Trametinib

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Trametinib
Trametinib.svg
Systematic (IUPAC) name
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
Clinical data
Trade names Mekinist
Pregnancy cat. D (US)
Legal status -only (US)
Identifiers
CAS number 871700-17-3
ATC code L01XE25
PubChem CID 11707110
ChemSpider 9881833
UNII 33E86K87QN YesY
ChEBI CHEBI:75998
Synonyms GSK1120212
Chemical data
Formula C26H23FIN5O4 
Mol. mass 615.39 g/mol

Trametinib (trade name Mekinist) is a cancer drug. It is a MEK inhibitor drug with anti-cancer activity.[1]

It inhibits MEK1 and MEK2.[1]

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 gene has become replaced by glutamic acid (E) making the mutant BRAF gene constituitively active.[2]

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.[3] Clinical trial data demonstrated that progression on single-agent trametinib occurs within 6 to 7 months.[4] To overcome this, trametinib was combined with the BRAF inhibitor dabrafenib.[4] 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.[5]

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