Trametinib
BRAF Inhibitor
DB08911
Approved Indication
Trametinib is indicated for the treatment of unresectable or metastatic melanoma with BRAF V600E or V600K mutations, as detected by an FDA-approved test.
2
Targets
0
Resistance Mutations
1
References
3D Structure
No structure available
No co-crystal structure available
Protein Targets
Mechanism of Action
Trametinib is a reversible, allosteric inhibitor of mitogen-activated extracellular signal regulated kinase 1 (MEK1) and MEK2 activation and of MEK1 and MEK2 kinase activity. MEK proteins are upstream regulators of the extracellular signal-related kinase (ERK) pathway, which promotes cellular proliferation. Trametinib helps with melanoma with the BRAF V600E or V600K as the mutation results in the constitutive activation of the BRAF pathway which includes MEK1 and MEK2.
Details
DrugBank ID
DB08911 ↗
Approval Date
2013-06-17
Molecular Weight
615.3948 g/mol
Drug Class
BRAF Inhibitor
ATC Codes
L01XE25
Synonyms
GSK 1120212, Trametinib Dimethyl Sulfoxide, Trametinibum
PubChem
CID: 11707110 ↗
ChEMBL
CHEMBL2103875 ↗
SMILES
CN1C(=O)C(C)=C2N(C(=O)N(C3CC3)C(=O)C2=C1NC1=CC=C(I)C=C1F)C1=CC(NC(C)=O)=CC=C1
ADMET Profile
Computing properties…
Drug References (DrugBank)