Drug intelligence / Profile preview

binimetinib

Development stage
Approved
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

Binimetinib is an orally administered small molecule inhibitor of mitogen-activated protein kinase kinase 1 and 2 (MEK1 and MEK2), which are key components of the RAS/RAF/MEK/ERK signaling pathway involved in cell proliferation and survival. By selectively inhibiting MEK1/2, binimetinib blocks downstream ERK phosphorylation, leading to reduced tumor cell proliferation and decreased production of inflammatory cytokines. It is primarily used in combination with encorafenib for the treatment of unresectable or metastatic melanoma with BRAF V600E or V600K mutations, as well as for metastatic non-small cell lung cancer (NSCLC) with a confirmed BRAF V600E mutation. Binimetinib was developed by Array BioPharma and is marketed under the brand name Mektovi. The drug received FDA approval on June 27, 2018.

Brand names
Mektovi
Other names
binimetinib
02

Targets

MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)

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