Polymer-of-prodrug (POP) materials enable new nucleoside reverse transcriptase inhibitor (NRTI) therapy strategies. The materials are prodrugs of NRTIs in the form of polymers. Suitable materials include products which are polymeric NRTI delivery systems comprising polymeric materials which are capable of degradation after administration to release NRTIs or NRTI prodrugs which themselves are capable of metabolism to the parent NRTIs. The NRTIs may optionally be selected from tenofovir (TFV), emtricitabine (FTC), lamivudine (3TC) and MK-8591 (EFdA). The invention facilitates long-acting (LA) regimens. Constructs of the materials may be in the form of injectable compositions or implants.
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Page/Page column 54-55; 57
(2020/07/14)
Novel trimethyl lock based enzyme switch for the self-assembly and disassembly of gold nanoparticles
A novel trimethyl lock based dual enzyme-responsive gold nanoparticles (AuNPs) conjugate was developed to control the self-assembly and disassembly of AuNPs in one population of nanoparticles, which can be easily monitored by naked eye, simple spectrophot
Application of the 'trimethyl lock' to Ganciclovir, a pro-prodrug with increased oral bioavailability
The synthesis and oral bioavailability of two potential prodrugs of Ganciclovir (1) based on the 'trimethyl lock' is described. The mono-3-(2'-Acetoxy-4'6'-dimethylphenyl)-3,3-dimethylpropanoic ester (2) showed a four-fold increase in oral bioavailability over the parent drug in rats.
Dillon, Michael P.,Cai, Haiying,Maag, Hans
p. 1653 - 1656
(2007/10/03)
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