Drug intelligence / Profile preview

binimetinib + ipilimumab + nivolumab

Development stage
Unknown
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

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)CTLA-4 (Cytotoxic t-lymphocyte–associated protein 4)

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