LY2165766

LY2165766 is a small molecule inhibitor of the glycine transporter 1 (GlyT1), developed by Eli Lilly through its Chorus LRL division for the treatment of schizophrenia. The drug's mechanism of action involves increasing the concentration of glycine in the synaptic cleft by blocking its reuptake into neurons and glial cells. Glycine acts as an obligatory co-agonist at the N-methyl-D-aspartate (NMDA) receptor; therefore, by elevating glycine levels, LY2165766 aims to enhance NMDA receptor signaling. This approach is intended to address the NMDA receptor hypofunction hypothesized to underlie the negative symptoms and cognitive impairments associated with schizophrenia. Clinical development reached Phase 1, including multiple-dose studies to evaluate the safety, tolerability, and pharmacokinetics of the compound in patients with schizophrenia.