Pharmacology of Macitentan, an Orally Active Tissue-Targeting Dual Endothelin Receptor Antagonist

  title={Pharmacology of Macitentan, an Orally Active Tissue-Targeting Dual Endothelin Receptor Antagonist},
  author={Marc Iglarz and Christoph Binkert and Keith Morrison and Walter Fischli and John Gatfield and Alexander Treiber and Thomas Weller and Martin H. Bolli and Christoph Boss and Stephan Buchmann and Bruno Capeleto and Patrick Hess and Changbin Qiu and Martine Clozel},
  journal={Journal of Pharmacology and Experimental Therapeutics},
  pages={736 - 745}
  • M. IglarzC. Binkert M. Clozel
  • Published 1 December 2008
  • Biology, Medicine, Chemistry
  • Journal of Pharmacology and Experimental Therapeutics
Macitentan, also called Actelion-1 or ACT-064992 [N-[5-(4-bromophenyl)-6-(2-(5-bromopyrimidin-2-yloxy)ethoxy)-pyrimidin-4-yl]-N′-propylaminosulfonamide], is a new dual ETA/ETB endothelin (ET) receptor antagonist designed for tissue targeting. Selection of macitentan was based on inhibitory potency on both ET receptors and optimization of physicochemical properties to achieve high affinity for lipophilic milieu. In vivo, macitentan is metabolized into a major and pharmacologically active… 

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