1497436-02-8Relevant articles and documents
Synthesis and biopharmaceutical studies of jltn as potential dasatinib prodrug
Liu, Fei,Lang, Li-Wei,Jiang, Ji,Lu, Hua-Jun,Wang, Jian-Min,Wang, Shih-Chen
, p. 877 - 881 (2013/09/12)
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.