binimetinib + capecitabine

This is a combination therapy consisting of binimetinib (also known as MEK162), a selective inhibitor of mitogen-activated protein kinase kinases 1 and 2 (MEK1/2), and capecitabine, an oral prodrug that is converted to fluorouracil in the body. Binimetinib inhibits the RAS/RAF/MEK/ERK signaling pathway by targeting MEK1/2, thereby blocking cell proliferation and survival signals in tumor cells with pathway activation. Capecitabine is metabolized to 5-fluorouracil (5-FU), which interferes with DNA synthesis by inhibiting thymidylate synthase and incorporates into RNA to disrupt its function. The combination has been investigated primarily for gemcitabine-pretreated biliary tract cancer (BTC) and shows promising antitumor efficacy especially in patients with RAS/RAF/MEK/ERK pathway mutations[1][6]. The recommended phase 2 dose for this combination is binimetinib 30 mg twice daily plus capecitabine 1250 mg/m² twice daily on a two-weeks-on, one-week-off schedule[6].

Brand names

MektoviXeloda

Other names

MEK162 + capecitabinebinimetinib + capecitabine