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An update on efflux and uptake transporters as determinants of statin response.
Rocha, Karina Cunha E; Pereira, Beatriz Maria Veloso; Rodrigues, Alice Cristina.
Afiliação
  • Rocha KCE; a Department of Pharmacology , Institute of Biomedical Sciences, University of Sao Paulo , Sao Paulo , SP , Brazil.
  • Pereira BMV; a Department of Pharmacology , Institute of Biomedical Sciences, University of Sao Paulo , Sao Paulo , SP , Brazil.
  • Rodrigues AC; a Department of Pharmacology , Institute of Biomedical Sciences, University of Sao Paulo , Sao Paulo , SP , Brazil.
Expert Opin Drug Metab Toxicol ; 14(6): 613-624, 2018 Jun.
Article em En | MEDLINE | ID: mdl-29842801
INTRODUCTION: 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 statin disposition and toxicity.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Inibidores de Hidroximetilglutaril-CoA Redutases / Transportador 1 de Ânion Orgânico Específico do Fígado / Membro 2 da Subfamília G de Transportadores de Cassetes de Ligação de ATP / Proteínas de Neoplasias Tipo de estudo: Etiology_studies Limite: Animals / Humans Idioma: En Revista: Expert Opin Drug Metab Toxicol Assunto da revista: METABOLISMO / TOXICOLOGIA Ano de publicação: 2018 Tipo de documento: Article País de afiliação: Brasil País de publicação: Reino Unido
Texto completo
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Inibidores de Hidroximetilglutaril-CoA Redutases / Transportador 1 de Ânion Orgânico Específico do Fígado / Membro 2 da Subfamília G de Transportadores de Cassetes de Ligação de ATP / Proteínas de Neoplasias Tipo de estudo: Etiology_studies Limite: Animals / Humans Idioma: En Revista: Expert Opin Drug Metab Toxicol Assunto da revista: METABOLISMO / TOXICOLOGIA Ano de publicação: 2018 Tipo de documento: Article País de afiliação: Brasil País de publicação: Reino Unido