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Objectives The aim of this review is to provide useful information not only for studying the effect of OATP1B1 gene mutation on pharmacokinetics of glinides but also for studying drug-drug interactions(DDIs) between glinides and other substrates of OATP1B1 for combination treatment of metabolic syndrome.Glinides are widely applied to the treatment of metabolic syndrome and showed individual difference because of OATP1B1 gene mutation.Glinides are always combined with other drugs for treatment of metabolic syndrome.However,DDIs should be considered so as to avoiding side effect.As we know,if glinides and combined drugs are both the substrates of OATP1B1 there may had mutual inhibition competition that causes DDIs.Methods This review summaried the recent studies and the sourece were was carried out in several databases (update to June 2010): ISI Web of KnowledgeSM (ISI WoK),SciFinder (CAPLUS,MEDLINE,REGISTRY,CASREACT,CHEMLIST,CHEMCATS) and PubMed (indexed for MEDLINE).Results The present review provides a baseline on the level of evidence available on pharmacokinetics and DDIs of glinides,and should be of help to those intending to research further on these topics.Cnclusions The OATP1B1 plays an important role in the pharmacokinetics and DDIs between glinides and other clinical related drugs.