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pembrolizumab + binimetinib
- Development stage
- Phase 2
- Lead developer
- Merck
- Modality
- Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
- Administration
- Intravenous, Oral
01
Overview
Pembrolizumab + binimetinib is an investigational combination therapy consisting of two distinct agents: pembrolizumab, a humanized monoclonal antibody that targets the programmed cell death protein 1 (PD-1) receptor on lymphocytes, and binimetinib, a potent and selective small molecule inhibitor of mitogen-activated protein kinase kinases 1 and 2 (MEK1/2). Pembrolizumab acts as an immune checkpoint inhibitor by blocking PD-1, thereby enhancing T-cell–mediated antitumor immunity. Binimetinib inhibits the MAPK/ERK pathway by targeting MEK1/2, which can reduce tumor proliferation and modulate the tumor microenvironment to increase immune infiltration. This combination has shown promising activity in early-phase clinical trials for metastatic triple-negative breast cancer (TNBC), advanced non-small cell lung cancer (NSCLC), and other solid tumors. The rationale for combining these agents is based on preclinical evidence that MEK inhibition may enhance responses to immunotherapy by increasing tumor immunogenicity[1][2][4][5].
- Brand names
- Keytruda (for pembrolizumab)Mektovi (for binimetinib)
- Other names
- MEK162 + MK-3475
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)
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