Drug General Information
Drug ID D04XVN
Drug Name Trametinib
Synonyms GSK 1120212; GSK-1120212; GSK1120212; JTP 74057; JTP-74057; Mekinist; Trametinib (GSK1120212); Trametinib (GSK1120212JTP 74057); Trametinib (MEK inhibitor); 33E86K87QN; A1-01871; AK174783; CHEBI:75998; UNII-33E86K87QN
Drug Type Small molecular drug
Company GlaxoSmithKline
Structure D04XVN
Drug Resistance Mutations
Target Name Dual specificity mitogen-activated protein kinase kinase 2 (MAP2K2) Target Info
Gene Name MAP2K2
Uniprot ID MP2K2_HUMAN
Species Homo sapiens
Reference Sequence MLARRKPVLPALTINPTIAEGPSPTSEGASEANLVDLQKKLEELELDEQQKKRLEAFLTQ
KAKVGELKDDDFERISELGAGNGGVVTKVQHRPSGLIMARKLIHLEIKPAIRNQIIRELQ
VLHECNSPYIVGFYGAFYSDGEISICMEHMDGGSLDQVLKEAKRIPEEILGKVSIAVLRG
LAYLREKHQIMHRDVKPSNILVNSRGEIKLCDFGVSGQLIDSMANSFVGTRSYMAPERLQ
GTHYSVQSDIWSMGLSLVELAVGRYPIPPPDAKELEAIFGRPVVDGEEGEPHSISPRPRP
PGRPVSGHGMDSRPAMAIFELLDYIVNEPPPKLPNGVFTPDFQEFVNKCLIKNPAERADL
KMLTNHTFIKRSEVEEVDFAGWLCKTLRLNQPGTPTRTAV [Homo sapiens]
Targeted Disease Skin cancer
Drug Resistance Mutations
Mutation info Missense: V35M [1]
Mutation info Missense: N126D [1]
Mutation info Missense: L46F [1]
Mutation info Missense: C125S [1]
Mutation Frequency 1 out of 4 patients
References
REF 1 The genetic landscape of clinical resistance to RAF inhibition in metastatic melanoma. Cancer Discov. 2014 Jan;4(1):94-109.

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