Zalicus Inc. (Nasdaq Global Market: ZLCS) today announced that preclinical data showing the advantages of applying Zalicus’s state dependent screening approach to identify novel calcium channel blockers for the treatment of pain was presented on March 18 at the 4th Annual RSC/SCI Symposium on Ion Channels as Therapeutic Targets Conference taking place from March 18-19, 2013 in Cambridge, UK.
In a poster presentation entitled “Screening for State-Dependent Blockers of Voltage Gated Calcium Channels,” Margaret S. Lee, PhD, Vice President of Research & Translational Medicine at Zalicus, demonstrated the utility of inactivation state screening to identify novel, potent, selective and state-dependent calcium channel blockers with efficacy in animal models of inflammatory and neuropathic pain.
“Rapid neuronal firing which occurs during chronic pathological pain results in accumulation of voltage gated calcium channels in an inactivated state. By specifically targeting this inactivated state of these channels, it may be possible to broaden the therapeutic window, minimize adverse effects and increase efficacy for these promising pain therapies,” said Dr. Lee. “Comparative screening in our cell based assays for state dependent modulation of ion channel function has resulted in the discovery of Z160 and Z944, Zalicus’s two most advanced novel, first-in-class calcium channel blockers. Both Z160 and Z944 have effectively demonstrated enhanced potency for their respective targets in the inactivated state.”
About Z160 and N-type Calcium Channel BlockersZ160 is a first-in-class, oral, state-dependent, selective N-type calcium channel (Cav 2.2) blocker, designed to selectively target neuronal pain signaling by modulating neurons that are undergoing high-frequency firing. Z160 has demonstrated efficacy in multiple animal models of neuropathic and inflammatory pain, suggesting that it has the potential to treat a broad range of chronic pain conditions. Additionally, clinical trials in over 200 subjects have established Z160 as a safe and well tolerated drug candidate. N-type calcium channels have been recognized as key targets in controlling pain because of their key role in transmitting pain through the spinal nerves to the brain. Zalicus has advanced Z160 into two Phase 2a proof-of-concept clinical studies in chronic neuropathic pain and plans to report top-line data in late 2013.