Correlation Analysis of Potential BCRP Probes in Different Monolayer Systems

Abstract

Breast Cancer Resistance Protein (BCRP) is a point of interest in Drug Drug Interaction (DDI) 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 sulfasalazine (SSZ) and rosuvastatin (RVS) have been suggested. In this paper the in vitro performance of five possible alternatives is evaluated: atorvastatin (AVS), chlorothiazide (CHT), dantrolene (DAN), topotecan (TPT), and teriflunomide (TRF), and benchmarked against SSZ and RVS in reference in vitro assays for BCRP DDI testing. Based on the results TRF is proposed as an alternate in vitro BCRP probe.