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<datestamp>2017-12-21</datestamp>
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<title lang=en>Evaluation of P-Glycoprotein Inhibitory Potential Using a Rhodamine 123 Accumulation Assay</title>
<creator>Jouan, Elodie</creator>
<creator>Le Vée, Marc</creator>
<creator>Mayati, Abdullah</creator>
<creator>Denizot, Claire</creator>
<creator>Parmentier, Yannick</creator>
<creator>FARDEL, Olivier</creator>
<contributor>Institut de recherche, santé, environnement et travail [Rennes] (Irset) ; Université d'Angers (UA) - Université des Antilles et de la Guyane (UAG) - Université de Rennes 1 (UR1) - École des Hautes Études en Santé Publique [EHESP] (EHESP) - Institut National de la Santé et de la Recherche Médicale (INSERM) - Structure Fédérative de Recherche en Biologie et Santé de Rennes ( Biosit : Biologie - Santé - Innovation Technologique )</contributor>
<contributor>Technologie Servier ; Technologie Servier</contributor>
<contributor>CHU Pontchaillou [Rennes]</contributor>
<description>International audience</description>
<source>Pharmaceutics</source>
<identifier>hal-01305488</identifier>
<identifier>https://hal-univ-rennes1.archives-ouvertes.fr/hal-01305488</identifier>
<source>https://hal-univ-rennes1.archives-ouvertes.fr/hal-01305488</source>
<source>Pharmaceutics, 2016, 8 (2), pp.12. 〈10.3390/pharmaceutics8020012〉</source>
<identifier>DOI : 10.3390/pharmaceutics8020012</identifier>
<relation>info:eu-repo/semantics/altIdentifier/doi/10.3390/pharmaceutics8020012</relation>
<identifier>PUBMED : 27077878</identifier>
<relation>info:eu-repo/semantics/altIdentifier/pmid/27077878</relation>
<language>en</language>
<subject lang=en> rhodamine 123</subject>
<subject lang=en> P-Glycoprotein</subject>
<subject lang=en>digoxin</subject>
<subject lang=en> drug–drug interactions</subject>
<subject lang=en> inhibition</subject>
<subject>[SDV] Life Sciences [q-bio]</subject>
<type>info:eu-repo/semantics/article</type>
<type>Journal articles</type>
<description lang=en>In vitro evaluation of P-glycoprotein (P-gp) inhibitory potential is now a regulatory issue during drug development, in order to predict clinical inhibition of P-gp and subsequent drug-drug interactions. Assays for this purpose, commonly based on P-gp-expressing cell lines and digoxin as a reference P-gp substrate probe, unfortunately exhibit high variability, raising thus the question of developing alternative or complementary tests for measuring inhibition of P-gp activity. In this context, the present study was designed to investigate the use of the fluorescent dye rhodamine 123 as a reference P-gp substrate probe for characterizing P-gp inhibitory potential of 16 structurally-unrelated drugs known to interact with P-gp. 14/16 of these P-gp inhibitors were found to increase rhodamine 123 accumulation in P-gp-overexpressing MCF7R cells, thus allowing the determination of their P-gp inhibitory potential, i.e., their half maximal inhibitor concentration (IC50) value towards P-gp-mediated transport of the dye. These IC50 values were in the range of variability of previously reported IC50 for P-gp and can be used for the prediction of clinical P-gp inhibition according to Food and Drug Administration (FDA) criteria, with notable sensitivity (80%). Therefore, the data demonstrated the feasibility of the use of rhodamine 123 for evaluating the P-gp inhibitory potential of drugs</description>
<date>2016</date>
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