Date: 2015-04-22
Type of information: Treatment of the first patient
phase: 2
Announcement: treatment of the first patient
Company: Pharmaleads (France)
Product: PL37
Action
mechanism: enzyme inhibitor/dual enkephalinase inhibitor. PL37 is the first DENKI ( Dual Enkephalinase Inhibitors) to reach Phase IIa. DENKIs target specifically the nociceptors (receptors reacting to painful stimuli) located on peripheral nerve endings. They increase the concentrations of enkephalins (endogenous morphine) only where they are produced in large concentrations in response to a painful stimulus. In the absence of PL37, enkephalins are very rapidly inactivated by two enzymes called enkephalinases. By inhibiting these enkephalinases, DENKIs induce lasting analgesic effects, as potent as those of morphine but without its side effects.
Disease: diabetic neuropathy
Therapeutic area: CNS diseases - Metaboic diseases
Country: France, UK
Trial details:
Latest
news: * On April 22, 2015, Pharmaleads, a company specialising in the discovery and early-stage development of small molecule inhibitors of metalloproteases for the treatment of severe pain, announced the inclusion of the first patient in Phase IIa clinical study of oral PL37 in diabetic neuropathy. This Phase II clinical study follows a major Phase I programme which demonstrated the tolerance and safety of PL37 in 136 healthy volunteers. This first Phase II study during which patients will receive PL37, the most advanced molecule in this new class of analgesics, is a world premiere for Dual Enkephalinase Inhibitors (DENKIs). This on-going clinical study will recruit 108 patients with diabetic neuropathy and poor pain relief provided by pregabalin or gabapentin, the most commonly prescribed treatments for neuropathic pain. Unfortunately, none of the treatments currently available to treat neuropathic pain are satisfactory. These drugs are truly effective in only less than a quarter of patients, and they are associated with major side effects (nausea, dizziness, somnolence), which reduce their therapeutic range. This Phase IIa study aims to demonstrate the superiority of PL37 versus placebo, when administered in combination with the standard treatment for diabetic neuropathy. This superiority is based on a remarkable synergy observed between PL37 and pregabalin or gabapentin. The difference between PL37 and placebo will be based on changes in the overall pain score evaluated by the patient during the treatment. A total of 12 study centres are currently active, or will be within the next few weeks, in hospitals in the UK, and 6 to 10 others will open before the summer in the diabetology department of university teaching hospitals in France. According to Michel Wurm, MD, Corporate Development Director at Pharmaleads, « One of the strengths of this study lies in the remarkable synergy (factor 6), demonstrated in rodents when PL37 is combined with gabapentin or pregabalin. This synergy is expected to provide a highly significant clinical benefit in this Phase IIa study when PL37 is added to the unsatisfactory previous treatment ».
