| Pharmaceutical Information |
| Drug Name |
Belumosudil |
| Drug ID |
BADD_D02532 |
| Description |
Belumosudil is used in the treatment of chronic graft-versus-host disease (GVHD) and has been investigated for the treatment of pulmonary arterial hypertension.[A236634] It is an inhibitor of rho-associated coiled-coil-containing protein kinases (ROCK), with significantly more selectivity for ROCK2 as compared to ROCK1 (IC50 100 nM vs. 3 μM, respectively).[L34749] In the treatment of GVHD, a condition in which donor T-cells begin to attack recipient tissues following allogeneic hematopoeitic stem cell transplantation (HSCT), belumosudil helps to resolve immune dysregulation by shifting the balance between Th17 cells and T-regulatory cells, thereby dampening the inflammatory cascade that can occasionally be fatal.[A236644,L34759]
Belumosudil was first approved by the FDA in July 2021, under the brand name Rezurock, for the treatment of chronic GVHD in patients who have tried and failed at least two prior lines of systemic therapy.[L34754] |
| Indications and Usage |
Belumosudil is indicated for the treatment of chronic graft-versus-host disease (GVHD) in adult and pediatric patients 12 years of age and older following failure of at least two other lines of systemic therapy.[L34749] |
| Marketing Status |
approved; investigational |
| ATC Code |
L04AA48 |
| DrugBank ID |
DB16703
|
| KEGG ID |
D11815
|
| MeSH ID |
C000718240
|
| PubChem ID |
11950170
|
| TTD Drug ID |
Not Available
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| NDC Product Code |
69988-0056; 79802-200 |
| UNII |
834YJF89WO
|
| Synonyms |
belumosudil | rezurock |
|
| Chemical Information |
| Molecular Formula |
C26H24N6O2 |
| CAS Registry Number |
911417-87-3 |
| SMILES |
CC(C)NC(=O)COC1=CC=CC(=C1)C2=NC3=CC=CC=C3C(=N2)NC4=CC5=C(C=C4)NN=C5 |
| Chemical Structure |
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| ADRs Induced by Drug |
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