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Clinical Trials

Date: 2011-11-24

Type of information:

phase: 1

Announcement:

Results

Company: Pharmaleads (France)

Product: PL37

Action mechanism:

PL37 is the leader of a new class of analgesics, the Dual ENKephalinase Inhibitors (DENKI). The compounds are able to induce a natural analgesia by inhibiting two enzymes responsible for the rapid degradation of enkephalins, the main endogenous opioids, thereby increasing the concentration of these powerful physiological analgesics, especially in the painful area.

Disease:

neuropathic pain

Therapeutic area: CNS diseases

Country: France, UK

Trial details: 126 of 168 healthy volunteers received PL37 orally in two randomized double-blind placebo-controlled studies. The first study consisted of administering a single increasing dose to 92 healthy volunteers including 16 women. Doses were up to 800 mg in men and 200 mg in women. The study also explored the interaction of PL37 with food. The linearity of the pharmacokinetics of the two active metabolites according to increasing doses of PL37 has been demonstrated.
The second study, conducted in Britain, consisted of three successive groups:
Group A, on 8 subjects. The maximum tolerated dose (MTD), which had not been reached on the first study, has been determined. This dose was greater than 1 g.
Group B was used to study 40 subjects in repeated doses over 5 days at doses of 800 mg to 4 g, administered in 4 doses.
Group C, including 28 subjects treated with 4 g daily for 5 days yielded the first evidence of efficacy in clinical pharmacology in the test to intradermal capsaicin.

Latest news:

Pharmaleads, biotechnology and medicinal chemistry company speciliazing in design and early development of small molecule protease inhibitors, has announced that its two Phase 1 studies for PL37 by oral route have yielded positive results. Both studies demonstrated the good safety and tolerability of PL37. A first proof of efficacy has been obtained in the second study. The group C showed a significant effect of oral PL37 compared with placebo, including a significant decrease in the intensity of pain and mechanical allodynia.

Pharmaleads is now actively preparing for the entry of PL37 into Phase 2a trials in the second quarter. The first phase I trials of PL265, the lead product of the second DENKI family, should begin in early 2012. The first molecule of a third DENKI family will also enter into regulatory preclinical development in 2012.

Is general: Yes