May 23, 2017
For over a year now, SOLVO has been collaborating with Ascendance Biotechnology (formerly Hepregen) in the commercialization of their unique HepatoPac® plates in Europe and Asia. Encouraged by positive customer feedback and repeated orders from our customers, our own experience with the plates and the response to our webinar series in 2016, we are launching a series of Science Letters to further educate you on the use of this platform.
This week: Investigating Enzyme-Transporter Interplay using Micropatterned Co-Cultures of Primary Hepatocytes
Regulatory agencies and drug metabolism scientists increasingly appreciate the importance of transporter – enzyme interplay in drug clearance. To understand and explore these complementary mechanisms requires the utilization of in vitro models with a full complement of enzymes and transporters expressed at physiologically relevant levels and correct subcellular localization. HepatoPac® fully satisfies these criteria, and is a liver model that provides a superior assessment of hepatic drug metabolism and transport processes compared to other traditional in vitro tools.
In this science letter, we discuss a case study involving Faldaprevir, a low-clearance drug which showed significant enrichment in the liver. In the case study, faldaprevir clearance was studied in HepatoPac®, taking into account drug transport, metabolism, and induction. Experiments included generation of faldaprevir metabolite profiles, their rates of formation, liver enrichment of the drug, faldaprevir active and passive uptake with and without inhibitors or Na+, and its enzyme and transporter kinetics.
HepatoPac® is available for a variety of species (rat, dog, or human) and can be delivered in different formats (24-, 72-, and 96-well). Apart from HepatoPac® products, SOLVO also offers services using HepatoPac® plates. Contact us to find out more!
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