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binimetinib + erlotinib

Development stage: Unknown
Lead developer: Moffitt Cancer Center
Modality: Small Molecules
Administration: Oral

Overview

A combination therapy consisting of binimetinib, a potent and selective MEK1/2 inhibitor, and erlotinib, an EGFR tyrosine kinase inhibitor. This combination targets dual inhibition of the MAP kinase pathway, which is activated in both EGFR and KRAS mutant populations. The rationale for combining these agents was to potentially overcome resistance mechanisms and achieve better tumor control in non-small cell lung cancer (NSCLC) patients with EGFR or KRAS mutations.

Brand names: Mektovi + Tarceva

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)ERBB2 (Erb-b2 receptor tyrosine kinase 2)MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)

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