MEK inhibitor + EGFR inhibitor

MEKi + EGFRi refers to the combination of a Mitogen-activated protein kinase kinase (MEK) inhibitor and an Epidermal Growth Factor Receptor (EGFR) inhibitor. This therapeutic strategy is primarily employed in the treatment of KRAS-mutated malignancies, such as pancreatic ductal adenocarcinoma (PDAC) and colorectal cancer. The rationale for this combination lies in the vertical inhibition of the MAPK/ERK signaling pathway; while MEK inhibitors block downstream signaling, they often trigger compensatory feedback activation of EGFR, which can lead to treatment resistance. By simultaneously inhibiting EGFR, the combination aims to achieve more durable suppression of the pathway. Specific examples of this combination include trametinib plus panitumumab or binimetinib plus cetuximab. In the context of KRAS G12R mutations, which are particularly prevalent in PDAC, this combination is being evaluated to improve patient outcomes where standard therapies have limited efficacy.

Other names

MEKi + EGFRiMEK inhibitor + EGFR inhibitorMEK/EGFR inhibition