Oral Oxytocin-Based Painkillers Offer Relief for Gut Pain

Researchers at the University of Queensland (UQ) have developed a new class of oral painkillers to treat chronic abdominal pain. The drugs are based on oxytocin, a peptide hormone known for its role in childbirth and breastfeeding. By modifying oxytocin’s chemical structure, the research team has made it stable in the gastrointestinal (GI) tract, paving the way for a safer and more effective treatment for gut-related pain.

Addressing limitations of current treatments

Chronic abdominal pain affects millions of people worldwide, with conditions like irritable bowel syndrome (IBS) and irritable bowel disease (IBD) impacting up to 15% of adults at some point in their lives. Current treatment options, such as anti-inflammatory drugs and opioids, are often associated with significant side effects, including the risk of addiction.

Led by Associate Professor Markus Muttenthaler from UQ’s Institute for Molecular Bioscience, the research team focused on peptides – molecules that are typically potent and selective with fewer side effects. Despite these advantages, peptides generally degrade rapidly in the gut, necessitating injectable forms of the medication. The team’s breakthrough has addressed this limitation, creating an oral formulation that retains efficacy.

Oxytocin re-engineered for oral use

Oxytocin, sometimes referred to as the “bonding hormone,” plays diverse roles in the body, including promoting uterine contractions and supporting social bonding. The UQ researchers identified the specific regions of the oxytocin molecule that are quickly broken down by gut enzymes. Using medicinal chemistry techniques, they modified these regions, enhancing the hormone’s stability without compromising its ability to activate oxytocin receptors.

This modification has led to the development of gut-stable molecules that can be taken orally and act directly in the colon. These molecules work without crossing the gut barrier into the bloodstream, reducing the risk of systemic side effects.

Implications for safe and targeted pain relief

This innovative approach offers a safer alternative to existing therapies, as it localizes the drug’s activity to the GI tract. By preventing pain without affecting other parts of the body, the treatment minimizes risks often seen with systemic drugs. The researchers believe this could be a game-changer for individuals with GI disorders.

“This is a very safe therapeutic approach as it reduces the risk of side effects in the rest of the body, a problem with many other systemic drugs,”

Dr. Markus Muttenthaler

Future directions for peptide-based drugs

While the primary focus is on abdominal pain, the team is exploring the potential of their gut-stabilization method to improve other peptide-based treatments for gastrointestinal disorders. The researchers are now seeking investment to advance pre-clinical studies and accelerate the development of this novel therapeutic approach.

Reference: Kremsmayr T, Schober G, Kaltenböck M, Hoare BL, Brierley SM, Muttenthaler M. Oxytocin analogues for the oral treatment of abdominal pain. Angew Chem Int Ed. 2024:e202415333. doi: 10.1002/anie.202415333

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