491 |
| Product use in unapproved indication | 587.29 | 26.84 | 306 | 4162 | 447071 | 110137760 |
| Hospitalisation | 139.56 | 26.84 | 81 | 4387 | 142412 | 110442419 |
| Alveolar proteinosis | 72.93 | 26.84 | 16 | 4452 | 1520 | 110583311 |
| Chronic graft versus host disease | 55.65 | 26.84 | 19 | 4449 | 9438 | 110575393 |
| Dry eye | 47.42 | 26.84 | 29 | 4439 | 55764 | 110529067 |
| Fatigue | 45.39 | 26.84 | 129 | 4339 | 1215829 | 109369002 |
| Chronic graft versus host disease oral | 40.02 | 26.84 | 8 | 4460 | 483 | 110584348 |
| Pneumonia | 37.60 | 26.84 | 98 | 4370 | 876616 | 109708215 |
| COVID-19 | 36.26 | 26.84 | 47 | 4421 | 245013 | 110339818 |
| Emotional disorder | 35.86 | 26.84 | 16 | 4452 | 16144 | 110568687 |
| Product dose omission in error | 33.02 | 26.84 | 17 | 4451 | 23495 | 110561336 |
| Influenza | 32.44 | 26.84 | 37 | 4431 | 169064 | 110415767 |
| Graft versus host disease in lung | 32.40 | 26.84 | 8 | 4460 | 1270 | 110583561 |
| Death | 31.85 | 26.84 | 80 | 4388 | 698789 | 109886042 |
| Graft versus host disease in skin | 31.35 | 26.84 | 12 | 4456 | 8242 | 110576589 |
| Chronic graft versus host disease in skin | 31.11 | 26.84 | 9 | 4459 | 2610 | 110582221 |
| Depressed mood | 30.95 | 26.84 | 23 | 4445 | 60786 | 110524045 |
| Graft versus host disease | 30.52 | 26.84 | 15 | 4453 | 18791 | 110566040 |
| Chronic graft versus host disease in eye | 29.16 | 26.84 | 6 | 4462 | 419 | 110584412 |
| Cough | 27.78 | 26.84 | 59 | 4409 | 461582 | 110123249 |
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 |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
| CHEBI has role | CHEBI:50748 | antipsoriatic |
| CHEBI has role | CHEBI:233423 | antifibrotic agent |
Related Drugs by ATC class:
L04AA Selective immunosuppressants 10 drugs
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 | 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 | 10183931 | Oct. 7, 2033 | TREATMENT OF CHRONIC GRAFT-VERSUS-HOST DISEASE (CHRONIC GVHD) AFTER FAILURE OF AT LEAST TWO PRIOR LINES OF SYSTEMIC THERAPY IN ADULT AND PEDIATRIC PATIENTS 12 YEARS AND OLDER |
| 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 | 10696660 | Oct. 7, 2033 | TREATMENT OF CHRONIC GRAFT-VERSUS-HOST DISEASE (CHRONIC GVHD) AFTER FAILURE OF AT LEAST TWO PRIOR LINES OF SYSTEMIC THERAPY IN ADULT AND PEDIATRIC PATIENTS 12 YEARS AND OLDER |
| EQ 200MG BASE | REZUROCK | KADMON PHARMS LLC | N214783 | July 16, 2021 | RX | TABLET | ORAL | 8357693 | June 20, 2034 | TREATMENT OF CHRONIC GRAFT-VERSUS-HOST DISEASE (CHRONIC GVHD) AFTER FAILURE OF AT LEAST TWO PRIOR LINES OF SYSTEMIC THERAPY IN ADULT AND PEDIATRIC PATIENTS 12 YEARS AND OLDER THROUGH INHIBITING RHO-ASSOCIATED, COILED-COIL CONTAINING PROTEIN KINASE |
| 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 |
| EQ 200MG BASE | REZUROCK | KADMON PHARMS LLC | N214783 | July 16, 2021 | RX | TABLET | ORAL | 12097202 | July 14, 2042 | TREATMENT OF CHRONIC GRAFT-VERSUS-HOST DISEASE (CHRONIC GVHD) AFTER FAILURE OF AT LEAST TWO PRIOR LINES OF SYSTEMIC THERAPY IN ADULT AND PEDIATRIC PATIENTS 12 YEARS AND OLDER WITH A GRADE 3 INFECTION ADVERSE REACTION |
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 |
| CHEBI:750359 | CHEBI |
| ICQ | PDB_CHEM_ID |
| CHEMBL2005186 | ChEMBL_ID |
| D11815 | KEGG_DRUG |
| 11950170 | PUBCHEM_CID |
| DB16703 | DRUGBANK_ID |
| CHEMBL4802130 | ChEMBL_ID |
| 11343 | INN_ID |
| C000718240 | MESH_SUPPLEMENTAL_RECORD_UI |
| C000619755 | MESH_SUPPLEMENTAL_RECORD_UI |
| 9558 | IUPHAR_LIGAND_ID |
| 1163566003 | SNOMEDCT_US |
| 1163567007 | SNOMEDCT_US |
| 1163571005 | SNOMEDCT_US |
| 4040727 | VANDF |
| 348524 | MMSL |
| 39721 | MMSL |
| d09774 | MMSL |
| 018817 | NDDF |
| 018818 | NDDF |
| 2564025 | RXNORM |
| 834YJF89WO | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Rezurock | HUMAN PRESCRIPTION DRUG LABEL | 1 | 79802-200 | TABLET | 200 mg | ORAL | NDA | 30 sections |