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 namesMekinist
Pregnancy cat.
Legal status
Identifiers
CAS number871700-17-3
ATC codeL01XE25
PubChemCID 11707110
ChemSpider9881833
UNII33E86K87QN YesY
ChEBICHEBI:75998
SynonymsGSK1120212
Chemical data
FormulaC26H23FIN5O4 
Mol. mass615.39 g/mol
 
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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 namesMekinist
Pregnancy cat.
Legal status
Identifiers
CAS number871700-17-3
ATC codeL01XE25
PubChemCID 11707110
ChemSpider9881833
UNII33E86K87QN YesY
ChEBICHEBI:75998
SynonymsGSK1120212
Chemical data
FormulaC26H23FIN5O4 
Mol. mass615.39 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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