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glesatinib + erlotinib
- Development stage
- Unknown
- Lead developer
- Bristol Myers Squibb
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
Glesatinib (MGCD265) is an oral multitargeted receptor tyrosine kinase inhibitor that targets wild-type and mutant forms of MET, as well as VEGFR-1, VEGFR-2, VEGFR-3, Ron, and Tie-2. Erlotinib is a small molecule inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase. The combination of glesatinib and erlotinib is being investigated for the treatment of advanced malignancies such as non-small cell lung cancer (NSCLC) and gastroesophageal cancer. This combination aims to overcome resistance mechanisms by simultaneously inhibiting both MET/VEGFR pathways (glesatinib) and EGFR signaling (erlotinib), which has shown synergistic antitumor activity in preclinical models. Clinical studies have demonstrated disease control in patients with NSCLC treated with this combination[3][4][5].
- Brand names
- Tarceva
- Other names
- glesatinib + erlotinibMGCD265 + erlotinibMGCD265 and erlotinibMGCD-265 and erlotinibMGCD 265 and erlotinib
02
Targets
MST1R (Recepteur d'origine nantais)TEK (Tie2)AXL (AXL receptor tyrosine kinase)EGFR (Epidermal growth factor receptor)MET (Mesenchymal-epithelial transition factor receptor)
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