Netupitant PET imaging and ADME studies in humans

@inproceedings{Spinelli2014NetupitantPI,
  title={Netupitant PET imaging and ADME studies in humans},
  author={Tulla Spinelli and Selma Calcagnile and Claudio Giuliano and Giorgia Rossi and Corinna Lanzarotti and Stuart Mair and Lloyd Stevens and Ian C. T. Nisbet},
  booktitle={Journal of clinical pharmacology},
  year={2014}
}
Netupitant is a new, selective NK1 receptor antagonist under development for the prevention of chemotherapy-induced nausea and vomiting. Two studies were conducted to evaluate the brain receptor occupancy (RO) and disposition (ADME) of netupitant in humans. Positron emission tomography (PET) imaging with the NK1 receptor-binding-selective tracer [(11) C]-GR205171 was used to evaluate the brain penetration of different doses of netupitant (100, 300, and 450 mg) and to determine the NK1 -RO… CONTINUE READING