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Single oral doses of 0.25 mg digoxin (P\u2010gp), 5 mg furosemide (OAT1 and OAT3), 500 mg metformin (OCT2, MATE1, and MATE2\u2010K), and 10 mg rosuvastatin (OATP1B1, OATP1B3, and BCRP) were administered separately or as a cocktail in a randomized six\u2010period crossover trial in 24 healthy male volunteers. As a cocktail, relative bioavailabilities of digoxin and metformin and furosemide AUC<jats:sub>0\u2010tz<\/jats:sub> were similar to separate dosing. However, when administered as a cocktail the C<jats:sub>max<\/jats:sub> of furosemide was 19.1% lower and the C<jats:sub>max<\/jats:sub> and AUC<jats:sub>0\u2010tz<\/jats:sub> of rosuvastatin were 38.6% and 43.4% higher, respectively. In addition, the effects of increased doses of metformin or furosemide on the cocktail were investigated in 11 and 12 subjects, respectively. The cocktail explored in this trial has the potential to be used for the <jats:italic>in vivo<\/jats:italic> screening of transporter\u2010mediated drug\u2013drug interactions. \u00a9 2016 American Society for Clinical Pharmacology and Therapeutics<\/jats:p>","DOI":"10.1002\/cpt.406","type":"journal-article","created":{"date-parts":[[2016,6,3]],"date-time":"2016-06-03T08:33:15Z","timestamp":1464942795000},"page":"259-267","source":"Crossref","is-referenced-by-count":68,"title":["Pharmacokinetic Evaluation of a Drug Transporter Cocktail Consisting of Digoxin, Furosemide, Metformin, and Rosuvastatin"],"prefix":"10.1111","volume":"100","author":[{"given":"P","family":"Stopfer","sequence":"first","affiliation":[{"name":"Boehringer Ingelheim Pharma GmbH &amp; Co. KG  Germany"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"T","family":"Giessmann","sequence":"additional","affiliation":[{"name":"Boehringer Ingelheim Pharma GmbH &amp; Co. 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