Drug intelligence / Profile preview

s49076

Development stage
Phase 2
Lead developer
Servier
Modality
Small Molecules
Administration
Oral
01

Overview

S49076 is a novel, orally administered, ATP‐competitive small molecule inhibitor targeting multiple receptor tyrosine kinases, specifically MET (hepatocyte growth factor receptor), AXL (AXL receptor tyrosine kinase), and fibroblast growth factor receptors FGFR1/2/3. It has demonstrated potent inhibition of these kinases in preclinical models, blocking cellular phosphorylation and downstream signaling pathways associated with tumor progression and resistance to other anticancer therapies. Preclinical studies showed that S49076 inhibits proliferation in MET‐ and FGFR2‐dependent cancer cells, blocks MET-driven migration in lung carcinoma cells, and suppresses colony formation in hepatocarcinoma cells expressing FGFR1/2 and AXL. In xenograft models, it exhibited strong antitumor activity both as a single agent and in combination with bevacizumab. Clinically, S49076 has been evaluated primarily for advanced solid tumors including glioblastoma and non-small cell lung cancer (NSCLC) in phase I/II trials[1][3][6].

Other names
S-49076(Free base)1265965-22-7UNII-65ZUU7MATUUNII65ZUU7MATUUNII 65ZUU7MATUCHEMBL3808948CHEMBL-3808948CHEMBL 3808948C72114C-72114C 72114SCHEMBL259822SCHEMBL-259822SCHEMBL 259822EX-A1858EX-A-1858EX-A 1858QAC96522QAC-96522QAC 96522BDBM50172080BDBM-50172080BDBM 50172080s8404s-8404s 8404AKOS032945113AKOS-032945113AKOS 032945113CCG-269111CCG269111CCG 269111CS-6191CS6191CS 6191AC–33035– BS–14862– DA–57615– HY–12965
02

Targets

AXL (AXL receptor tyrosine kinase)AURKB (Aurora kinase B)FGFR1 (Fibroblast growth factor receptor 1)FGFR2 (Keratinocyte growth factor receptor)FGFR3 (Fibroblast growth factor receptor 3)ER-XMET (Mesenchymal-epithelial transition factor receptor)

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