During the symposium “Next Generation Analgesics,” led by Dr. Nora Volkow, director of the National Institutes on Drug Abuse (NIDA), Lawrence Toll, Ph.D., co-founder and chief neuropharmacologist of Phoenix PharmaLabs, described the drug. His talk “PPL-103: A kappa partial agonist with potent antinociceptive activity and low abuse potential” focused on the promising success that has been achieved in a large number of published, as well as non-published, in vivo studies to date.
All opioids on the market today bind to the mu receptor in the brain and then aggressively stimulate that receptor. The mu receptor produces euphoria that leads to abuse and addiction. PPL-103 is a patented analog that binds strongly to all three opioid receptors in the brain (mu, kappa and delta) and then partially stimulates those receptors in a more balanced manner. This partial stimulation derives potent analgesic benefit from all three receptors, but is not sufficiently strong to produce the serious opioid side-effects associated with any single receptor. This results in a first-ever opiate analgesic that appears to be non-addicting and free of all significant dangerous side effects.
In vivo studies conducted to date have demonstrated that PPL-103 is:
- An orally active potent pain killer (10x stronger than morphine)
- Does not cause death from overdose (even when given at 350x dose)
- Does not cause physical dependence or withdrawal
- Does not cause constipation (even at 100X dose)
- Has demonstrated potential as an opioid addiction therapy drug, replacing currently used treatments that are themselves addictive opioids.
Phoenix PharmaLabs expects to file an IND to commence human clinical trials in the coming 18 months.
Phoenix PharmaLabs (www.phoenixpharmalabs.com) is a privately held, preclinical drug discovery company focused on the development and commercialization of new potent, non-addictive treatments for pain and new therapies for the treatment of addiction.