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cobimetinib

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Associated Genetic Biomarkers
Associated Diseases

Overview

Generic Name(s):
cobimetinib
NCI Definition [1]:
An orally bioavailable small-molecule inhibitor of mitogen-activated protein kinase kinase 1 (MAP2K1 or MEK1), with potential antineoplastic activity. Cobimetinib specifically binds to and inhibits the catalytic activity of MEK1, resulting in inhibition of extracellular signal-related kinase 2 (ERK2) phosphorylation and activation and decreased tumor cell proliferation. Preclinical studies have demonstrated that this agent is effective in inhibiting the growth of tumor cells bearing a B-RAF mutation, which has been found to be associated with many tumor types. A threonine-tyrosine kinase and a key component of the RAS/RAF/MEK/ERK signaling pathway that is frequently activated in human tumors, MEK1 is required for the transmission of growth-promoting signals from numerous receptor tyrosine kinases.

Biomarker-Directed Therapies

Clinical Trials

View Clinical Trials for cobimetinib

Cobimetinib has been investigated in 55 clinical trials, of which 46 are open and 9 are closed. Of the trials investigating cobimetinib, 2 are early phase 1 (2 open), 8 are phase 1 (6 open), 11 are phase 1/phase 2 (10 open), 32 are phase 2 (27 open), and 2 are phase 3 (1 open).

BRAF Codon 600 Missense, BRAF V600E, and NRAS Mutation are the most frequent biomarker inclusion criteria for cobimetinib clinical trials.

Melanoma, malignant solid tumor, and breast carcinoma are the most common diseases being investigated in cobimetinib clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Cobimetinib
Top Biomarker Inclusion Criteria for Closed Clinical Trials Investigating Cobimetinib
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating cobimetinib 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]:
gdc-0973, cobimetinib (substance), mek inhibitor gdc-0973, mek inhibitor gdc-0973, cobimetinib, xl518, cobimetinib, cotellic, cobimetinib (product)
Drug Categories [2]:
MEK inhibitors, Serine/threonine kinase inhibitors, Tyrosine kinase inhibitors
Drug Target(s) [2]:
MAP2K1, MAP2K2
NCIT ID [1]:
C68923
SNOMED ID [1]:
R-FF715

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.