trametinib

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Associated Genetic Biomarkers

Associated Diseases

Overview

Generic Name(s):

trametinib

Trade Name(s):

Mekinist

NCI Definition [1]:

An orally bioavailable inhibitor of mitogen-activated protein kinase kinase (MEK MAPK/ERK kinase) with potential antineoplastic activity. Trametinib specifically binds to and inhibits MEK 1 and 2, resulting in an inhibition of growth factor-mediated cell signaling and cellular proliferation in various cancers. MEK 1 and 2, dual specificity threonine/tyrosine kinases often upregulated in various cancer cell types, play a key role in the activation of the RAS/RAF/MEK/ERK signaling pathway that regulates cell growth.

Biomarker-Directed Therapies

Trametinib can be used in the treatment of melanoma, cholangiocarcinoma, ganglioglioma, non-small cell lung carcinoma, and pilocytic astrocytoma. BRAF, BRAF V600E, and BRAF V600K are the most frequent biomarker inclusion criteria for use of trametinib [2].

Melanoma +

Disease is predicted to be sensitive to trametinib: -

Biomarker Criteria:

Sample must match one or more of the following:

BRAF V600E, BRAF V600K

Clinical Setting(s): Metastatic (FDA)

Note: Trametinib is FDA approved for single-agent use to treat patients with unresectable or metastatic melanoma with BRAF V600E/K; however, trametinib monotherapy is no longer an NCCN-recommended treatment option due to relatively poor efficacy compared with BRAF inhibitor monotherapy and BRAF/MEK inhibitor combination therapy.

Biomarker Criteria: Sample must match one or more of the following: BRAF V600E, BRAF V600K	Clinical Setting(s): Metastatic (FDA)
	Note: Trametinib is FDA approved for single-agent use to treat patients with unresectable or metastatic melanoma with BRAF V600E/K; however, trametinib monotherapy is no longer an NCCN-recommended treatment option due to relatively poor efficacy compared with BRAF inhibitor monotherapy and BRAF/MEK inhibitor combination therapy.

Clinical Trials

View Clinical Trials for trametinib

Trametinib has been investigated in 89 clinical trials, of which 73 are open and 16 are closed. Of the trials investigating trametinib, 2 are early phase 1 (2 open), 27 are phase 1 (24 open), 17 are phase 1/phase 2 (14 open), 40 are phase 2 (30 open), and 3 are phase 3 (3 open).

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

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

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Trametinib

Top Biomarker Inclusion Criteria for Closed Clinical Trials Investigating Trametinib

This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating trametinib 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]:

gsk1120212, Mekinist, trametinib (product), gsk-1120212, jtp74057, mek inhibitor gsk1120212, jtp-74057, trametinib, n-(3-{3-cyclopropyl-5-[(2-fluoro-4-iodophenyl)amino]-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydropyrido[4,3-d]pyrimidin-1(2h)-yl}phenyl)acetamide, trametinib, mek inhibitor gsk1120212, jtp 74057, gsk 1120212, trametinib (substance), trametinibum, tmt212

Drug Categories [2]:

MEK inhibitors, Serine/threonine kinase inhibitors, Tyrosine kinase inhibitors

Drug Target(s) [2]:

MAP2K1, MAP2K2

NCIT ID [1]:

C77908

SNOMED ID [1]:

R-FF6EF

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.

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