Population PK/PD Modeling of Efficacy and Safety of CB1R Inverse Agonist Taranabant in Obese Patients

Conference: ACoP


  • Taranabant is a cannabinoid-1 receptor (CB1R) inverse agonist, that was being developed by Merck and Co., Inc. as a potential treatment of obesity[1].
  • Endocannabinoids have been implicated in the regulation of appetite and food intake. Exogenous cannabinoids, such as tetrahydrocannabinol, are agonists of brain cannabinoid-1 receptors (CB1R) and are associated with increases in food intake[2].
  • Taranabant has exhibited dose-dependent increases in both weight-loss and adverse experiences (AE) in clinical studies.
  • The objective of the present work was to develop exposureresponse models for both efficacy and safety (16 pre-specified AEs) to better characterize the therapeutic window of taranabant in overweight or obese patients.

American Conference on Pharmacometrics (ACoP), Mashantucket, Connecticut, October 2009

By Xiujiang Susie Li, Bo Jin, Lanyan Fang, Huafeng Zhou, Julie Passarell, Qiang Lu, Jing Su, Carol Addy, Ngozi Erondu, Shailaja Suryawanshi, Jill Fiedler-Kelly, Julie Stone