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Erlotinib + trametinib
- Development stage
- Unknown
- Lead developer
- Novartis
- 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
Erlotinib + trametinib is a combination of two small molecule targeted therapies used in clinical research for the treatment of cancers with acquired resistance to epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors. Erlotinib is an EGFR tyrosine kinase inhibitor that blocks the activity of the epidermal growth factor receptor, thereby inhibiting cancer cell proliferation and survival. Trametinib is a MEK inhibitor that targets mitogen-activated protein kinase kinases 1 and 2 (MEK1/2), components of the MAPK/ERK pathway involved in cell division and survival. The combination has been studied primarily in patients with metastatic EGFR-mutant non-small cell lung cancer (NSCLC) who have developed resistance to prior EGFR TKI therapy[2][8]. The rationale for this combination is to overcome resistance mechanisms by dual inhibition of both EGFR and downstream MEK signaling pathways.
- Brand names
- MekinistTarceva
- Other names
- erlotinibtrametinib
02
Targets
MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)EGFR T790M (Epidermal growth factor receptor T790M mutant)
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