Pharmaleads presented the results at the recent Annual International Conference on Opioids.

The search for alternatives to opiod painkillers is underway. One company focusing efforts in this area is Paris-based Pharmaleads. In collaboration with researchers at the University Paris Descartes, France, the Universitat Pompeu Fabra, Barcelona, Spain, and the University of Michigan, US, the company is developing Dual ENKephalinase Inhibitors (DENKIs).

Enkephalins comprise a class of peptides produced by the body to relieve pain. These peptides are degraded by the enkephalinase enzymes aminopeptidase (APN) and neprilysin (NEP). DENKIs are designed to inhibit APN and NEP, preventing the degradation of enkephalins and increasing their local concentrations in areas only where pain is initiated, allowing the natural, physiological management of pain to occur. Opiates, on the other hand, act on opioid receptors throughout the entire body.

In a poster presentation at the recent Annual International Conference on Opioids in Boston, Pharmaleads reported on new clinical and preclinical data showing the efficacy, safety and tolerability of its DENKI candidates PL265 and PL37. 

The company and its collaborators presented data showing that the two DENKIs “are devoid of any abuse potential even at high doses and after repeated administration while providing similar levels of pain relief to opiates, but without their side-effects,” according to Pharmaleads Vice President of Medical Affairs Michel Wurm.

PL265 is being developed for the oral treatment of neuropathic pain, inflammatory diseases of the bowel and osteoarthritis pain, as well as the topical treatment of ocular and inflammatory pain. PL37 is being developed as an alternative to injectable opiates for the treatment of post-surgical, traumatic and cancer pain.