REVIEW 2-Methyl-2-(4-(3-methyl-2-oxo-8-(quinolin-3-yl)-2,3-dihydroimidazo[4,5-c]quinolin-1-yl)phenyl)propanenitrile (BEZ235) is an imidazo[4,5-c]quinoline derivative that inhibits PI3K and mTOR kinase activity by binding to the ATP-binding cleft of these enzymes. In cellular settings using human tumor cell lines, this molecule is able to effectively and specifically block the dysfunctional activation of the PI3K pathway, inducing G1 arrest. The cellular activity of NVP-BEZ235 translates well in in vivo models of human cancer. Thus, the compdound was well tolerated, displayed disease stasis when administered orally, and enhanced the efficacy of other anticancer agents when used in in vivo combination studies. Ex vivo pharmacokinetic/pharmacodynamic analyses of tumor tissues showed a time-dependent correlation between compound. concentration. and PI3K/Akt pathway inhibition. Collectively, the preclinical. data show that NVP-BEZ235 is a potent dual PI3K/mTOR modulator with favorable pharmaceutical properties. Recent have indicate that the activated PI3K/Akt/mTOR signaling pathway induced by various anticancer drugs explains resistance, and BEZ235 can be used to resensitize various cancer cells.
REFERENCES
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Sznol, Joshua A.; Jilaveanu, Lucia B.; Kluger, Harriet M. Studies of NVP-BEZ235 in melanoma, Current Cancer Drug Targets (2013), 13(2), 165-174.
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Lin SF, Huang YY, Lin JD, Chou TC, Hsueh C, Wong RJ, Utility of a PI3K/mTOR inhibitor (NVP-BEZ235) for thyroid cancer therapy. PLoS One. 2012;7(10):e46726.
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Sznol JA, Jilaveanu LB, Kluger HM.Studies of NVP-BEZ235 in melanoma. Curr Cancer Drug Targets. 2013 Feb;13(2):165-74.
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