title: Effect of age on the pharmacokinetics of fimasartan (BR-A-657).
abstract: OBJECTIVE
  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 (AUC(0→∞)) 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 AUC(0→∞) was 69.4% higher in older than in young subjects. The maximum plasma concentration (C(max)), time to reach C(max) 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).
authors.affiliation: Kyungpook National University Graduate School and Hospital, Department of Biomedical Science and Clinical Trial Center, Jung-gu, Daegu, Republic of Korea.
authors.forename: Hae Won
authors.initials: HW
authors.lastname: Lee
authors.forename: Mi-Sun
authors.initials: MS
authors.lastname: Lim
authors.forename: Sook Jin
authors.initials: SJ
authors.lastname: Seong
authors.forename: Joomi
authors.initials: J
authors.lastname: Lee
authors.forename: Jeonghyeon
authors.initials: J
authors.lastname: Park
authors.forename: Jeong Ju
authors.initials: JJ
authors.lastname: Seo
authors.forename: Joo-Youn
authors.initials: JY
authors.lastname: Cho
authors.forename: Kyung-Sang
authors.initials: KS
authors.lastname: Yu
authors.forename: Young-Ran
authors.initials: YR
authors.lastname: Yoon
mesh_terms: D000328:Adult; D000367:Age Factors; D000368:Aged; D057911:Angiotensin Receptor Antagonists / Q000009:adverse effects / Q000097:blood / Q000493:pharmacokinetics* / Q000494:pharmacology; D019540:Area Under Curve; D001713:Biphenyl Compounds / Q000009:adverse effects / Q000097:blood / Q000493:pharmacokinetics* / Q000494:pharmacology; D006207:Half-Life; D006801:Humans; D006973:Hypertension / Q000378:metabolism*; D008297:Male; D008875:Middle Aged; D011743:Pyrimidines / Q000009:adverse effects / Q000097:blood / Q000493:pharmacokinetics* / Q000494:pharmacology; D013607:Tablets; D013777:Tetrazoles / Q000009:adverse effects / Q000097:blood / Q000493:pharmacokinetics* / Q000494:pharmacology; D055815:Young Adult
chemical_list: D057911:Angiotensin Receptor Antagonists; D001713:Biphenyl Compounds; D011743:Pyrimidines; D013607:Tablets; D013777:Tetrazoles; C558933:fimasartan