Vabicaserin

Abstract

Vabicaserin is a potent 5‐hydroxytryptamine 2C receptor full agonist. It is currently under development for the treatment of psychotic symptoms. Vabicaserin was extensively metabolized in humans after oral administration of nonradiolabeled material. The primary biotransformation pathway of vabicaserin in humans was carbamoyl glucuronidation. The systemic exposure ratios of the carbamoyl glucuronide to parent drug ranged from 20 to 29. Minor plasma metabolites were isomers of hydroxyl vabicaserin, vabicaserin imine, vabicaserin nitrone, hydroxyl vabicaserin glucuronide, didehydrohydroxyl vabicaserin glucuronide, and hydroxyl vabicaserin imine. The urinary metabolic profile was similar to plasma profile, except that a hydroxyl vabicaserin carbamoyl glucuronide and two vabicaserin N‐glucuronides were observed in the urine.