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Promising New Approaches for Discovering Ion-Channel Modulators

Decision Resources, Inc, May 2006, Pages: 21


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Ion-channel protein complexes represent a promising and exciting class of therapeutic targets with applications across many disease indications. Drugs that modulate ion-channel activity are first-line therapies in several therapeutic areas, such as cardiovascular disorders, central and peripheral nervous system disorders, and metabolic disorders, and the use of specific ion-channel modulators will likely expand into other major therapeutic areas, such as oncology. However, the pharmaceutical and biotechnology industries have not aggressively exploited ion channels as drug targets because they require difficult, labor-intensive, and low-throughput assays. Fortunately, recent scientific and technological advances are affecting ion-channel R&D significantly. In this report, we examine the function of ion channels and potential ion-channel targets, describe traditional and new methods of screening, profile companies specializing in ion-channel research, and discuss the outlook for the field.

Business Implications
Ion channels represent a promising and exciting class of therapeutic targets. Ion channels constitute one of the largest classes of novel potential drug targets; studies suggest that that the human genome contains 400 or more genes that encode distinct channels. Agents targeting ion channels have applications across many disease indications.
The drug industry has not yet aggressively exploited ion channels as drug targets. Ion channels are highly complex, and targeting them requires detailed knowledge about their structure and function. Traditionally, identifying ion-channel modulators has required difficult, labor-intensive, and low-throughput assays that require the expertise of highly skilled scientists to perform. However, the need to fill drug pipelines and bring new drugs to market is encouraging companies to develop programs aimed at these difficult targets.
Recent technological developments have led to the introduction of new technology platforms that enable higher-throughput screening for ion-channel modulators. These new, high-throughput methods are particularly useful for primary screening of smaller, focused compound libraries. The spread of new screening technologies should eventually increase the number of ion-channel modulators progressing into clinical development.
Smaller companies that specialize in ion channels enjoy some competitive advantages in this field. These companies are well positioned to use smaller, focused libraries of compounds for screening, and they are forming small, cohesive teams of highly skilled specialists. We expect that partnering between these companies and pharmaceutical companies seeking to inlicense novel agents will increase.



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