Global InformationBelumosudil information
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| Trade names | Rezurock, Rholistiq |
| Other names | KD025, SLx-2119 |
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| Routes of administration | By mouth |
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| Formula | C26H24N6O2 |
| Molar mass | 452.518 g·mol−1 |
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Belumosudil, sold under the brand name Rezurock among others, is a medication used for the treatment of chronic graft versus host disease (cGvHD).[1][5][6] It is in the class of drugs known as serine/threonine kinase inhibitors.[6] Specifically, it is an inhibitor of Rho-associated coiled-coil kinase 2 (ROCK2; ROCK-II).[7] Belumosudil binds to and inhibits the serine/threonine kinase activity of ROCK2. This inhibits ROCK2-mediated signaling pathways which play major roles in pro- and anti-inflammatory immune cell responses. A genomic study in human primary cells demonstrated that the drug also has effects on oxidative phosphorylation, WNT signaling, angiogenesis, and KRAS signaling.[8]
The most common side effects include infection, tiredness or weakness, nausea, diarrhea, shortness of breath, cough, swelling, bleeding, stomach (abdominal) pain, muscle or bone pain, headache, and high blood pressure.[9]
Belumosudil was approved for medical use in the United States in July 2021.[5][6] The US Food and Drug Administration considers it to be a first-in-class medication.[10]
- ^ a b c "Rholistiq". Therapeutic Goods Administration (TGA). 26 November 2021. Archived from the original on 28 December 2021. Retrieved 28 December 2021.
- ^ a b "AusPAR: Belumosudil". Therapeutic Goods Administration (TGA). 10 May 2022. Archived from the original on 10 May 2022. Retrieved 10 May 2022.
- ^ "Archived copy" (PDF). Archived (PDF) from the original on 29 June 2022. Retrieved 29 June 2022.
{{cite web}}: CS1 maint: archived copy as title (link) - ^ "Summary Basis of Decision - Rholistiq". Health Canada. 23 October 2014. Retrieved 6 August 2022.
- ^ a b c "Rezurock- belumosudil tablet". DailyMed. Archived from the original on 21 August 2021. Retrieved 20 August 2021.
- ^ a b c d "FDA approves belumosudil for chronic graft-versus-host disease". U.S. Food and Drug Administration (FDA). 16 July 2021. Archived from the original on 16 July 2021. Retrieved 16 July 2021.
This article incorporates text from this source, which is in the public domain.
- ^ Boerma M, Fu Q, Wang J, Loose DS, Bartolozzi A, Ellis JL, et al. (October 2008). "Comparative gene expression profiling in three primary human cell lines after treatment with a novel inhibitor of Rho kinase or atorvastatin". Blood Coagulation & Fibrinolysis. 19 (7): 709–18. doi:10.1097/MBC.0b013e32830b2891. PMC 2713681. PMID 18832915.
- ^ Park J, Chun KH (5 May 2020). "Identification of novel functions of the ROCK2-specific inhibitor KD025 by bioinformatics analysis". Gene. 737: 144474. doi:10.1016/j.gene.2020.144474. PMID 32057928. S2CID 211111888.
- ^ Cite error: The named reference
FDA snapshotwas invoked but never defined (see the help page). - ^ Advancing Health Through Innovation: New Drug Therapy Approvals 2021 (PDF). U.S. Food and Drug Administration (FDA) (Report). 13 May 2022. Archived from the original on 6 December 2022. Retrieved 22 January 2023. This article incorporates text from this source, which is in the public domain.
