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belumosudil
- Development stage
- Approved
- Lead developer
- Kadmon
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Belumosudil is an oral small molecule inhibitor of rho-associated coiled-coil-containing protein kinase 2 (ROCK2), with significantly higher selectivity for ROCK2 over ROCK1. It is used to treat chronic graft-versus-host disease (cGVHD) in adults and children aged 12 years and older who have received at least two prior unsuccessful treatments. By inhibiting ROCK2, belumosudil modulates immune responses by downregulating pro-inflammatory Th17 cells and upregulating regulatory T-cells through the regulation of STAT3/STAT5 phosphorylation, thereby reducing inflammation and fibrosis. The drug was developed by Kadmon Holdings, which is now part of Sanofi[1][3][6][7][8].
- Brand names
- Rezurock
- Other names
- belumosudil
02
Targets
ROCK2 (Rho-associated coiled-coil containing protein kinase 2)ROCK1 (Rho-associated coiled-coil containing protein kinase 1)
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