Drug intelligence / Profile preview

osi-930

Development stage
Phase 1
Lead developer
Astellas Pharma
Modality
Small Molecules
Administration
Oral
01

Overview

OSI-930 is a selective thiophene-derived tyrosine kinase inhibitor with potential antineoplastic activity. It is an orally active small molecule that primarily inhibits the receptor tyrosine kinases c-Kit and vascular endothelial growth factor receptor 2 (VEGFR2), as well as platelet-derived growth factor receptors. By targeting these pathways, OSI-930 aims to inhibit both cancer cell proliferation and tumor angiogenesis. Preclinical studies have shown broad efficacy in models of small cell lung cancer, glioblastoma, colorectal cancer, renal cancer, head and neck cancer, non-small cell lung cancer and gastric cancers[1][5]. In clinical trials for advanced solid tumors in the USA and China (where it was out-licensed to Simcere Pharma as SIM-930), it demonstrated safety and preliminary antitumor activity[6][8].

Other names
3-(quinolin-4-ylmethylamino)-N-(4-(trifluoromethoxy)phenyl)thiophene-2-carboxamide728033-96-3UNII-G1PEG5Q9Y2UNII-G-1PEG5Q9Y2UNII-G 1PEG5Q9Y2SIM-930 (in China after out-licensing to Simcere Pharma)[1][4]
02

Targets

KIT (c-KIT proto-oncogene receptor tyrosine kinase)VEGFR2 (Vascular endothelial growth factor receptor 2)PDGFRB (Platelet-derived growth factor receptor beta)

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