cyprotex
the ADME Tox specialists

hERG safety

  • The human ether-a-go-go related gene (hERG) encodes the inward rectifying voltage gated potassium channel in the heart (IKr) which is involved in cardiac repolarization.
  • Inhibition of the hERG current causes QT interval prolongation resulting in potentially fatal ventricular tachyarrhythmia called Torsade de Pointes.
  • A number of drugs have been withdrawn from late stage clinical trials due to these cardiotoxic effects, therefore it is important to identify inhibitors early in drug discovery.
  • The Cyprotex hERG Safety assay employs the Ionworks™ HT System (Molecular Devices) as an automated patch clamp electrophysiology measurement.
  • The Ionworks™ HT system delivers high quality, accurate and sensitive data which is comparable with the traditional single cell patch clamp method.
  hERG Safety
 
‘The impressive list of drugs, already on the market or still under development that have been reported to adversely prolong repolarisation, makes it imperative to investigate any new chemical entity for this potential side effect before its first use in man.’
1Haverkamp W, Breithardt G, Camm AJ, Janse MJ, Rosen MR, Antzelevitch C, Escande D, Franz M, Malik M, Moss A and Shah R. (2000) Eur Heart J 21 (15); 1216-31.
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References

1 Haverkamp W et al. (2000) Eur Heart J 21 (15); 1216-31.
2 Finlayson K et al. (2004) Eur J Pharmacol 500; 129-142.

3 Kiss L et al. (2003) Assay Drug Dev Technol 1; 127-135.
4 Schroeder K et al. (2003) J Biomol Screen 8 (1); 50-64.

 
hERG safety

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This website was last updated
on 16th April 2014
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