belumosudil mesylate

{
  "id": "MLC-T-ONC-011943",
  "term": "belumosudil mesylate",
  "field": "Oncology and biomedicine",
  "definition": "The mesylate salt form of belumosudil, 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.",
  "synonyms": [
    "2-(3-(4-(1H-indazol-5-ylamino)quinazolin-2-yl)phenoxy)-N-(propan-2-yl)acetamide methanesulfonate (1:1)",
    "KD025 mesylate"
  ],
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/belumosudil-mesylate/"
}