In Vitro Proarrhythmic Liability | IPS Therapeutique

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In vitro proarrhythmic liability assessment (hERG inhibition).jpg

In Vitro Proarrhythmic Liability Assessment

Decreases in K+ channel conduction widens the action potential and lead to prolonged QT intervals, which can be proarrhythmic
This assessment is part of the core safety pharmacology package, along with CNS and respiratory safety assessments

In vitro proarrhythmic liability assessment (hERG inhibition).jpg

Vitro Proarrhythmic Liability Assessment - Readouts & Application

Readouts:

Current amplitude and activation/inactivation kinetics
IC50 value used to measure cardiac safety margins
Reversibility of the effect

Application:

“hERG inhibition”, as the assay is often called, is necessary for regulatory submission. It is often conducted as a non-GLP compliant screen before initiating a GLP-compliant study as per the ICH S7A&B guidelines and the associated Q&A document.

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