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binimetinib

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Associated Genetic Biomarkers
Associated Diseases

Overview

Generic Name(s):
binimetinib
Trade Name(s):
Mektovi
NCI Definition [1]:
An orally available inhibitor of mitogen-activated protein kinase kinase 1 and 2 (MEK1/2) with potential antineoplastic activity. Binimetinib, noncompetitive with ATP, binds to and inhibits the activity of MEK1/2. Inhibition of MEK1/2 prevents the activation of MEK1/2 dependent effector proteins and transcription factors, which may result in the inhibition of growth factor-mediated cell signaling. This may eventually lead to an inhibition of tumor cell proliferation and an inhibition in production of various inflammatory cytokines including interleukin-1, -6 and tumor necrosis factor. MEK1/2 are dual-specificity threonine/tyrosine kinases that play key roles in the activation of the RAS/RAF/MEK/ERK pathway and are often upregulated in a variety of tumor cell types.

Biomarker-Directed Therapies

Clinical Trials

View Clinical Trials for binimetinib

Binimetinib has been investigated in 55 clinical trials, of which 48 are open and 7 are closed. Of the trials investigating binimetinib, 2 are early phase 1 (2 open), 13 are phase 1 (10 open), 15 are phase 1/phase 2 (12 open), 22 are phase 2 (21 open), and 3 are phase 3 (3 open).

BRAF V600E, KRAS Mutation, and BRAF V600K are the most frequent biomarker inclusion criteria for binimetinib clinical trials.

Malignant solid tumor, non-small cell lung carcinoma, and melanoma are the most common diseases being investigated in binimetinib clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Binimetinib
Top Biomarker Inclusion Criteria for Closed Clinical Trials Investigating Binimetinib
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating binimetinib and the cancer types associated with these biomarkers. These numbers are derived from a set of 5,956 clinical trials for which biomarker status defines treatment.

Drug Details

Synonyms [2]:
mek162, MEKTOVI, arry-162, arry-438162, mek inhibitor arry-438162
Drug Categories [2]:
MEK inhibitors, Serine/threonine kinase inhibitors, Tyrosine kinase inhibitors
Drug Target(s) [2]:
MAP2K1, MAP2K2
NCIT ID [1]:
C84865

References

1. National Cancer Institute. NCI Thesaurus Version 18.11d. https://ncit.nci.nih.gov/ncitbrowser/. [2018-07-30] [2018-08-02].

2. All assertions and clinical trial landscape data are curated from primary sources. You can read more about the curation process here.