Side Effect Free Opioid Drug Now in Clinical Trials


Founder of Health Rising and Phoenix Rising
Staff member
After realizing that it may be possible to activate opioid receptor pathways which do not cause the many side effects associated with opioids - but still reduce pain - researchers went on a big data study. First they mapped the tremendously complex receptor using a computer program - and then looked for molecules that would stick to the part of the receptor that triggered the "good pathway"

The team ran 3 million possibilities through the computer and picked the 23 best candidates to test in a lab. One chemical, PZM21, seems to do what they hoped: Turn the opioid receptor on without using much beta-arrestin. They report their findings in Nature on Wednesday.

They found one chemical, then tweaked it to make it more potent and then gave it to mice. The mice didn't display any of the behaviors associated with opioid side effects. (Mice get addicted to opioids as well).

"I think this was really a tour de force," says Gavril Pasternak, a researcher at the Memorial Sloan Kettering Cancer Center who's also trying to develop new opioids but was not involved in this study. "They're new entities with totally different pharmacological profiles. These are great promise for opiates over the course of the next five to 10 years."

Manglik and some of his collaborators have founded a company that will try to bring these new drugs to market, and the pharmaceutical company Trevena is running a very similar molecule through clinical trials now.


Founder of Health Rising and Phoenix Rising
Staff member
Quite a few drug companies are apparently working on this....No surprise there given the huge market; hopefully at least one will get it right. :)

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