Drug intelligence / Profile preview

SAR125844

Development stage
Phase 2
Lead developer
Sanofi
Modality
Small Molecules
Administration
Intravenous
01

Overview

**SAR125844** is a highly selective small molecule inhibitor of the MET tyrosine kinase (also known as hepatocyte growth factor receptor or c-Met). It was developed for intravenous administration and has demonstrated nanomolar activity against wild-type c-Met. The drug disrupts c-Met-mediated signal transduction pathways by binding to the receptor and inhibiting its kinase activity. This mechanism can result in inhibition of tumor cell proliferation and survival in cancers with MET amplification or dysregulation. Clinical studies have focused on advanced solid tumors—particularly those with MET gene amplification—including non-small cell lung cancer (NSCLC) and gastric cancer. In phase I/II trials, partial responses were observed mainly in patients with MET-amplified NSCLC and gastric cancer. The maximum tolerated dose was established at 570 mg/m² administered intravenously once weekly; the safety profile was considered favorable overall but included common adverse events such as fatigue/asthenia and gastrointestinal symptoms[5][8][10].

Other names
Urea, N-[6-[[6-(4-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazin-3-yl]thio]-2-benzothiazolyl]-N'-[2-(4-morpholinyl)ethyl]-1-(6-{[6-(4-fluorophenyl)[1,2,4]triazolo[4,3-b]pyridazin-3-yl]sulphanyl}-1,3-benzothiazol-2-yl)-3-[2-(morpholin-4-yl)ethyl]ureaUNII-XH93U6NIJEUNII-XH-93U6NIJEUNII-XH 93U6NIJE
02

Targets

MET (Mesenchymal-epithelial transition factor receptor)

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