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Synonyms: KD-025 | KD025 | Rezurock® | SLx 2119 | SLx2119
belumosudil is an approved drug (FDA (2021))
Compound class: Synthetic organic
Comment: Belumosudil (KD025) is an oral and selective inhbitor of Rho associated coiled-coil containing protein kinase 2 (ROCK2) , with clinical anti-inflammatory/immunomodulatory activity.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Boerma M, Fu Q, Wang J, Loose DS, Bartolozzi A, Ellis JL, McGonigle S, Paradise E, Sweetnam P, Fink LM et al.. (2008)
Comparative gene expression profiling in three primary human cell lines after treatment with a novel inhibitor of Rho kinase or atorvastatin.
Blood Coagul Fibrinolysis, 19 (7): 709-18. [PMID:18832915]
2. Cutler CS, Lee SJ, Arai S, Rotta M, Zoghi B, Lazaryan A, Ramakrishnan A, DeFilipp Z, Salhotra A, Chai-Ho W et al.. (2021)
Belumosudil for Chronic Graft-versus-Host Disease (cGVHD) After 2 or More Prior Lines of Therapy: The ROCKstar Study.
Blood, [Epub ahead of print]. DOI: 10.1182/blood.2021012021 [PMID:34265047]
3. Jagasia M, Lazaryan A, Bachier CR, Salhotra A, Weisdorf DJ, Zoghi B, Essell J, Green L, Schueller O, Patel J et al.. (2021)
ROCK2 Inhibition With Belumosudil (KD025) for the Treatment of Chronic Graft-Versus-Host Disease.
J Clin Oncol, 39 (17): 1888-1898. DOI: 10.1200/JCO.20.02754 [PMID:33877856]
4. Tengesdal IW, Kitzenberg D, Li S, Nyuydzefe MS, Chen W, Weiss JM, Zhang J, Waksal SD, Zanin-Zhorov A, Dinarello CA. (2018)
The selective ROCK2 inhibitor KD025 reduces IL-17 secretion in human peripheral blood mononuclear cells independent of IL-1 and IL-6.
Eur J Immunol, 48 (10): 1679-1686. [PMID:30098001]