First Clinical Experience With TRV130: Pharmacokinetics and Pharmacodynamics in Healthy Volunteers

@article{Soergel2014FirstCE,
  title={First Clinical Experience With TRV130: Pharmacokinetics and Pharmacodynamics in Healthy Volunteers},
  author={David G. Soergel and Ruth Ann Subach and Brian M. Sadler and John Connell and Alan S Marion and Conrad L. Cowan and Jonathan D. Violin and Michael W. Lark},
  journal={The Journal of Clinical Pharmacology},
  year={2014},
  volume={54}
}
TRV130 is a G protein‐biased ligand at the µ‐opioid receptor. In preclinical studies it was potently analgesic while causing less respiratory depression and gastrointestinal dysfunction than morphine, suggesting unique benefits in acute pain management. A first‐in‐human study was conducted with ascending doses of TRV130 to explore its tolerability, pharmacokinetics, and pharmacodynamics in healthy volunteers. TRV130 was well‐tolerated over the dose range 0.15 to 7 mg administered intravenously… 
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