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Analysis of Torsadogenic and Pharmacokinetic Profile of E-4031 in Dogs Bridging the Gap of Information Between in Vitro Proarrhythmia Assay and Clinical Observation in Human Subjects

Analysis of Torsadogenic and Pharmacokinetic Profile of E-4031 in Dogs Bridging the Gap of Information Between in Vitro Proarrhythmia Assay and Clinical Observation in Human Subjects

Ai Goto, Hiroko Izumi-Nakaseko, Mihoko Hagiwara-Nagasawa, Koki Chiba, Kentaro Ando, Atsuhiko T Naito, Atsushi Sugiyama

J Pharmacol Sci. 2018 Jun;137(2):237-240.

PMID: 29980434

Abstract:

We analyzed torsadogenic and pharmacokinetic profile of E-4031 using chronic atrioventricular block dogs. E-4031 in intravenous doses of 0.03, 0.1 and 0.3 mg/kg over 10 min prolonged QT/QTc, and increased short-term variability of QT in a dose-related manner (n = 4), resulting in onset of torsade de pointes in 1 animal after the middle dose and 4 animals after the high dose, while it attained peak plasma concentrations of 16.5, 60.5 and 182.5 ng/mL at 10 min after their start of administration, respectively (n = 2). These results bridge the gap of information between in vitro proarrhythmia assay and clinical observation in human subjects.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP113559130	E-4031		113559-13-0	Price

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