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afatinib + savolitinib
- Development stage
- Preclinical
- Lead developer
- Boehringer Ingelheim
- 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
Afatinib + savolitinib is an investigational oral combination therapy comprising two small molecule tyrosine kinase inhibitors. Afatinib is an irreversible inhibitor of the ErbB family of receptors—including EGFR (ErbB1), HER2 (ErbB2), and HER4 (ErbB4)—and blocks downstream signaling pathways involved in cell proliferation and survival. Savolitinib is a potent and highly selective inhibitor of the MET receptor tyrosine kinase. The combination targets tumors with co-alterations in EGFR and MET pathways—particularly non-small cell lung cancer (NSCLC) with activating EGFR mutations and acquired resistance mediated by MET amplification or overexpression. This dual blockade aims to overcome resistance to single-agent EGFR inhibition by simultaneously suppressing both oncogenic drivers[8][10][6].
- Brand names
- Gilotrif (afatinib)Orpathys (savolitinib)
- Other names
- afatinib + savolitinib
02
Targets
MET (Mesenchymal-epithelial transition factor receptor)EGFR T790M (Epidermal growth factor receptor T790M mutant)ERBB2 (Erb-b2 receptor tyrosine kinase 2)ERBB4 (Erb-b2 receptor tyrosine kinase 4)
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