Drug intelligence / Profile preview

binimetinib + panitumumab

Development stage
Phase 2
Lead developer
Pfizer
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous
01

Overview

Binimetinib (MEK162) is a selective small molecule inhibitor of MEK1 and MEK2, key kinases in the MAPK/ERK signaling pathway. Panitumumab is a fully human monoclonal antibody that targets the epidermal growth factor receptor (EGFR), blocking ligand-induced activation and downstream signaling. The combination of binimetinib and panitumumab has been investigated primarily for metastatic colorectal cancer (mCRC), particularly in patients with RAS mutant or wild-type tumors. The rationale for this combination is to overcome resistance to EGFR inhibition by simultaneously targeting both EGFR and the MAPK pathway. Clinical studies have shown that this combination results in substantial toxicity and limited clinical activity, with most patients experiencing significant adverse events such as diarrhea, rash, nausea, vomiting, fatigue, and skin reactions[1][2][10]. The development status remains investigational.

Other names
binimetinib + panitumumabMEK162 + panitumumab
02

Targets

EGFR (Epidermal growth factor receptor)MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)

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