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Drug intelligence / Profile preview
binimetinib + ipilimumab + nivolumab
- Development stage
- Phase 2
- Lead developer
- Pfizer
- Modality
- Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
- Administration
- Oral, Intravenous
01
Overview
This is a combination regimen of three drugs: binimetinib, a selective MEK1/2 inhibitor; ipilimumab, a monoclonal antibody targeting cytotoxic T lymphocyte-associated antigen 4 (CTLA4); and nivolumab, a monoclonal antibody targeting programmed cell death protein 1 (PD1). Binimetinib inhibits the MAPK pathway by blocking MEK1/2 activity, which is often upregulated in cancers with RAS or BRAF mutations. Ipilimumab and nivolumab are immune checkpoint inhibitors that enhance anti-tumor immune responses by blocking CTLA4 and PD1 pathways respectively. This triplet combination has been studied primarily in advanced melanoma and metastatic colorectal cancer to assess whether combining targeted therapy with dual immunotherapy can improve outcomes compared to immunotherapy alone[6][7]. The regimen has shown limited efficacy in RAS-mutant microsatellite-stable metastatic colorectal cancer but remains under investigation for melanoma.
- Brand names
- Mektovi (binimetinib)Yervoy (ipilimumab)Opdivo (nivolumab)
- Other names
- binimetinib + ipilimumab + nivolumab
02
Targets
CTLA-4 (Cytotoxic t-lymphocyte–associated protein 4)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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