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Effects of icosapent ethyl (Eicosapentaenoic acid ethyl ester) on pharmacokinetic parameters of rosiglitazone in healthy subjects
Author(s) -
Braeckman Rene A.,
Stirtan William G.,
Soni Paresh N.
Publication year - 2014
Publication title -
clinical pharmacology in drug development
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.711
H-Index - 22
eISSN - 2160-7648
pISSN - 2160-763X
DOI - 10.1002/cpdd.150
Subject(s) - rosiglitazone , medicine , cmax , pharmacokinetics , eicosapentaenoic acid , triglyceride , pharmacology , adverse effect , fatty acid , insulin , chemistry , cholesterol , biochemistry , polyunsaturated fatty acid
Background Icosapent ethyl is a high‐purity form of eicosapentaenoic acid ethyl ester approved to reduce triglyceride levels in adults with triglycerides ≥500 mg/dL. Candidates for triglyceride‐lowering therapy include patients with diabetes mellitus who may be receiving rosiglitazone. We assessed the effects of icosapent ethyl on the pharmacokinetic parameters of rosiglitazone. Methods Subjects received a single 8‐mg oral dose of rosiglitazone alone and with oral icosapent ethyl 4 g/day in this open‐label drug–drug interaction study. Pharmacokinetic end points included area under the concentration versus time curve from time zero to infinity (AUC 0–inf ) and maximum observed concentration (C max ) for rosiglitazone with and without icosapent ethyl. Results Of 30 subjects enrolled, 28 completed the study. Icosapent ethyl 4 g/day at steady‐state did not significantly change the single‐dose AUC 0–inf or C max of rosiglitazone 8 mg. Least squares geometric mean ratios (90% confidence interval) for AUC 0–inf and C max of rosiglitazone given with icosapent ethyl versus rosiglitazone alone were 0.90 (87.00–93.40) and 1.01 (92.02–109.9), respectively. No serious adverse events were reported and no subject discontinued due to an adverse event. Conclusions At steady‐state concentrations, icosapent ethyl did not inhibit the pharmacokinetics of rosiglitazone. Co‐administration of icosapent ethyl and rosiglitazone was safe and well tolerated.