Paris, France, 29 June 2017 – Pharmaleads, an emerging pharmaceutical company developing innovative products for the management of acute and chronic severe pain, today announced it has successfully completed a Phase I single ascending dose (SAD) trial in France with its oral DENKI candidate PL265 that is being developed for the treatment of neuropathic pain. The Company is now preparing to start a Phase I multiple ascending dose (MAD) study with oral PL265 in the UK. Data from the MAD study is expected in 2018.
The Phase I SAD results have shown that single doses of PL265, administered orally were safe and well-tolerated. Pharmacokinetic and pharmacodynamic studies showed that PL265, which is a pro-drug, was slowly transformed in plasma into its active metabolite (PL254). PL254 inhibited both of its target enzymes, aminopeptidase N (APN) and neprilysin (NEP), which are responsible for the physiological degradation of enkephalins. This inhibition was effective for more than 24 hours after single doses of 400 and 800mg of PL265, making it an ideal oral candidate for the treatment of neuropathic chronic pain.
Pharmaleads’ DENKIs, are the only drugs in clinical development that can inhibit both enkephalin-degrading enzymes APN and NEP, thereby increasing the local concentration of enkephalins resulting in local and sustained pain relief without the side-effects observed with opioids. PL265 is the second DENKI to start human clinical development at Pharmaleads.