Membrane transporters can have clinically relevant effects on the pharmacokinetics and pharmacodynamics of a drug in various organs and tissues by controlling its absorption, distribution and elimination. Together with metabolizing enzymes, they can drive a drug’s pharmacological action, as well as a drug can modulate transporter expression or activity, hence the importance of evaluating transporter-mediated drug-drug interactions recommended by the FDA guidelines. Genomembrane have developed transiently expressing ready-to-use cells to study FDA approved transporters (TransiPort). I had described this product range and their unique features in a previous post. I would like to introduce in this one 2 newly released cells overexpressing OATP1A2 and OATP2B1 transporters. [Read more…]
These cell lines transiently express the current FDA and EMA recommended SLC drug transporters (eg. OCT1 and OCT2; OAT1 and OAT3; MATE1; MAT2K…). Conditioned as cryopreserved format, they provide flexibility for experimental planning and can be assayed in just 2 days.
Transporters have become increasingly important in drug development due to the major role they play in absorption, distribution and excretion of endogenous and exogenous compounds, as transporter-mediated drug-drug interactions (DDI) are associated with potential toxicological and pharmacological consequences. As shown in numerous publications, the effects of transporters on the pharmacokinetics of several drugs and associated DDI have been reported. Consequently, recent guidance documents released by the US FDA and European Medicines Agency (EMA) emphasize the importance of evaluating the potential of new drug candidates for transporter-mediated DDI.
Solute carrier (SLC) transporters are located in the small intestine, liver, kidney, blood-brain barrier, and so on. They play a role in the up-take of various drugs, as well as endogenous nutrients into cells and thus may influence the ADME properties of, or indeed adverse reactions to, a compound of interest. Thus, investigation of SLC transporters is expected to be helpful during drug development. [Read more…]