HPR Dr. Schaffler GmbH in cooperation with Zalicus announces positive results of Z944 Phase 1B Clinical Study in Pain

Positive results of Z944 Phase 1B Clinical Study in Pain

Efficacy Signals in Inflammatory and Neuropathic Pain Observed

Second U.S. Patent Issues for Z944 Providing Exclusivity to 2029

Munich, Germany – June 17th, 2014 – HPR Dr. Schaffler GmbH, a contract research organization, which conducts Phase 1 clinical trials in the field of CNS pain research, announced positive results of a Phase 1b clinical study for its customer Zalicus (Z944). Research object is a novel oral T-type calcium channel modulator in development for the treatment of pain. The Phase 1b study is an experimental clinical model utilizing Laser-Evoked-Potentials (LEP) to provide both objective and subjective assessments of the activity of Z944 in induced pain states. Based on these results, Zalicus is planning to advance a modified-release formulation of Z944 into Phase 2 clinical development in an appropriate pain indication in 2014. In addition, a second United States patent for Z944 (U.S. Patent number 8,569,344) covering methods of treating pain was issued on October 29, 2013, providing additional patent protection for Z944 in the United States until at least 2029.

“This is the first T-type calcium channel modulator to demonstrate clinical translation in pain, and these results are indicative of Z944’s potential activity in modulating pain signaling. We look forward to further evaluating a modified release formulation of Z944 in a relevant clinical pain syndrome in 2014,” commented Mark H.N. Corrigan, MD, President and CEO of Zalicus.

This exploratory, double-blind placebo-controlled, randomized cross-over, Phase 1b clinical study enrolled 16 healthy volunteers and was conducted in a single center in Germany.
The primary objective of the study was to compare the analgesic/anti-hyperalgesic properties of three different single doses of Z944 in a model of inflammatory pain and in a model of chronic neuropathic pain as compared with placebo.
Highlights of the results of the Z944 Phase 1b LEP study results include:
Statistically significant and meaningful reductions at each of the three doses compared to placebo of overall peak-to-peak (PtP) amplitude of LEPs in models of both inflammatory (p≤0.0002) and neuropathic (p<0.05) pain. Consistent trends in reduction of subjective pain scores compared to placebo using a visual analog scale in both pain models. Meaningful trends in effects based on dose and concentration, providing important insights into the potential therapeutic window and effective plasma concentrations of Z944. Z944 was generally well tolerated with dose dependent CNS side effects and no serious adverse events.
In this study, hypersensitivity to laser thermal stimulation was induced by UV light exposure as a model of inflammatory pain and by topical capsaicin as a model of neuropathic pain. Electrical voltage fluctuations evoked by laser thermal stimulation were quantified with vertex-Electroencephalography(EEG) in addition to a subject-reported pain score. Many currently approved and emerging pain drugs have been evaluated using the LEP model, providing the ability to benchmark the efficacy of Z944 against other therapies.

About Z944 and T-type Calcium Channels

Z944 is a novel, oral, state-dependent, selective T-type calcium channel modulator that has demonstrated efficacy in multiple preclinical inflammatory pain models and in a Phase 1b experimental model of pain. T-type calcium channels have been recognized as key targets for therapeutic intervention in a broad range of cell functions and have been implicated in pain signaling. Zalicus is planning to advance a modified release formulation of Z944 through further clinical development.

Please download press release for clinical study on Z944.

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About Klaus Schaffler

Dr. med. Klaus Schaffler (MD) has been specializing in the electrophysiology and pharmacology of the human central nervous system (CNS) – as well as in the field of human experimental pain research. During this development process, HPR Dr. Schaffler GmbH has issued over 175 presentations/ publications (sharing more than 50 on pain/ analgesia) and has conducted more than 150 phase-I studies with quite different objectives.