Lipophilic nalmefene prodrugs to achieve a one-month sustained release.

  title={Lipophilic nalmefene prodrugs to achieve a one-month sustained release.},
  author={Tim Gaekens and M. Guillaume and H. Borghys and L. D. De Zwart and R. de Vries and R. Embrechts and A. Vermeulen and A. Megens and J. Leysen and P. Herdewijn and P. Annaert and J. Atack},
  journal={Journal of controlled release : official journal of the Controlled Release Society},
  • Tim Gaekens, M. Guillaume, +9 authors J. Atack
  • Published 2016
  • Chemistry, Medicine
  • Journal of controlled release : official journal of the Controlled Release Society
Nalmefene is an opioid antagonist which as a once-a-day tablet formulation has recently been approved for reducing ethanol intake in alcoholic subjects. In order to address the compliance issue in this patient population, a number of potential nalmefene prodrugs were synthesized with the aim of providing a formulation that could provide plasma drug concentrations in the region of 0.5-1.0ng/mL for a one-month period when dosed intramuscular to dogs or minipigs. In an initial series of studies… Expand
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