07/25/2018 - Role of transporters in drug ADME

Correlation Analysis of Potential Breast Cancer Resistance Protein Probes in Different Monolayer Systems

Sáfár Zs, Jani M, Makai I, Fekete Z, Bui A, Molnár É, Pádár P, Pratt JR, Kis E, Beéry E, Krajcsi P.

J Pharm Sci. 2018 Nov;107(11):2742-2747. doi: 10.1016/j.xphs.2018.07.014. Epub 2018 Jul 25.

Erratum in: J Pharm Sci. 2019 Jan 29

PMID: 30055222


Breast cancer resistance protein (BCRP) is a point of interest in drug-drug interaction safety testing. Therefore, a consensus probe that can be applied as victim in multiple experimental settings is of great benefit. Identification of candidates has been driven by the amount and quality of available clinical data, and as a result, drugs such as sulfasalazine and rosuvastatin have been suggested. In this article, the in vitro performance of 5 possible alternatives was evaluated: atorvastatin, chlorothiazide, dantrolene, topotecan, and teriflunomide, and benchmarked against sulfasalazine and rosuvastatin in reference in vitro assays for BCRP drug-drug interaction testing. Based on the results, teriflunomide is proposed as an alternate in vitro BCRP probe.

Keywords: ABC transporters; Caco-2 cells; Madin-Darby canine kidney (MDCK) cells; drug interaction; in vitro models.

Copyright © 2018 American Pharmacists Association®. Published by Elsevier Inc. All rights reserved.

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