Transporters are membrane-bound proteins that facilitate the uptake or excretion of a wide range of compounds from nutrients, such as vitamins, to xenobiotic drugs like statins. Over the past decade, the regulatory agencies have identified examples of transporter-mediated drug-drug interactions (DDIs) that change drug safety and efficacy levels. In order to reduce potential DDI risks, the FDA has issued a guidance document to assist the drug development process.1 With this enhanced scrutiny of potential transporter-mediated DDIs, drug makers have also increased their research to study the potential contributions of transporters to the pharmacokinetics of their lead compounds. For example, poor brain penetration, elevated biliary or renal elimination may be indications of transporter-mediated effects limiting systemic exposure to their intended target site.
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