belumosudil   Click here for help

GtoPdb Ligand ID: 9558

Synonyms: KD-025 | KD025 | Rezurock® | SLx 2119 | SLx2119
Approved drug Immunopharmacology Ligand
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) [1], with clinical anti-inflammatory/immunomodulatory activity.
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2D Structure
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Physico-chemical Properties
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Hydrogen bond acceptors 6
Hydrogen bond donors 3
Rotatable bonds 8
Topological polar surface area 104.82
Molecular weight 452.2
XLogP 5.15
No. Lipinski's rules broken 1
SMILES / InChI / InChIKey
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Canonical SMILES CC(NC(=O)COc1cccc(c1)c1nc(Nc2ccc3c(c2)cn[nH]3)c2c(n1)cccc2)C
Isomeric SMILES CC(NC(=O)COc1cccc(c1)c1nc(Nc2ccc3c(c2)cn[nH]3)c2c(n1)cccc2)C
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)
InChI Key GKHIVNAUVKXIIY-UHFFFAOYSA-N
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Summary of Clinical Use Click here for help
Belumosudil (KD025) was evaluated in clinical studies for immunosuppressive, anti-inflammatory and anti-fibrotic efficacy. The FDA approved belumosudil (Rezurock®) in July 2021, as a treatment for chronic graft-versus-host disease that has failed to be controlled by at least two prior lines of systemic therapy.
Clinical Trials
Clinical Trial ID Title Type Source Comment References
NCT03919799 KD025 in Subjects With Diffuse Cutaneous Systemic Sclerosis Phase 2 Interventional Kadmon Corporation, LLC
NCT02841995 A Study to Evaluate the Safety, Tolerability, and Activity of KD025 in Subjects With Chronic Graft Versus Host Disease Phase 2 Interventional Kadmon Corporation, LLC
NCT02688647 A Study to Evaluate the Safety, Tolerability, and Activity of KD025 in Subjects With Idiopathic Pulmonary Fibrosis Phase 2 Interventional Kadmon Corporation, LLC
NCT02317627 Study of KD025 in Subjects With Psoriasis Vulgaris Who Failed First-Line Therapy Phase 2 Interventional Kadmon Corporation, LLC