J.B. Scott, J. Zadina
Tulane University,
United States
Keywords: Glycosylated cyclic peptides, opioid receptor agonists, endomorphin analogs, pain management, blood-brain barrier penetration
Summary:
This innovative technology features glycosylated cyclic peptides that function as mu opioid receptor agonists, offering a novel approach to pain management and opioid use disorder (OUD) treatment. The compounds are specifically designed with strategic glycosylation of endomorphin-based peptides to enhance blood-brain barrier penetration while maintaining high mu opioid receptor selectivity. Unlike traditional opioids that often lead to addiction and severe side effects, these specially designed endomorphin analogs provide effective pain relief with significantly reduced abuse potential and respiratory depression risks. The peptides incorporate multiple strategic modifications including cyclization, unnatural amino acid substitutions, and specific sugar moiety attachments that together enhance metabolic stability, bioavailability, and therapeutic efficacy. In preclinical studies, these compounds have demonstrated potent analgesic effects comparable to morphine but with reduced tolerance development and minimal reward-seeking behavior in animal models. The technology has shown promise in preliminary studies and has received significant funding from the National Institutes of Health and Veterans Affairs, demonstrating its potential clinical importance. Tuleviate represents a potentially revolutionary advancement in addressing the dual challenges of effective pain management and reducing opioid dependency in clinical practice, with applications for both acute and chronic pain conditions.