LGX818

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Systematic (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
Clinical data
Legal status
  • Investigational
Identifiers
ATC code None
ChemSpider 28536139
Chemical data
Formula C22H27ClFN7O4S
Molecular mass 540.011 g/mol
  • C[C@@H](CNc1nccc(n1)c2cn(nc2c3cc(cc(c3F)NS(=O)(=O)C)Cl)C(C)C)NC(=O)OC
  • 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

  1. ↑ Liveblogging First-Time Disclosures of Drug Structures from #ACSNOLA, 2013, C. Drahl
  2. ↑ http://patentscope.wipo.int/search/en/detail.jsf?docId=WO2011023773
  3. ↑ http://patentscope.wipo.int/search/en/detail.jsf?docId=WO2011025927
  4. ↑ 4.0 4.1 http://www.novartis.com/downloads/investors/event-calendar/2012/6-bridging-science-and-patients.pdf
  5. ↑ http://www.cancer.gov/clinicaltrials/search/view?cdrid=728588&version=HealthProfessional&protocolsearchid=11645832
  6. ↑ http://www.cancer.gov/clinicaltrials/search/view?cdrid=745927&version=HealthProfessional&protocolsearchid=11645832
  7. ↑ http://www.arraybiopharma.com/_documents/Publication/PubAttachment571.pdf Preliminary Results From a Phase Ib/II, Open-Label, Dose-Escalation Study of the Oral Selective BRAF Inhibitor LGX818 in Combination With the Oral MEK1/2 Inhibitor MEK162 in BRAF V600–Dependent Advanced Solid Tumors
  8. ↑ http://clinicaltrials.gov/ct2/show/NCT01909453?term=LGX818&rank=1 Study Comparing Combination of LGX818 Plus MEK162 and LGX818 Monotherapy Versus Vemurafenib in BRAF Mutant Melanoma (COLUMBUS)
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