This invention consists of a new class of potent opioid analgesics targeting a unique opioid receptor. With the ability to treat pain with reduced adverse effects traditionally associated with opioids, this target receptor and mechanism of action may usher in a new wave of drugs distinct from anything currently on the market or in the pipeline.
This invention’s current lead compounds are synthesized from naltrexone, an FDA-approved opioid receptor antagonist used to treat opiate addiction. Their activity is distinct from traditional opioids because they target a variant of the mu opioid receptor rather than the typical mu, kappa1, or delta receptors targeted by known opioids. The compounds’ effectiveness in alleviating pain with diminished side effects has been confirmed in animal models.
- 50-fold more potent than morphine
- No respiratory depression
- No physical dependence
- No cross-tolerance with morphine
- Limited constipation
Pain is the most common symptom for which patients seek medical attention. In 2014, sales of opioid analgesics reached $14.8B globally, with the US, UK, Germany, Canada, and France accounting for nearly 80% of the global market. Yet suboptimal treatment and other problems, such as addiction, abound. In the US alone, estimated economic loss resulting from pain and related complications exceeds $635B per year. With an estimated 80% of patients who take opioids experiencing at least one adverse effect, there is a need for new and improved pain-relief medications.
Pain relief in an array of pain models (acute, inflammatory, and neuropathic)
PCT application PCT/US2011/056827 filed 10/19/11 and published 04/26/12
U.S. application 13/879,908 filed 05/17/2014; ex-U.S. applications filed on 4/17/13
Gavril Pasternak, MD/PhD, Dept. of Neurology; Laboratory Head, Molecular Pharmacology Program, Memorial Sloan Kettering
Eileen Flowers, PhD, Licensing Manager