G. Rossi, S. O. Tilola, Cecilia Rudengren
May 20, 2012
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Influential Citations
13
Citations
Journal
Journal of Clinical Oncology
Abstract
9054 Background: Netupitant (NETU) is a highly selective neurokinin 1 (NK1) receptor antagonist for the prevention of nausea and vomiting associated with emetogenic chemotherapy. In this study, PET imaging with the NK1 receptor-binding–selective tracer 11C-GR205171 was used to determine the levels and the duration of central NK1 receptor occupancy (RO) achieved by therapeutic doses of NETU. Methods: This was a single dose, randomized, open-label, PET study investigating the degree of NK1 RO in human brain after single oral doses of NETU (100, 300 or 450 mg) in 6 healthy male subjects. PET scans and blood samples for NETU determination were obtained up to 96 hrs post dose. The Patlak model was used to define the net uptake rate of 11C-GR205171 in the brain regions of interest while the percent of NK1 RO was calculated as the relative difference between the uptake rate at baseline and post-treatment administration. Results: NETU plasma concentrations over the 100 mg to 450 mg dose range were comparable with...