Effect of Cyclosporine and Rifampin on the Pharmacokinetics of Macitentan, a Tissue-Targeting Dual Endothelin Receptor Antagonist

@inproceedings{Bruderer2011EffectOC,
  title={Effect of Cyclosporine and Rifampin on the Pharmacokinetics of Macitentan, a Tissue-Targeting Dual Endothelin Receptor Antagonist},
  author={Shirin Bruderer and P{\"a}ivi {\"A}{\"a}nismaa and Marie-Claude Homery and Stephanie H{\"a}usler and Kyle A. Landskroner and Patricia N. Sidharta and Alexander Treiber and Jasper Dingemanse},
  booktitle={The AAPS Journal},
  year={2011}
}
Macitentan is a dual endothelin receptor antagonist under phase 3 investigation in pulmonary arterial hypertension. We investigated the effect of cyclosporine (Cs) and rifampin on the pharmacokinetics of macitentan and its metabolites ACT-132577 and ACT-373898 in healthy male subjects. In addition, in vitro studies were performed to investigate interactions between macitentan and its active metabolite ACT-132577 with human organic anion-transporting polypeptides (OATPs). The clinical study (AC… CONTINUE READING
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