The role and efficacy of Binimetinib

Binimetinib and encorafenib target two different kinases in the RAS/RAF/MEK/ERK pathway. Furthermore, the combination of bimetinib and encorafenib delayed the emergence of drug resistance in mouse BRAF V600E mutant human melanoma xenografts compared with either drug alone. In a BRAF V600E mutant NSCLC patient-derived mouse xenograft model, the combination of bimetinib and encorafenib resulted in greater antitumor activity in terms of tumor growth inhibition compared with bimetinib alone. Tumor growth delay was increased after combined administration compared with administration alone.

In vitro, bimetinib inhibits extracellular signal-related kinase (ERK) phosphorylation in cell-free assays, as well as viability and MEK-dependent phosphorylation of BRAF-mutated human melanoma cell lines. Bimetinib also inhibited ERK phosphorylation and tumor growth in vivo in a BRAF mutant mouse xenograft model. MEK is an enzyme that regulates the biosynthesis of inflammatory cytokines such as TNF, IL-6, and IL-1; therefore, the antitumor activity of bimetinib may be mediated by interfering with cytokine biosynthesis. No clinically significant QT prolongation was observed with bimetinib45 mg twice daily.

The original drug bimetinib has not yet been launched in China, and therefore is not covered by medical insurance. Bimetiniboriginal drug sold overseas, specifications15mg*84 tablets may cost more than 10,000 yuan per box (the price may fluctuate due to exchange rates), which is relatively expensive. There is currently no generic drug of Bimetinib produced and launched. For more drug information and specific prices, please consult a medical consultant.