A pharmacokinetic PET study of NK1 receptor occupancy

• DOI: 10.1007/s00259-011-1954-2
• Publication Date: 2011-10-12T08:33:39Z
• Authors: Stefano Zamuner; Eugenii A. Rabiner; Sofia A. Fernandes; Massimo Bani; Roger N. Gunn; Roberto Gomeni; Emilangelo Ratti; Vincent J. Cunnin...
• Keywords: Radioligand; Occupancy

Purpose There is growing recognition of the importance of integrating drug occupancy data acquired by positron emission tomography (PET) with the plasma pharmacokinetics of the drug, in order to establish proper dose selection in subsequent clinical trials. Here we present a study in human subjects of the occupancy of NK1 receptors achieved following different doses of casopitant, a selective NK1 antagonist.