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Simulation of multiple ion channel block provides improved early prediction of compounds' clinical torsadogenic risk

Abstract:

Aims: The level of inhibition of the human Ether-à-go-go-related gene (hERG) channel is one of the earliest preclinical markers used to predict the risk of a compound causing Torsade-de-Pointes (TdP) arrhythmias. While avoiding the use of drugs with maximum therapeutic concentrations within 30-fold of their hERG inhibitory concentration 50% (IC50) values has been suggested, there are drugs that are exceptions to this rule: hERG inhibitors that do not cause TdP, and drugs that can cause TdP bu...

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Publisher copy:
10.1093/cvr/cvr044

Authors


G.R. Mirams More by this author
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Journal:
Cardiovascular Research
Volume:
91
Issue:
1
Pages:
53-61
Publication date:
2011
DOI:
ISSN:
00086363
URN:
uuid:678ef23c-23d1-4799-9f01-327b58fd59e6
Local pid:
cs:5027

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