IndraLab

Statements


KCNH2 inhibits dTDP. 7 / 7
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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."

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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."

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"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."

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"The narrow safety margin for halofantrine partly explains why the potent hERG channel inhibition leads to QTc prolongation and even TdP."

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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."

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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."

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"Therefore while almost all drugs that cause TdP block hERG, the converse is not true."