期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 27, 期 5, 页码 1175-1178出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2017.01.069
关键词
Everolimus; Glutathione; mTOR; Prodrug; Injectable; Long-acting
资金
- Key Science and Technology Innovation Team of Zhejiang Province [2013TD10]
A novel water-soluble everolimus prodrug, glutathione-everolimus, was designed and synthesized by introducing an endogenous tripeptide with an acetyl as the linker. The improvement in water solubility allowed the conjugate to be developed into an injectable drug. The results of biological evaluation in vitro and in vivo suggested that the prodrug was more effective and long acting than everolimus. Meanwhile, the pharmacokinetics study in vivo confirmed that the delivery of everolimus through the injection of the prodrug can overcome the low bioavailability of oral everolimus. (C) 2017 Published by Elsevier Ltd.
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