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binimetinib + mFOLFIRI
- Development stage
- Unknown
- Lead developer
- Pfizer
- Modality
- Small Molecules
- Administration
- Oral, Intravenous
01
Overview
Binimetinib (MEK162) is a selective and potent allosteric inhibitor of the kinases MEK1 and MEK2 in the MAP kinase pathway. It is used in combination with chemotherapy regimens such as modified FOLFIRI (mFOLFIRI), which consists of folinic acid (leucovorin), fluorouracil (5-FU), and irinotecan. This combination has been investigated primarily for advanced or metastatic colorectal cancer (mCRC) with KRAS mutations. Binimetinib inhibits ERK phosphorylation downstream of RAS/RAF mutations, potentially enhancing the antitumor activity of cytotoxic agents like 5-FU by targeting tumor cell proliferation pathways[2][4][8]. The regimen is under clinical investigation for its safety and efficacy in patients with KRAS-positive metastatic colorectal cancer[2].
- Other names
- MEK162 + mFOLFIRIbinimetinib + modified FOLFIRIMEK162 plus mFOLFIRIMEK-162 plus mFOLFIRIMEK 162 plus mFOLFIRI
02
Targets
TOP1 (DNA Topoisomerase I)MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)TS (Thymidylate synthase)
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