Ion channels are protein structures found in virtually every cell of the human body. Ion channels span the cell membrane and regulate the flow of ions, which are charged particles such as sodium, potassium, calcium and chloride, into and out of cells. There are currently 35 drugs that modulate ion channels and are marketed by third parties for multiple therapeutic indications.

Key elements of our ion channel technology include our cloning of over 300 human ion channel genes, which we believe represents substantially all of the human ion channel genome; expertise in developing high throughput screens for ion channel targets; ion channel focused chemistry libraries of over 250,000 compounds;  proprietary computational chemistry methods; an extensive ion channel database, which integrates biological and chemical information about our targets and compounds; pharmacology and bioanalytic capabilities; and an extensive intellectual property portfolio consisting of approximately 55 United States patents and approximately 40 United States patent applications as well as numerous foreign counterparts.  By integrating a number of scientific and drug development disciplines, we are able to efficiently discover and develop small molecule compounds that are more specific for the medically relevant ion channel, and therefore have a reduced likelihood of adverse side effects and clinical failure.

We pursue a target class approach to ion channel drug discovery. In this approach, we start with all potential ion channel targets and seek to identify applications to the treatment of various diseases. We believe that our approach provides for a more efficient drug discovery process, because our in-depth understanding of the targets and methods for finding small molecule modulators of these targets obviates the need to develop new research tools each time a new target is identified. Instead, we use our knowledge and skill to quickly find potential small molecule modulators of particular ion channel targets. We then use these small molecules to validate the particular target in a relevant animal model of disease. If a small molecule demonstrates activity in the animal model, it both validates the target and provides a starting point for further medicinal chemistry efforts.

Utilizing our proprietary know-how and integrated scientific and drug development capabilities, we have identified multiple drug candidates that modulate ion channels.

Icagen is conducting clinical and preclinical studies in its core focus areas, which include the following:

• Epilepsy and Neuropathic Pain

              ICA-105665 is currently in Phase I clinical studies.  ICA-105665 is a novel

              opener of the KCNQ ion channel which in preclinical studies has

              demonstrated a broad spectrum of activity in models of epilepsy.  In addition,

              ICA-105665 has also demonstrated activity in certain models of neuropathic    

              pain.

• Asthma

             Senicapoc, formerly known as ICA-17043 is currently in Phase I clinical studies.

             In several previous clinical studies senicapoc has demonstrated a favorable

             safety and tolerability profile.

• Pain Control

              Icagen has a broad research effort directed at novel ion channel targets for

              pain control.  Icagen recently entered into a collaboration with Pfizer for the

              discovery and development of novel pharmaceuticals directed against three

              sodium channel targets.  In addition, Icagen is pursuing research directed at

              multiple calcium channels as well as other novel ion channel targets in its

              pain control program.

• Inflammatory Disorders

              Icagen has a broad research effort directed at novel ion channel targets for

              inflammatory disorders.  As a result, Icagen has identified several ion channel

              targets that are expressed at high levels in some immune system cells and

              that may play an important role in modulating the inflammatory response. 

              Icagen has discovered compounds that are active in vitro against some of

              these targets, leading to decreases in calcium entry into immune  system

              cells, decreases in immune system cell proliferation, decreases in immune

              system cell migration into tissues and other measures of inflammatory

              responses.  Icagen has also demonstrated effects of our compounds in

              animal models of inflammatory diseases

In addition to the areas noted above, Icagen is continuing to explore the human ion channel genome, for which it has completed the cloning of all human ion channel genes, to identify new therapeutic opportunities.