A SYNTHESIS OF A GLYCOSYLATED OXYTOCIN DERIVATIVE FOR THE TREATMENT OF OPIOID USE DISORDER

Abstract

Oxytocin is an endogenous cyclic neuropeptide that has important effects on the reproductive and nervous system as well as the other major organ systems of the body. Oxytocin is an archaic and important peptide that has been conserved for over 600 million years of evolution. Today, this peptide is used clinically as an i.v. infusion to induce labor, prevent post-partum bleeding, and to stimulate lactation. However, oxytocin's therapeutic potential is limited due to its low half-life in serum, poor blood-brain barrier (BBB) penetration, and low selectivity. Glycosylated oxytocin derivatives, such as SSOxy-6, have been designed to avoid these issues and are of interest for many therapeutic applications. Currently, opioids are the main class of drugs used for analgesia, but these drugs carry dangerous side effects. Opioid use can lead to constipation, dependance, opioid-induced respiratory depression (OIRD), and overdose. Opioid use disorder (OUD) is a growing issue and prescription opioids are one of the most misused drugs in the U.S. Glycosylated oxytocin derivatives can potentially be used for the treatment of pain and as a safer alternative to opioids. In addition, glycosylated oxytocin derivatives can also be used as another tool in the treatment of OUD and could help reduce the prevalence of OUD in the U.S.