Synthesis and Biopharmaceutical Studies of JLTN as Potential Dasatinib Prodrug

DOI Web Site Web Site PubMed 参考文献2件
  • Liu Fei
    Department of Nuclear Medicine, Peking Union Medical College & Chinese Academy of Medical Sciences, Peking Union Medical College Hospital
  • Lang Li-Wei
    Department of Nuclear Medicine, Peking Union Medical College & Chinese Academy of Medical Sciences, Peking Union Medical College Hospital
  • Jiang Ji
    Clinical Pharmacology Research Center, Peking Union Medical College & Chinese Academy of Medical Sciences, Peking Union Medical College Hospital
  • Lu Hua-Jun
    BL Pharmaceuticals
  • Wang Jian-Min
    BL Pharmaceuticals
  • Wang Shih-Chen
    Department of Nuclear Medicine, Peking Union Medical College & Chinese Academy of Medical Sciences, Peking Union Medical College Hospital

この論文をさがす

抄録

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.

収録刊行物

参考文献 (2)*注記

もっと見る

キーワード

詳細情報 詳細情報について

問題の指摘

ページトップへ