Pharmacokinetic Interaction Among Ezetimibe, Rosuvastatin, and Telmisartan

Ki Young Huh, Sang Won Lee, Si Beum Lee, Kyung Tae Kim, In Jin Jang, Seung Hwan Lee

Research output: Contribution to journalArticlepeer-review

Abstract

To evaluate the pharmacokinetic interactions among rosuvastatin, ezetimibe, and telmisartan, a randomized, open-label, 3-period, 6-sequence crossover study was conducted in healthy subjects. Subjects received one of the following treatments once daily for 7 days in each period with a 1-week washout: a fixed-dose combination of ezetimibe/rosuvastatin 10/20 mg, telmisartan 80 mg, combination therapy of ezetimibe/rosuvastatin 10/20 mg, or telmisartan 80 mg. Blood samples were collected up to 24 hours postdose at steady state. Geometric mean ratios (GMRs) and their 90% confidence intervals (CIs) of the combination therapy to monotherapy for the maximum plasma concentration (Cmax,ss), and the area under the time-concentration curve within a dosing interval at steady state (AUCtau,ss) were estimated. Among the 36 randomized subjects, 31 subjects completed the study. The GMRs and 90%CIs of Cmax,ss and AUCtau,ss of total ezetimibe were not significantly altered. The Cmax,ss of free ezetimibe was increased (GMR, 1.85; 90%CI, 1.56–2.19) but not for the AUCtau,ss (GMR, 1.16; 90%CI, 1.06–1.26). Similarly, the Cmax,ss of rosuvastatin was increased (GMR, 2.13; 90%CI, 1.88–2.43) without a change in the AUCtau,ss (GMR, 1.09; 90%CI, 1.03–1.15). The Cmax,ss (GMR, 1.16; 90%CI, 1.01–1.32) and AUCtau,ss (GMR, 1.26; 90%CI, 1.17–1.37) of telmisartan were slightly increased. Considering the therapeutic range of the components, the interaction would have limited clinical impact.

Original languageEnglish
Pages (from-to)1290-1296
Number of pages7
JournalClinical Pharmacology in Drug Development
Volume10
Issue number11
DOIs
StatePublished - Nov 2021

Keywords

  • drug-drug interactions
  • dyslipidemia
  • ezetimibe
  • hypertension
  • rosuvastatin
  • telmisartan

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