Structure via PubChem · Public domain (PubChem)
belumosudil
Sign in to saveAlso known as SLx-2119, KD025, KD-025
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.
Chemical data
- Formula
- C26H24N6O2
- Molecular weight
- 452.5 g/mol
- IUPAC name
- 2-[3-[4-(1H-indazol-5-ylamino)quinazolin-2-yl]phenoxy]-N-propan-2-ylacetamide
- SMILES
- CC(C)NC(=O)COC1=CC=CC(=C1)C2=NC3=CC=CC=C3C(=N2)NC4=CC5=C(C=C4)NN=C5
- InChIKey
- GKHIVNAUVKXIIY-UHFFFAOYSA-N
- XLogP
- 4.8
- Polar surface area
- 105 Ų
- H-bond donors
- 3
- H-bond acceptors
- 6
- Formal charge
- 0
via PubChem
Drug data · ChEMBL
- Max clinical phase
- Approved
- Molecule type
- Small molecule
- First approval
- 2021
- Admin. routes
- oral
- Indications
- diffuse scleroderma, psoriasis, idiopathic pulmonary fibrosis, liver disease
via ChEMBL · EBI
Wikidata facts
- Subclass of
- chemical compound
- Mass
- 452.196
- Has use
- medication
Show 5 more facts
- canonical SMILES
- CC(C)NC(=O)COC1=CC=CC(=C1)C2=NC3=CC=CC=C3C(=N2)NC4=CC5=C(C=C4)NN=C5
- chemical formula
- C₂₆H₂₄N₆O₂
- subject has role
- protein kinase inhibitors
- medical condition treated
- graft-versus-host disease
- Commons category
- Belumosudil
Sources (2)
via Wikidata · CC0
~4 min read
Encyclopedic overview
5 sectionsContents
- Medical uses
- History
- Society and culture
- Legal status
- References
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.
Excerpted from Wikipedia’s “belumosudil” article, available under the CC BY-SA 4.0 licence.