N and T-Type Calcium Channel Blockers

N-type CCB

Neuromed is the only company to successfully advance a small molecule N-type calcium channel blocker into clinical trials. Prialt®, also an N-type calcium channel blocker, is a new drug shown to be effective in the relief of many different kinds of severe chronic pain, even pain refractory to intrathecal morphine. However, Prialt® is a peptide that must be delivered through a surgically implanted intrathecal pump. In contrast, Neuromed's N-type calcium channel blockers are being developed in oral form.

N-type calcium channel blockers represent a new class of analgesics that are selective for calcium channels involved in pain signal transmission. The concentration of calcium entering certain nerve cells in the spinal cord is directly linked to pain signal transmission.

Calcium channels control the entry of calcium into the neuron. When a pain signal is transmitted, the channel opens and the calcium concentration increases, triggering the release of neurotransmitters from synaptic vesicles, thereby sending the pain signal to the brain where it is perceived as pain. Morphine and other related drugs also affect calcium channels but indirectly, by binding to opioid receptors. When morphine activates these receptors, it not only inhibits N-type calcium channels, it also affects other processes, which leads to side effects such as sedation, motor impairment, addiction and gastrointestinal problems.

In March 2006, Neuromed partnered with Merck & Co. to research, develop and commercialize novel N-type calcium channel blockers for pain and other disorders.

T-type CCB

Neuromed is revealing the therapeutic potential of T-type calcium channel blockers. We have a dedicated team of scientists developing therapies to block this important validated target. Our robust program is producing compounds showing promise for further development as therapies for pain.

Beyond pain, T-type calcium channels blockers show potential for the development of drugs aimed at treating epilepsy and hypertension. T-type calcium channels in heart cells regulate pacemaker activity and are implicated as therapeutic targets for hypertension and certain arrhythmias. Additionally, genetic studies suggest T-type calcium channels are involved in certain types of epilepsy.