Preclinical data of Zalicus sodium channel compound published in journal PAIN

Zalicus Inc. (NASDAQ: ZLCS) today announced the publication of preclinical data in the journal PAIN. The paper describes the activity of Z212, a novel proprietary small organic compound that acts to modulate Nav1.7 and Nav1.8 sodium channels and to reduce neuropathic pain by targeting the hyper-excitability associated with chronic pain signaling pathways. Through its unique mechanism of action, Z212 has been shown to both reduce the excitability of neurons and reverse pain hypersensitivity in preclinical models. Zalicus is utilizing its ion channel discovery platform and scientific expertise to develop a pipeline of novel, orally active compounds targeting critical N-type and T-type calcium and selected sodium channels implicated in chronic pain.

“By targeting the sodium channels in the peripheral and central nociceptive signaling pathways through its unique mechanism of action, Z212 has the potential to become a safe and effective treatment for chronic inflammatory and neuropathic pain”

Zalicus's most advanced preclinical ion channel product candidate, Z944, a novel T-type calcium channel blocker, has been selected to advance into IND-enabling toxicology studies prior to the initiation of a Phase 1 study in 2011. Z212 and multiple other preclinical compounds have been identified and are being evaluated for additional clinical starts in 2011.

In the paper entitled, "A novel slow-inactivation-specific ion channel modulator attenuates neuropathic pain," Hildebrand et al., PAIN (2011), pre-published online (doi:10.1016/j.pain.2010.12.035), Zalicus researchers describe the design, synthesis and activity of the unique sodium channel pain blocking compound Z212 to preferentially attenuate hyperexcitable neurons while largely sparing normally firing neurons.

"By targeting the sodium channels in the peripheral and central nociceptive signaling pathways through its unique mechanism of action, Z212 has the potential to become a safe and effective treatment for chronic inflammatory and neuropathic pain," commented Mark H.N. Corrigan, MD, President and CEO of Zalicus. "With the addition of selected sodium channel targets to its screening platform Zalicus continues to utilize its considerable expertise in ion channels to develop a pipeline of novel, orally available agents that address these attractive targets for pain intervention."

Improved Calcium and Sodium Channel Blockers through Electrophysiological Screening

Our industry leading selective ion channel modulation platform allows us to identify product candidates that harness the potential of targeting calcium and sodium channels for acute and chronic pain. Zalicus utilizes proprietary drug design and electrophysiological screening processes to create drug candidates with improved levels of specificity and mechanisms of action, potentially leading to greatly enhanced safety and tolerability profiles compared to existing agents. Building on this work, we are currently pursuing programs at developing N-type and T-type calcium channels and selected sodium channel blockers.