hERG Screening

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  • Published date: January 15, 2020
    • Shirley, New York, United States

Cardiotoxicity is one of the major safety concerns in drug discovery, which is the leading reason for development termination and market withdraw or restriction. Particularly, hERG ion channel inhibition or blockade is responsible for 25-40% of all preclinical lead compound discontinuance. Human ether-a-go-go (hERG), a potassium channel that is abundant in the cardiomyocytes, represents one pivotal component for IKr currents and cardiac repolarization. Drug-induced interference of hERG causes QT interval prolongation, which is associated with fatal ventricular tachyarrhythmia called Torsade de Pointes (TdP). Given the unacceptable adverse effects of hERG inhibition and the fact that many drug-like molecules exhibit hERG affinity, hERG assessment has become one priority requirement by regulatory agencies before IND submission. https://www.creative-biolabs.com/drug-discovery/therapeutics/herg-screening.htm .

Jerry Carter
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