Trade names Mekinist CAS Number 871700-17-3 UNII 33E86K87QN ATC code L01XE25 (WHO) Formula C26H23FIN5O4 ChemSpider ID 9881833 | Legal status US: ℞-only PubChem CID 11707110 Molar mass 615.39 g/mol Synonyms GSK1120212 ChEBI ID 75998 Trade name Mekinist | |
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Pregnancy
category US: D (Evidence of risk) | ||
Trametinib (trade name Mekinist) is a cancer drug. It is a MEK inhibitor drug with anti-cancer activity.
It inhibits MEK1 and MEK2.
Trametinib had good results for metastatic melanoma carrying the BRAF V600E mutation in a phase III clinical trial. In this mutation, the amino acid valine (V) at position 600 within the BRAF protein has become replaced by glutamic acid (E) making the mutant BRAF protein constitutively active.
In May 2013, trametinib was approved as a single-agent by the Food and Drug Administration for the treatment of patients with V600E mutated metastatic melanoma. Clinical trial data demonstrated that resistance to single-agent trametinib often occurs within 6 to 7 months. To overcome this, trametinib was combined with the BRAF inhibitor dabrafenib. As a result of this research, on January 8, 2014, the FDA approved the combination of dabrafenib and trametinib for the treatment of patients with BRAF V600E/K-mutant metastatic melanoma.