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Endogenous Biomarkers for SLC Transporter-Mediated Drug-Drug Interaction Evaluation

Yang Li, Zahra Talebi, Xihui Chen, Alex Sparreboom, Shuiying Hu

2021Molecules29 citationsDOIOpen Access PDF

Abstract

Membrane transporters play an important role in the absorption, distribution, metabolism, and excretion of xenobiotic substrates, as well as endogenous compounds. The evaluation of transporter-mediated drug-drug interactions (DDIs) is an important consideration during the drug development process and can guide the safe use of polypharmacy regimens in clinical practice. In recent years, several endogenous substrates of drug transporters have been identified as potential biomarkers for predicting changes in drug transport function and the potential for DDIs associated with drug candidates in early phases of drug development. These biomarker-driven investigations have been applied in both preclinical and clinical studies and proposed as a predictive strategy that can be supplanted in order to conduct prospective DDIs trials. Here we provide an overview of this rapidly emerging field, with particular emphasis on endogenous biomarkers recently proposed for clinically relevant uptake transporters.

Topics & Concepts

DrugTransporterPharmacologyPolypharmacyBiomarkerDrug developmentDrug metabolismEndogenyMedicineComputational biologyBiologyInternal medicineBiochemistryGeneDrug Transport and Resistance MechanismsPharmacological Effects and Toxicity StudiesPharmacogenetics and Drug Metabolism
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