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March 16, 2022

Efflux Transporters – Challenges, Failures, and Success Stories




8:00 am (PT)

11:00 am (ET)

4:00 pm (GMT)

5:00 pm (CET)

6:00 pm (IST)

12:00 pm (Beijing)

01:00 am (Tokyo, Seoul)


Zsuzsanna Gaborik, PhD
Head od R&D Laboratory
SOLVO Biotechnology

Summary of the presentation:

SOLVO distinguishes itself by the emphasis we put on continuously improving the quality, accuracy, and predictive value of our in vitro assays to deliver high quality data to our clients. Although our service portfolio is constantly growing, much of the efforts, failures, and success stories of our Research and Development team often remains hidden behind the scenes. While efflux transporters have a key role in drug absorption, distribution, and clearance and are common mediators of drug-drug interactions, their investigation has always been challenging. Due to their localization and mode of action, in vitro methods available for their investigation range from rather simple methods to complex models. When comparing the most commonly used assay systems, we need to consider or avoid endogenous efflux transporter expression, as well as drug concentration at the binding site of transporter, and assay duration. Despite such differences, however, the calibration of vesicular transport versus transcellular transport assays with drugs of known DDI effects resulted in comparable DDI prediction accuracy, both for P-gp and BCRP. While the in vitro transporter assays may seem straightforward, it is recognized that experimental outcomes and predictive value are influenced by several factors. Therefore, better understanding of these experimental models, more complex study setups using the appropriate controls are needed to acquire high quality in vitro data that can be reliably used for establishing physiologically based PK models. Considering all these requirements, our latest webinar aims to give an insight into the challenges, difficulties, and ideas behind our assay developments.

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