Encorafenib

Encorafenib

Clinical data
ATC code	None
Legal status
Legal status	Investigational
Identifiers
IUPAC name Methyl [(2S)-1-{[4-(3-{5-chloro-2-fluoro-3-[(methylsulfonyl)amino]phenyl}-1-isopropyl-1H-pyrazol-4-yl)-2-pyrimidinyl]amino}-2-propanyl]carbamate
PubChem CID	50922675
ChemSpider	28536139
Chemical and physical data
Formula	C22H27ClFN7O4S
Molar mass	540.011 g/mol
3D model (JSmol)	Interactive image
SMILES C[C@@H](CNc1nccc(n1)c2cn(nc2c3cc(cc(c3F)NS(=O)(=O)C)Cl)C(C)C)NC(=O)OC
InChI InChI=1S/C22H27ClFN7O4S/c1-12(2)31-11-16(17-6-7-25-21(28-17)26-10-13(3)27-22(32)35-4)20(29-31)15-8-14(23)9-18(19(15)24)30-36(5,33)34/h6-9,11-13,30H,10H2,1-5H3,(H,27,32)(H,25,26,28)/t13-/m0/s1 Key:CMJCXYNUCSMDBY-ZDUSSCGKSA-N

Encorafenib, also known as LGX818 is a drug candidate for the treatment of melanoma with the V600E mutation in the B-RAF kinase. The substance is being developed by Novartis and was disclosed at the spring 2013 American Chemical Society meeting in New Orleans.^[1][2][3]

It is a Selective BRAF Inhibitor,^[4] and is in phase III clinical trials.

Clinical trials

Several clinical trials of LGX818, either alone or in combinations with the MEK inhibitor MEK162,^[5] CDK4 inhibitor LEE011^[6] are being run. The initial results are encouraging^[4] and were presented at ASCO 2013.^[7] As a result of a successful Phase Ib/II trials, Phase III trials are currently being initiated.^[8]

References