Pharmaleads announces the inclusion of the first patient in Phase IIa study of oral PL37 for pain in diabetic neuropathy
World premiere for Dual Enkephalinase Inhibitors (DENKIs), a new class of analgesics and first novel concept for decades in the treatment of chronic pain.
Paris, 22 April 2015 – Pharmaleads, a company specialising in the discovery and early-stage development of small molecule inhibitors of metalloproteases for the treatment of severe pain, announces today 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).
PL37 is the first DENKI 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 (entodogenous 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.