Your browser doesn't support javascript.
loading
Show: 20 | 50 | 100
Results 1 - 1 de 1
Filter
Add more filters










Database
Language
Publication year range
1.
Bioorg Med Chem Lett ; 27(5): 1175-1178, 2017 03 01.
Article in English | MEDLINE | ID: mdl-28169165

ABSTRACT

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.


Subject(s)
Antineoplastic Agents/pharmacology , Everolimus/analogs & derivatives , Prodrugs/chemical synthesis , Prodrugs/pharmacology , Animals , Antineoplastic Agents/pharmacokinetics , Biological Availability , Cell Line, Tumor , Everolimus/pharmacokinetics , Humans , Mice , Mice, Nude , Solubility
SELECTION OF CITATIONS
SEARCH DETAIL
...