A Population PK Model for Cariprazine and the Metabolites

Authors: Khariton T, Phillips L, Bihorel S, Fiedler-Kelly J, Kapás M, Periclou A, Ghahramani P
Conference: ACoP
Keywords: bootstrap, bootstrapping, CYP3A4, dopamine, GAM, IBW, manic, NONMEM, once daily, oral, PPK, psychiatry, psychotherapeutic agents, steady state, visual predictive check
Division: Clinical Pharmacology and Pharmacometrics (CPP)

Introduction

Cariprazine (CAR) is a potent dopamine D3/D2 receptor partial agonist with preferential binding to D3 receptors. Cariprazine was originally discovered by Gedeon Richter Plc. in Budapest, Hungary, and is under development by Forest Research Institute, Inc. (FRI) and Gedeon Richter Plc. for the treatment of schizophrenia, bipolar disorder, and major depressive disorder and also by Mitsubishi Tanabe Pharma Corporation for the treatment of schizophrenia in Japan. CAR possesses two major pharmacologically active metabolites, desmethyl cariprazine (DCAR) and didesmethyl cariprazine (DDCAR). Metabolism of cariprazine and its major active metabolites is mediated by two enzymes, CYP3A4 and, to a lesser extent, CYP2D6.

American Conference on Pharmacometrics (ACoP), Fort Lauderdale, Florida, May 2013

By Tatiana Khariton, Luann Phillips, Sébastien Bihorel, Jill Fiedler-Kelly, Margit Kapás, Antonia Periclou, Parviz Ghahramani