Novel Painkiller with Little or No Signs of Addiction and Other Serious Opioid Side Effects Patented by Phoenix PharmaLabs

SALT LAKE CITY, April 8, 2015 /PRNewswire/ -- Phoenix PharmaLabs, Inc. ("Phoenix"), announced today that the United States Patent Office issued a Composition patent on March 24, 2015 for the Company's advanced analog known as PPL-103 that belongs to a unique new class of opioids for the treatment of pain as well as opioid addiction.

The leading potent opioid analgesics in use today such as Morphine, Oxycodone, Hydrocodone, Methadone, Fentanyl, etc. bind strongly to the mu receptor in the brain and then aggressively agonize that receptor, leading to a number of severe side effects. However, Phoenix has developed a novel family of New Molecular Entity (NME) opioids that have high binding affinity at all three opiate receptors: mu, kappa and delta.  These unique ligands have more balanced receptor activity than morphine and other opioids, with partial activity at mu, somewhat higher, but not full, kappa activity, and moderate delta activity. Thus, PPL-103 derives potent analgesia primarily from mu and kappa, but does not stimulate those receptors so intensely that they trigger the negative side effects of either receptor.  This profile results in first-ever opiate analgesics that appear to be non-addicting and free of all significant dangerous side effects.

Extensive animal efficacy studies of this family of opioids conducted by prominent scientists at leading institutions [1] demonstrated the following:

• Robust analgesic potency (10-20x stronger than morphine)
• Little or no euphoric reward (which leads to abuse and addiction)
• No dysphoria
• No death from overdose - even at 350x the analgesic dose
• No constipation – even at 100x dose

Also, the drugs did not precipitate withdrawal in dependent primates and therefore offer very promising use for addiction therapy as a preferred substitute for addictive opiates such as Methadone and Suboxone.

"Eliminating the incentive for pain drug abuse has to start with the underlying motivation," said Dr. John Lawson, Founder and CSO of Phoenix. "Any effective pain drug like PPL-103 that has no (or at least substantially reduced) ability to generate euphoria in users is unlikely to support abuse and addiction. No patients in pain will later abuse such a drug if it doesn't produce a "high" in them," he said. Further, PPL-103 has shown that it produces only moderate levels of respiratory depression at highly elevated dosages (150x analgesic dose). "The ability to deliver high-quality pain relief without the threat of death from respiratory depression alone is a major improvement over existing available therapies," said Bill Crossman, CEO of Phoenix.

Recent focus on abuse-deterrent formulations (ADFs):
Recently the focus of pharma companies has been to attempt to reduce opioid abuse and addiction through the development and promotion of extended-release (ER) and/or abuse-deterrent formulations (ADFs). But drug seekers have been reported to actually prefer the ER formulations because tampering with these products provides them with a higher maximum concentration of the drug, and while ADFs can discourage abuse, the drugs are still addicting and they can still be abused. In fact, black-market methods to circumvent some leading ADFs can be found right online. [2] "While the various ADF strategies are helpful, they are really just attacking the abuse and addiction problem from the periphery, whereas Phoenix's technology goes directly to the core solution to the problem," said Crossman. "If ADFs are deemed to be a beneficial strategy then why not use those strategies in combination with an Active Pharmaceutical Ingredient (API) like PPL-103 instead of highly addictive opiates like morphine, oxycodone or hydrocodone?"

"We want to get PPL-103 into human clinical trials as quickly as possible. The predictive validity from animals to humans is quite high for opioids, and therefore we believe that there is a high probability that PPL-103 will be safe, effective and beneficial for humans," said Crossman.

[1] Larry Toll and colleagues at SRI International and Torrey Pines Institute for Molecular Studies, Lou Harris and colleagues at Virginia Commonwealth University (VCU), and Jim Woods and colleagues at the University of Michigan

[2] Fudin J Abuse-Deterrent Opioid Formulations: Purpose, Practicality, and Paradigms [internet]. 2015. [Accessed 2015 March 24]. Available from: http://www.pharmacytimes.com/contributor/jeffrey-fudin/2015/01/abuse-deterrent-opioid-formulations-purpose-practicality-and-paradigms

www.phoenixpharmalabs.com

Bill Crossman
860-305-6955
[email protected]
 

SOURCE Phoenix PharmaLabs, Inc.

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http://www.phoenixpharmalabs.com