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Belumosudil
Chemical compound / From Wikipedia, the free encyclopedia
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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]
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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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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]