Powerful Overdose Treatment Raises Hope for Combating Opioid Crisis

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Scientists have found a way to make the most widely used opioid overdose treatment more effective, raising hopes that it could reduce the drug-related deaths that kill tens of thousands of people in the United States each year.

An international team of researchers has discovered a compound that makes naloxone more than seven times more effective, potentially allowing the antidote to be administered in lower doses.

Opioid addiction and its deadly consequences have become a focal point for U.S. politicians and health officials, with more than 70,000 Americans dying each year from overdoses involving the drug over the past several years. The crisis has been exacerbated by the rapid availability of powerful synthetic opioids such as fentanyl.

Naroxone is widely known by its brand name Narcan. Naroxone booster discovered, Published in Nature Professor Brian Kobilka, who led the study, said the research conducted Wednesday is part of a broader effort to use chemical means to combat the damaging effects of opioids.

“This approach will hopefully save lives, but it won’t solve the underlying problem of opioid addiction,” says Kobilka, who shared the 2012 Nobel Prize in Chemistry. His lab is developing nonopioid painkillers that eliminate the risk of addiction. Vertex Pharmaceuticals, a U.S. biotech, has a similar drug in late-stage clinical trials.

Kobilka and other scientists from the U.S., Japan, and Denmark sifted through a library of 4.5 billion candidate compounds and discovered a compound they called “368,” which binds to a specific type of opioid receptor site. Compound 368 amplifies naloxone’s ability to block addictive opioids like fentanyl and morphine, while minimizing withdrawal symptoms.

Kobilka noted that the recent breakthrough is still “very early in the drug development process,” but it raises the prospect of progress in addressing the scourge of opioid addiction in the U.S., Canada and other countries.

This is “an important advance and opens up new avenues of research in finding solutions to the opioid crisis,” said Catherine Cahill, a research scientist at the Jane & Terry Semel Institute for Neuroscience and Human Behavior in Los Angeles, in a commentary published in Nature.

Naloxone, one of two approved overdose reversal drugs, is a key tool used by U.S. health officials to combat the opioid epidemic. In April, the state of California signed a contract with a generic version manufacturer to expand free doses of the drug. Naloxone is available free of charge at pharmacies in several other states, including New Jersey and Nevada.

Last year, Narcan, manufactured by Emergent BioSolutions, was approved by the Food and Drug Administration to be sold over-the-counter. Emergent has blocked efforts to produce an over-the-counter version of Narcan for years in order to increase its profits. A two-dose box of Narcan costs $44.99.

Emergent, which had nearly $500 million in sales from Narcan last year, said in a statement that “this early research looks promising and is critical to advancing the science of naloxone to address the opioid crisis.”

The authors added that they could not comment further on the study because they used a naloxone product that is administered by subcutaneous injection while manufacturing Narcan in nasal spray form.

Michael Litterer, vice president of RWJBarnabas Health Institute for Prevention and Recovery, one of New Jersey’s largest health systems, said the most significant benefit of the enhanced version of naloxone will be as an antidote to the “rapid potency of fentanyl.”

“There is a general lack of availability of naloxone, let alone in sufficient quantities to counter high-potency fentanyl,” he added.

Ryan Hanson, an assistant professor of pharmacy at the University of Washington in Seattle, said that when a user overdoses on fentanyl, emergency services sometimes “don’t have enough naloxone to save the person.” “When you put these products together, you save a lot of lives,” he added.