IndraLab

Statements

KCNH2 inhibits dTDP. 7 / 7
| 7
reach
"The results of the nonclinical and clinical validation studies described in this article will inform how CiPA may result in modification to the ICH guidelines to shift from focusing on hERG block and QT prolongation to informing proarrhythmic risk, as not all hERG blocking and QT prolonging drugs cause TdP."
28986934
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"Not all hERG channel blockers induce TdP because they can also modulate other channels that counteract the hERG channel mediated effect."
15749156
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"Therefore while almost all drugs that cause TdP block hERG, the converse is not true."
19027781
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"Further, even though all drug induced torsadogenic compounds have a low IC 50 (strong blockers of hERG), not all hERG blockers with strong potencies lead to TdP."
29297274
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"In a survey of the literature, Redfern et al. reported that the margin between the hERG IC 50 value and plasma exposure of the drug might be a valuable parameter for predicting the risk of QT prolongation and TdP induced by a hERG blocker."
18587422
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"The robust association between I Kr / hERG blocking propensity and TdP makes it essential that drug candidates are screened for I Kr / hERG blockade."
18616963
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"The current paradigm of cardiac safety screening for, primarily, hERG activity to eliminate TdP causing drugs from reaching the market has reduced incidence of adverse drug induced TdP."
26891981