Experimental painkiller molecule as powerful as morphine, but not addictive

30 Aug 2018

Image: mwinkler/Shutterstock

As an opioid epidemic spreads across the western world, researchers believe they’re close to developing a non-addictive painkiller.

Figures from the US National Institute on Drug Abuse (NIDA) estimate that about 115 people in the country are overdosing on opioids every single day.

Aside from the financial costs such an addiction brings to a national healthcare system, it can be hugely traumatic for the person addicted to these drugs, and for their families.

Now, in an effort to hopefully eliminate the addictive nature of these drugs, a team of scientists from Wake Forest School of Medicine and NIDA has revealed what it believes is a major step towards achieving this goal.

In a paper published to Science Translational Medicine, the team described a new chemical compound called AT-121 that has dual therapeutic action. This allows it to suppress the addictive effects of opioids, but also produce morphine-like analgesic effects in non-human primates.

“In our study, we found AT-121 to be safe and non-addictive, as well as an effective pain medication,” said Mei-Chuan Ko of the research team.

“In addition, this compound also was effective at blocking abuse potential of prescription opioids, much like buprenorphine does for heroin, so we hope it could be used to treat pain and opioid abuse.”

A replacement for prescription opioids

The team had set out to create a compound to work on both the mu opioid receptor – found in most painkillers – and the nociception receptor, which opposes or blocks addiction of mu opioids.

Some of the most common drugs, such as fentanyl and oxycodone, only work with the mu opioid receptor, resulting in addiction.

To put into numbers its potential, AT-121 not only gave effective, non-addictive pain relief, but it also did so at a dose 100 times lower than that of morphine.

“The fact that this data was in non-human primates, a closely related species to humans, was also significant because it showed that compounds such as AT-121 have the translational potential to be a viable opioid alternative or replacement for prescription opioids,” Ko said.

The researchers now hope to further studies to test its safety, with the eventual aim of getting approval for human trials.

Colm Gorey was a senior journalist with Silicon Republic