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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% (IC(50)) 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...

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Publication status:
Published

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Publisher copy:
10.1093/cvr/cvr044

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Journal:
Cardiovascular research
Volume:
91
Issue:
1
Pages:
53-61
Publication date:
2011-07-05
DOI:
EISSN:
1755-3245
ISSN:
0008-6363
URN:
uuid:f7c85a24-cb5a-496e-9dc4-717c1a9d93f3
Source identifiers:
237657
Local pid:
pubs:237657

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