December 1, 2010
Taranabant PK Study Published
Results of a population pharmacokinetic (PK) analysis of taranabant were published in the December 2010 issue of the AAPS Journal. Data from 12 phase 1 studies and one phase 2 study were pooled from subjects administered single and multiple oral doses of taranabant ranging from 0.5 to 8 mg. A total of 6,834 taranabant plasma concentrations from 187 healthy and 385 obese subjects were used to develop the population PK model in NONMEM. A standard covariate analysis using forward selection and backward elimination was conducted. A 3-compartment model with first-order absorption and elimination adequately described plasma taranabant concentrations. The population mean estimates for apparent clearance and apparent steady-state volume of distribution were 25.4 L/h and 2,578 L, respectively. Statistically significant covariate effects were modest in magnitude and not considered clinically relevant.
Taranabant is a cannabinoid-1 receptor inverse agonist developed for the treatment of obesity. The study was sponsored by Merck & Co in collaboration with Cognigen Corporation.
Li XS, Nielsen J, Cirincione B, Li H, Addy C, Wagner J, Hartford A, Erondu N, Gantz I, Morgan J, Stone J. Development of a population pharmacokinetic model for taranabant, a cannibinoid-1 receptor inverse agonist. AAPS J. 2010:12(4):537-547. doi: 10.1208/s12248-010-9212-2
