Hepatic drug transporters: the journey so far

التفاصيل البيبلوغرافية
العنوان: Hepatic drug transporters: the journey so far
المؤلفون: S A Foley, Robert J. Riley, Matthew G. Soars, Beth Williamson, P Barton
المصدر: Expert Opinion on Drug Metabolism & Toxicology. 12:201-216
بيانات النشر: Informa Healthcare, 2016.
سنة النشر: 2016
مصطلحات موضوعية: Drug, media_common.quotation_subject, Pharmacology, Toxicology, Bioinformatics, 030226 pharmacology & pharmacy, 03 medical and health sciences, 0302 clinical medicine, Drug Discovery, Animals, Humans, Medicine, Drug Interactions, Pharmacokinetics, media_common, business.industry, Drug discovery, Membrane Transport Proteins, Biological Transport, Transporter, General Medicine, Liver, Pharmaceutical Preparations, Drug Design, 030220 oncology & carcinogenesis, business
الوصف: The key role of transporter biology in both the manifestation and treatment of disease is now firmly established. Experiences of sub-optimal drug exposure due to drug-transporter interplay have supported incorporation of studies aimed at understanding the interactions between compounds and drug transporters much earlier in drug discovery. While drug transporters can impact the most pivotal pharmacokinetic parameter with respect to human dose and exposure projections, clearance, at a renal or hepatobiliary level, the latter will form the focus of this perspective.A synopsis of guidelines on which transporters to study together with an overview of the currently available toolkit is presented. A perspective on when to conduct studies with various hepatic transporters is also provided together with structural "alerts" which should prompt early investigation.Great progress has been made in individual laboratories and via consortia to understand the role of drug transporters in disease, drug disposition, drug-drug interactions and toxicity. A systematic analysis of the value posed by the available approaches and an inter-lab comparison now seems warranted. The emerging ability to use physico-chemical properties to guide future screening cascades promises to revolutionise the efficiency of early drug discovery.
تدمد: 1744-7607
1742-5255
الوصول الحر: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5adede26936155a26e5bd682b90e295eTest
https://doi.org/10.1517/17425255.2016.1132308Test
رقم الانضمام: edsair.doi.dedup.....5adede26936155a26e5bd682b90e295e
قاعدة البيانات: OpenAIRE