Encorafenib (LGX818)

Description: Encorafenib (formerly LGX818; LGX-818; trade name Braftovi), an approved anticancer drug, is a highly potent, and orally bioavailable B-RAFV600E inhibitor with potential antineoplastic activity. It inhibits B-Raf V600E with an IC50 of 4 nM. It has little effect against wild-type BRAF. As of June 2018, Encorafenib was approved by FDA to treat unresectable or metastatic melanoma. Encorafenib has selective anti-proliferative and apoptotic activity on cells expressing BRAFV600E. It shows no significant activity against a panel of 100 kinases and no suppression of cell growth with more than 400 cell lines expressing BRAFV600E. In human melanoma xenograft models, oral administration of Encorafenib shows strong decrease in phospho-MEK and induces tumor regression. Raf kinase is a serine/threonine enzyme in the RAFMAPK/ERK signaling pathway. By inhibiting the activation of the RAF/MAPK/ERK signaling pathway, encorafenib may result in a decrease in the proliferation of tumor cells.

References: 1 Cancer Res, 2012, 72(8 Supplement): 3790; 2 J Hematol Oncol. 2013 Apr 25; 6:30

Related CAS#: 1269440-29-0 (R-isomer)