Influence of hepatic dysfunction on the pharmacokinetics and safety of fimasartan

Choon Ok Kim, Hae Wan Lee, Eun Sil Oh, Sook Jin Seong, Do Young Kim, Joomi Lee, Sang Hoon Ahn, Young Ran Yoon, Chang Min Cho, Min Soo Park

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Abstract

This study was designed to assess the pharmacokinetics (PK) and safety of fimasartan, an angiotensin II type 1 receptor blocker, in hepatic impairment patients as compared with healthy subjects. An open-label, single-dose, parallel study was conducted in 6 healthy male volunteers and 12 subjects with hepatic impairment. Healthy subjects were matched with hepatic dysfunction patients on the basis of age, gender, and body weight. After a single 120-mg oral administration of fimasartan, PK parameters and safety were analyzed between the hepatic dysfunction groups and healthy group. Compared with the healthy subjects, the geometric mean ratio and 90% confidence intervals for the maximum plasma concentration and the mean area under the plasma concentration-time curve from 0 to infinity (AUC)inf were 0.77 (0.24-2.47) and 1.11 (0.50-2.46), respectively, for the mild hepatic impairment and 6.55 (3.56-12.03) and 5.17 (4.19-6.37), respectively, for moderate hepatic impairment. However, there was no significant difference in time to peak plasma concentration (t max) and elimination half-life, and there were no serious or severe adverse events in all subjects. Subjects with mild hepatic impairment exhibited similar bioavailability compared with healthy subjects, whereas subjects with moderate hepatic impairment seemed to exhibit a higher level of systemic exposure to fimasartan than healthy subjects. In addition, all subjects were tolerable with fimasartan.

Original languageEnglish
Pages (from-to)524-529
Number of pages6
JournalJournal of Cardiovascular Pharmacology
Volume62
Issue number6
DOIs
Publication statusPublished - 2013 Dec 1

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All Science Journal Classification (ASJC) codes

  • Pharmacology
  • Cardiology and Cardiovascular Medicine

Cite this

Kim, C. O., Lee, H. W., Oh, E. S., Seong, S. J., Kim, D. Y., Lee, J., Ahn, S. H., Yoon, Y. R., Cho, C. M., & Park, M. S. (2013). Influence of hepatic dysfunction on the pharmacokinetics and safety of fimasartan. Journal of Cardiovascular Pharmacology, 62(6), 524-529. https://doi.org/10.1097/FJC.0000000000000010