Belumosudil

Belumosudil
Clinical data
Trade names	Rezurock, Rholistiq
Other names	KD025, SLx-2119
License data	US DailyMed: Belumosudil;
Pregnancy; category	AU: D;
Routes of; administration	By mouth
ATC code	L04AA48 (WHO) ;
Legal status
Legal status	AU: S4 (Prescription only); CA: ℞-only; US: ℞-only;
Identifiers
	IUPAC name 2-[3-[4-(1H-Indazol-5-ylamino)quinazolin-2-yl]phenoxy]-N-propan-2-ylacetamide;
CAS Number	911417-87-3; as salt: 2109704-99-4;
PubChem CID	11950170; as salt: 146025939;
DrugBank	DB16703; as salt: DBSALT003188;
ChemSpider	10124479;
UNII	834YJF89WO; as salt: 6MX7XE1M0U;
KEGG	D11815; as salt: D11816;
ChEMBL	ChEMBL2005186; as salt: ChEMBL4802130;
CompTox Dashboard (EPA)	DTXSID80238425 ;
Chemical and physical data
Formula	C26H24N6O2
Molar mass	452.518 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CC(C)NC(=O)COC1=CC=CC(=C1)C2=NC3=CC=CC=C3C(=N2)NC4=CC5=C(C=C4)NN=C5;
	InChI InChI=InChI=1S/C26H24N6O2/c1-16(2)28-24(33)15-34-20-7-5-6-17(13-20)25-30-23-9-4-3-8-21(23)26(31-25)29-19-10-11-22-18(12-19)14-27-32-22/h3-14,16H,15H2,1-2H3,(H,27,32)(H,28,33)(H,29,30,31) ; Key:GKHIVNAUVKXIIY-UHFFFAOYSA-N ;

Belumosudil, sold under the brand name Rezurock among others, is a medication used for the treatment of chronic graft versus host disease (cGvHD). It is in the class of drugs known as serine/threonine kinase inhibitors. Specifically, it is an inhibitor of Rho-associated coiled-coil kinase 2 (ROCK2; ROCK-II). ROCK2-mediated signaling pathways are major players in pro- and anti-inflammatory immune cell responses. A study in cultured human cells demonstrated that the drug also has effects on oxidative phosphorylation, WNT signaling, angiogenesis, and KRAS signaling.

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.

Belumosudil was approved for medical use in the United States in July 2021. The US Food and Drug Administration considers it to be a first-in-class medication.