Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
Notes
Synthesis and Biopharmaceutical Studies of JLTN as Potential Dasatinib Prodrug
Fei LiuLi-Wei LangJi JiangHua-Jun LuJian-Min WangShih-Chen Wang
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Keywords: Dasatinib, prodrug, JLTN
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2013 Volume 61 Issue 8 Pages 877-881

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Abstract

Dasatinib was identified as a potent orally administered Src/Abl kinase inhibitor with excellent antiproliferative activity against Philadelphia chromosome-positive chronic myelogenous leukemia in chronic phase. The low bioavailability of Dasatinib may be due to both incomplete oral absorption and first-pass metabolism. A prodrug, JLTN, was synthesized to minimize the first-pass effect of Dasatinib and improve the oral bioavailability following oral administration via targeting intestinal peptide transporter and enhancing chemical stability. Biological evaluation data indicated that there was a 150%-fold increase in oral bioavailability of this prodrug compared to the parent drug Dasatinib in monkeys.

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© 2013 The Pharmaceutical Society of Japan
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