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Drug intelligence / Profile preview
pembrolizumab + FOLFIRI + binimetinib
- Development stage
- Phase 1
- Lead developer
- Merck
- Modality
- Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules, Monoclonal Antibodies → Antibody-Based Therapeutics
- Administration
- Intravenous, Oral
01
Overview
This drug is an **experimental combination regimen** comprising pembrolizumab (a PD-1 immune checkpoint inhibitor monoclonal antibody), FOLFIRI (a chemotherapy regimen consisting of leucovorin [folinic acid], fluorouracil [5-FU], and irinotecan), and binimetinib (a small-molecule MEK inhibitor). The combination is being studied for advanced or metastatic colorectal cancer, specifically microsatellite stable/mismatch-repair proficient colorectal cancer, where monotherapy response rates to immunotherapy have been poor. The rationale for the combination is to enhance anti-tumor immunity via pembrolizumab, augment cytotoxicity via FOLFIRI, and sensitize tumors to immunotherapy by inhibiting the MAPK pathway with binimetinib[1][3][5].
- Brand names
- Keytruda + FOLFIRI + Mektovi
- Other names
- pembrolizumab + FOLFIRI + binimetinib
02
Targets
MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)PDCD1 (Programmed cell death protein 1 receptor)TS (Thymidylate synthase)TOP1 (DNA Topoisomerase I)
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