Belumosudil

Definition

An orally bioavailable inhibitor of Rho-associated coiled-coil kinase 2 (ROCK2; ROCK-II), with potential immunomodulating activity. Upon oral administration, belumosudil binds to and inhibits the serine/threonine kinase activity of ROCK2. This inhibits ROCK2-mediated signal transduction pathways and modulates various pro- and anti-inflammatory immune cell responses through the regulation of signal transducer and activator of transcription 3 and 5 (STAT3/STAT5) phosphorylation. This downregulates pro-inflammatory Th17 cells and increases regulatory T (Treg) cells. Belumosudil also inhibits ROCK2-mediated fibrotic processes, including stress fiber formation, myofibroblast activation and pro-fibrotic gene transcription. ROCK2 is upregulated in various diseases, including various fibrotic, neurodegenerative and autoimmune diseases.

Also known as 2-[3-[4-(1H-indazol-5-ylamino)-2-quinazolinyl]phenoxy]-N-(1-methylethyl)-acetamide, BELUMOSUDIL, KD 025, KD-025, KD025, Rho-associated Coiled-coil Kinase 2 Inhibitor KD025, ROCK-II Inhibitor KD025, ROCK2 Inhibitor KD025, SLx 2119, SLx-2119, SLx2119 — per NCIT

Also identified as

• ATC L04AA48 per RXNORM
• NCIT NCIT:C128786 per NCIT
• SCTID 1163566003 per RXNORM
• SCTID 1163571005 per RXNORM
• UNII 834YJF89WO per RXNORM

Indications