Use of SilensomesTM for the analysis of the inhibitory effect of Amiodarone on Warfarin metabolism

Use of SilensomesTM for the analysis of the inhibitory effect of Amiodarone on Warfarin metabolism

SilensomesTM correspond to batches of cryopreserved pooled of human liver microsomes (HLM) chemically silenced for one specific CYP450 using a mechanism based inhibitor (MBI) (1). SilensomesTM can be handled like conventional HLM. SilensomesTM allow qualitative CYP phenotyping, quantitative metabolized fraction (fm ) and intrinsic Clearance (Clint ) evaluation. It is well known that alterations of CYP mediated drug metabolism by simultaneous administration of other drugs is one of the most common causes of drug-drug interactions. One of them regards the possible effects of the antiarhythmic drug Amiodarone (AMIO) on the metabolism of warfarin (WRF). WRF is a widely used anticoagulant with a narrow therapeutic index and compounds affecting its metabolism may have serious consequences. WRF is mostly metabolized by CYP2C9, with the formation of different hydroxylated metabolites (OH-WRF) and AMIO is described to inhibit CYP2C9 (2). The studies reported here aimed to an in vitro experimental demonstration of the above prediction, to support the interpretation of the clinical data in a more robust manner. For that, we exploited Control SilensomesTM and CYP2C9 SilensomesTM, studying the involvement of CYP2C9 in the metabolism of S-WRF, and the effects of amiodarone on its metabolism.

Prochains événements

Actualités

    Lancement de Wepredic ! Groupe fédérateur d'acteurs des techno in vitro

    Lancement de Wepredic ! Groupe fédérateur d'acteurs des techno in vitro :) Christophe Chesné, Ph.D et Directeur Général d'Eurosafe, est aussi le fondateur de Biopredic International, Starlight et Advancells. Ces entreprises expertes des technologies in vitro pour la toxicologie, travaillent quotidiennement avec les grands acteurs pharma, cosmétiques et de la chimie. Wepredic a donc été créé pour rassembler ces 4 marques et couvrir ainsi le domaine des kits d'essai in vitro amenés à remplacer l'animal de laboratoire. Découvrez l'édito de Christophe Chesné sur les raisons de ce choix stratégique !

    Lire plus

    Nouveau logo, nouvelle identité visuelle pour Eurosafe !

    Eurosafe fait "peau neuve", dans le cadre de la refonte globale des marques du Groupe Wepredic, la maison mère. Un nouveau logo pour illustrer notre métier : évaluer la sécurité des produits cosmétiques et pharmaceutiques !

    Lire plus

    Gingival irritation on a reconstructed model (3D)

    Eurosafe is pleased to inform you that our tests on reconstructed models have been enhanced with a new security screening for all your oral products (e.g. toothpaste, mouthwash): "Gingival irritation on a reconstructed model (3D)".

    Lire plus