Bicifadine

Abstract

Bicifadine is a serotonin‐norepinephrine‐dopamine reuptake inhibitor. It is being developed as an analgesic to treat different pain conditions. Metabolism of [ 14 C]‐bicifadine in healthy adult male subjects was studied following a single oral dose of 200 mg. Hydroxylation and oxidation reactions yielded hydroxymethyl bicifadine, bicifadine lactam metabolite, carboxyl bicifadine, and carboxyl bicifadine lactam as the major circulating metabolites. Minor metabolites found in plasma and urine were glucuronide conjugate of carboxyl bicifadine and glucuronide conjugate of carboxyl bicifadine lactam.