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Abstract
Objectives: The aim of this study was to compare the pharmacokinetics (PK) and safety of fimasartan (BR-A-657), an angiotensin II receptor antagonist, between healthy young (19 – 45 years) and older (≥ 65 years) male subjects.
Methods: To assess the effect of age on PK and safety, fimasartan was administered as a single 240 mg tablet to 12 young and 10 older male subjects, followed by serial blood sampling over 48 h. Plasma concentrations of fimasartan were analyzed using validated HPLC-MS/MS. Clinical and laboratory adverse events were assessed.
Results: After oral administration of 240 mg fimasartan, the mean area under the plasma concentration-time curve from time zero to infinity (AUC0→∞) was 2899.0 ng/ml/h in the older, which was significantly greater than in young subjects (1767.4 ng/ml/h; p = 0.03). The geometric mean AUC0→∞ was 69.4% higher in older than in young subjects. The maximum plasma concentration (Cmax), time to reach Cmax and elimination half-life for fimasartan did not differ significantly between the older and young groups. Importantly, fimasartan was well tolerated during this study.
Conclusions: While some PK parameters were statistically different between the two groups, the effect of age on the PK was modest (e.g., AUC increase < twofold in older subjects).
Acknowledgements
There is some overlap (in part) between this manuscript and an abstract that was presented (poster) in the 2011 American Society of Clinical Pharmacology and Therapeutics (ASCPT) annual meeting (from 2 to 5 March 2011 in Dallas, TX, USA). The authors would like to thank J Choi and YK Jun, Boryung Pharmaceutical Co. Ltd., for their helpful comments. The authors would like to thank R Twaen and the editors from Textcheck Inc., Basseterre, St. Kitts, check for assistance in checking the English of this manuscript. HW Lee and M-s Lim contributed equally to this work.