molecules of the month

An Active Prodrug, Triple Reuptake Inhibitor for Major Depressive Disorder  While SNRIs and selective serotonin reuptake inhibitors (SSRIs) have been hugely successful in treating major depressive disorder (MDD), many patients remain resistant to treatment or do not experience full symptom relief. The majority of current treatments for MDD increase levels of synaptic serotonin and/or norepinephrine by inhibiting their reuptake transporters SERT and NET, respectively.  Ansofaxine (LY03005) is a new triple reuptake inhibitor (TRI) optimized from a serotonin-norepinephrine reuptake inhibitor (SNRI) by employing an interesting active prodrug strategy. In contrast to traditional prodrugs, which tend to be inactive on their own but release an active metabolite, LY03005 not only increases the exposure of its parent SNRI metabolite, desvenlafaxine, in the brain,…