LGX818
 | |
| 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 |
|
| Identifiers | |
| ATC code | None |
| ChemSpider | 28536139 |
| Chemical data | |
| Formula | C22H27ClFN7O4S |
| Molar mass | 540.011 g/mol |
| |
| |
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
- ↑ Liveblogging First-Time Disclosures of Drug Structures from #ACSNOLA, 2013, C. Drahl
- ↑ http://patentscope.wipo.int/search/en/detail.jsf?docId=WO2011023773
- ↑ http://patentscope.wipo.int/search/en/detail.jsf?docId=WO2011025927
- 1 2 http://www.novartis.com/downloads/investors/event-calendar/2012/6-bridging-science-and-patients.pdf
- ↑ http://www.cancer.gov/clinicaltrials/search/view?cdrid=728588&version=HealthProfessional&protocolsearchid=11645832
- ↑ http://www.cancer.gov/clinicaltrials/search/view?cdrid=745927&version=HealthProfessional&protocolsearchid=11645832
- ↑ 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
- ↑ 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)
| ||||||||||||||||||||||||||||||