美国Icagen
主要研发用于治疗疼痛和相关不适应症状的离子通道药物。
Icagen is a biopharmaceutical company focused on the discovery, development and commercialization of novel small molecule drugs that modulate ion channel targets. The company has developed an integrated technology platform that allows for the efficient discovery of drug leads.
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 numerous 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 United States patents and 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 Pain
ICA-105665 is a novel opener of the KCNQ potassium ion channel which has
demonstrated a broad spectrum of activity in preclinical models of both
epilepsy and pain. In Phase I safety studies, the compound was shown to be
well tolerated in both healthy volunteers and in epilepsy patients. ICA-105665
was subsequently studied in patients with photosensitive epilepsy, with two of
the four patients tested in the 400mg dose cohort showing a positive
response. This study was subsequently extended to doses of 500mg and
600mg, but due to a serious adverse event in the 600mg dose cohort the
study was placed on clinical hold. In an extension to the multiple ascending
dose safety study in healthy volunteers, ICA-105665 continued to be well
tolerated at doses up to 600mg. The Company is currently discussing
potential next steps with its advisors and with the FDA, with analysis of the
complete data set from both studies ongoing.
Pain Control
Icagen has a broad research effort directed at novel ion channel targets for
pain control. In August, 2007, 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 ion channel targets in its pain control program.
Inflammatory Disorders
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.