Last abstract: A risk profile of fenspiride using ion channel data and in silico action potential modeling (2020)

By On 01/12/2020


Crumb W.J. Jr  & Christophe B.  (2020)

A risk profile of fenspiride using ion channel data and in silico action potential modeling

Journal of pharmacological and toxicological methods, 105, 106793


Safety Pharmacological Society / Barcelone / September 23-26, 2019


Recently, the marketing authorization for fenspiride containing products has been suspended in the EU due to reports of QT prolongation and torsade de pointes. As indicated in the Public Assessment report for Fenspiride, a total of 5 cases of QT prolongation including 3 cases of torsade de pointes were reported since the marketing of fenspiride. Most of these cases were in patients which had known or suspected risk factors for QT prolongation or arrhythmias (eg congenital LQT) or in patients taking other QT prolonging drugs or doses of fenspiride well above therapeutic. The goal of the present study was to characterize the effects of fenspiride on 3 ion channels which are known to play an important role in QT prolongation: hERG, late Nav1. 5, and Cav1. 2. Evaluating drugs against these ion channels and modeling with in silico action potential models is part of the new CiPA paradigm. In addition, we wanted to …