An update on efflux and uptake transporters as determinants of statin response

Expert Opinion on Drug Metabolism & Toxicology
Karina Cunha E RochaAlice Cristina Rodrigues

Abstract

Statins are used in the treatment of dyslipidemia promoting primary and secondary prevention against detrimental cardiovascular events. ATP-binding cassette (ABC) and solute carrier (SLC) membrane transporters transport statins across the cell membrane. Differences in drug transporter tissue expression and activity contribute to variability in statin pharmacokinetics (PK) and response. Areas covered: The purpose of this review is to discuss factors impacting transporter expression and the effect this has on statin efficacy and safety. Previous studies have demonstrated that genetic polymorphisms, drug-drug interactions (DDI), nuclear receptors, and microRNAs affect statin PK and pharmacodynamics. Expert opinion: Genetic variants of ABCG2 and SLCO1B1 transporters affect statin PK and, as a result, the intended lipid-lowering response. However, the effect size is small, limiting its applicability in clinical practice. Furthermore, genetic variants do not totally explain the observed intervariability in statin response. Thus, it is likely that transcriptional and post-transcriptional regulation of drug transporters are also highly involved. Further studies are required to understand the contribution of each of these new factors in...Continue Reading

References

Jan 25, 2000·American Journal of Physiology. Gastrointestinal and Liver Physiology·J KönigD Keppler
Nov 4, 2000·Expert Opinion on Investigational Drugs·K KajinamiY Saito
May 12, 2001·Science·E S Istvan, J Deisenhofer
Oct 5, 2001·The American Journal of Medicine·P H ChongC Franklin
Oct 19, 2002·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Ken-ichi NezasaMasahiro Koike
May 15, 2003·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·M D PerloffD J Greenblatt
May 15, 2003·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·K NezasaM Koike
Jun 18, 2003·Clinical Pharmacology and Therapeutics·Yohei NishizatoYuichi Sugiyama
Sep 2, 2003·Methods and Findings in Experimental and Clinical Pharmacology·M J GarcíaJ R Prous
Apr 30, 2004·Clinical Pharmacology and Therapeutics·Jessica MwinyiThomas Gerloff
May 26, 2004·The Journal of Pharmacology and Experimental Therapeutics·Masaru HiranoYuichi Sugiyama
Nov 24, 2004·Pharmaceutical Research·Chihiro KondoYuichi Sugiyama
Apr 2, 2005·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Kaoru KobayashiKan Chiba
Apr 20, 2005·Cancer Chemotherapy and Pharmacology·Kuniaki MorisakiSusan E Bates
Jun 16, 2005·Molecular Pharmacology·Masaru HiranoYuichi Sugiyama
Jul 28, 2005·Molecular Pharmacology·Kathrin KopplowDietrich Keppler
Aug 9, 2005·Clinical Pharmacology and Therapeutics·Janne T BackmanPertti J Neuvonen
Sep 6, 2005·Pharmacogenetics and Genomics·Danxin WangWolfgang Sadée
Oct 4, 2005·Clinical Pharmacology and Therapeutics·Jae-Yong ChungIn-Jin Jang
Nov 2, 2005·The Journal of Pharmacy and Pharmacology·Hideki FujinoJunji Kojima
Mar 22, 2006·The Pharmacogenomics Journal·L M MangraviteR M Krauss
Apr 6, 2006·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Masaru HiranoYuichi Sugiyama
Oct 4, 2006·Clinical Pharmacology and Therapeutics·Mikko NiemiPertti J Neuvonen
Jan 16, 2007·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Yvonne MeierStephan R Vavricka
Feb 14, 2007·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Annick SeithelJörg König
May 3, 2007·Clinical Pharmacology and Therapeutics·M K PasanenM Niemi
Sep 28, 2007·The New England Journal of Medicine·Philip BarterUNKNOWN Treating to New Targets Investigators
Jul 12, 2008·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Satoshi KitamuraYuichi Sugiyama
Jul 25, 2008·The New England Journal of Medicine·UNKNOWN SEARCH Collaborative GroupR Collins
Apr 21, 2009·Clinica Chimica Acta; International Journal of Clinical Chemistry·Yi-Jing HeHong-Hao Zhou

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Citations

Mar 13, 2019·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Dafne Garcia-MateosGracia Merino
Dec 7, 2019·The Pharmacogenomics Journal·Cristina Ruiz-IruelaAriadna Padró-Miquel
Dec 6, 2020·International Journal of Clinical Practice·Jonida Haxhi, Paul D Thompson
Dec 24, 2019·Acta Pharmaceutica Sinica. B·Yuhua LiHuichang Bi
Nov 25, 2020·International Journal of Molecular Sciences·Christopher MurphyAlvaro Garcia
Nov 14, 2020·Genes·Mónica GalochaMiguel Cacho Teixeira
Aug 18, 2021·Pharmacological Reports : PR·Carolina Dagli-HernandezRosario Dominguez Crespo Hirata
Aug 19, 2021·Anti-cancer Drugs·Guodong ZhaoJinhai Tang

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