Drugs, hERG and sudden death.
Early recognition of potential QT/TdP liability is now an essential component of the drug discovery/drug development program. The hERG assay is an indispensable step and a high-quality assay must accompany any investigational new drug (IND) application. While it is the gold standard at present, the hERG assay is too labor-intensive and too low throughput to be used as a screen early in the discovery/development process. A variety of indirect high throughput screens have been used.
Brown
A M
AM
MetroHealth Campus, Case Western Rreserve University, Cleveland, OH 44128, USA. abrown@chantest.com
D016757:Death, Sudden, Cardiac / Q000209:etiology*; D004353:Drug Evaluation, Preclinical / Q000379:methods* / Q000592:standards; D000072237:ERG1 Potassium Channel; D051638:Ether-A-Go-Go Potassium Channels; D006801:Humans; D008133:Long QT Syndrome / Q000209:etiology; D015221:Potassium Channels / Q000378:metabolism*; D024642:Potassium Channels, Voltage-Gated; D016593:Terfenadine / Q000009:adverse effects / Q000494:pharmacology
D000072237:ERG1 Potassium Channel; D051638:Ether-A-Go-Go Potassium Channels; C000606913:KCNH2 protein, human; D015221:Potassium Channels; D024642:Potassium Channels, Voltage-Gated; D016593:Terfenadine