Drug intelligence / Profile preview

glesatinib

Development stage
Phase 2
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Oral
01

Overview

Glesatinib is an orally bioavailable, small-molecule, multitargeted tyrosine kinase inhibitor with potential antineoplastic activity. It primarily targets the mesenchymal epithelial transition factor (MET) and AXL receptor tyrosine kinases, as well as other kinases such as Tek/Tie2 and vascular endothelial growth factor receptors (VEGFR1/2/3). By inhibiting these kinases, glesatinib disrupts signaling pathways involved in tumor cell proliferation and angiogenesis. It has been investigated mainly for the treatment of advanced or metastatic non-small cell lung cancer (NSCLC) with MET dysregulation (mutations or amplification), both as monotherapy and in combination regimens. Glesatinib has shown modest clinical activity in phase 2 trials for NSCLC patients with MET alterations[2][3][4][5][7].

Other names
glesatinib
02

Targets

TEK (Tie2)MST1R (Recepteur d'origine nantais)AXL (AXL receptor tyrosine kinase)MET (Mesenchymal-epithelial transition factor receptor)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR3 (Vascular endothelial growth factor receptor 3)

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