A novel CRTH2 antagonist: Single‐ and multiple‐dose tolerability, pharmacokinetics, and pharmacodynamics of ACT‐453859 in healthy subjects

  title={A novel CRTH2 antagonist: Single‐ and multiple‐dose tolerability, pharmacokinetics, and pharmacodynamics of ACT‐453859 in healthy subjects},
  author={M. G{\'e}hin and D. Strasser and J. Zisowsky and H. Farine and P. Groenen and J. Dingemanse and P. Sidharta},
  journal={The Journal of Clinical Pharmacology},
  • M. Géhin, D. Strasser, +4 authors P. Sidharta
  • Published 2015
  • Medicine
  • The Journal of Clinical Pharmacology
  • The chemoattractant receptor‐homologous molecule expressed on T‐helper 2 cells (CRTH2) is a G‐protein‐coupled receptor for prostaglandin D2, a key mediator in inflammatory disorders. In this randomized, double‐blind, placebo‐controlled study we investigated the single‐ and multiple‐dose tolerability, pharmacokinetics (PK), and pharmacodynamics (PD) up to a dose of 800 mg once a day of ACT‐453859, a potent and selective CRTH2 antagonist. ACT‐453859 was moderately rapidly absorbed and followed a… CONTINUE READING
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