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Xenobiotica
the fate of foreign compounds in biological systems
Volume 46, 2016 - Issue 1
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Clinical Pharmacokinetics and Metabolism

Characterization of fimasartan metabolites in human liver microsomes and human plasma

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Pages 40-51 | Received 10 Mar 2015, Accepted 29 Apr 2015, Published online: 11 Jun 2015

References

  • Baranczewski P, Stańczak A, Sundberg K, et al. (2006). Introduction to in vitro estimation of metabolic stability and drug interactions of new chemical entities in drug discovery and development. Pharmacol Rep 58:453–72
  • Castro-Perez JM. (2007). Current and future trends in the application of HPLC–MS to metabolite-identification studies. Drug Dis Today 12:249–56
  • Chi YH, Lee H, Paik SH, et al. (2011). Safety, tolerability, pharmacokinetics, and pharmacodynamics of fimasartan following single and repeated oral administration in the fasted and fed states in healthy subjects. Am J Cardiovasc Drugs 11:335–46
  • Christ DD, Wong PC, Wong YN, et al. (1994). The pharmacokinetics and pharmacodynamics of the angiotensin II receptor antagonist losartan potassium (DuP 753/MK 954) in the dog. J Pharmacol Exp Ther 268:1199–205
  • Davi H, Tronquet C, Miscoria G, et al. (2000). Disposition of irbesartan, an angiotensin II AT1-receptor antagonist, in mice, rats, rabbits, and macaques. Drug Metab Dispos 28:79–88
  • Gao H, Materne OL, Howe DL, Brummel CL. (2007). Method for rapid metabolite profiling of drug candidates in fresh hepatocytes using liquid chromatography coupled with a hybrid quadrupole linear ion trap. Rapid Commun Mass Spectrom 21:3683–93
  • Hamilton RA, Garnett WR, Kline BJ. (1981). Determination of mean valproic acid serum level by assay of a single pooled sample. Clin Pharmacol Ther 29:408–13
  • Han J, Park SJ, Thu VT, et al. (2013). Effects of the novel angiotensin II receptor type I antagonist, fimasartan on myocardial ischemia/reperfusion injury. Int J Cardiol 168:2851–9
  • Huang J, Bathena SP, Alnouti Y. (2010). Metabolite profiling of praziquantel and its analogs during the analysis of in vitro metabolic stability using information-dependent acquisition on a hybrid triple quadrupole linear ion trap mass spectrometer. Drug Metab Pharmacokinet 25:487–99
  • Ieiri I, Nishimura C, Maeda K, et al. (2011). Pharmacokinetic and pharmacogenomic profiles of telmisartan after the oral microdose and therapeutic dose. Pharmacogenet Genomics 21:495–505
  • Jeon H, Lim KS, Shin KH, et al. (2012). Assessment of the drug–drug interactions between fimasartan and hydrochlorothiazide in healthy volunteers. J Cardiovasc Pharmacol 59:84–91
  • Jeong ES, Kim YW, Kim HJ, et al. (2015). Glucuronidation of fimasartan, a new angiotensin receptor antagonist, is mainly mediated by UGT1A3. Xenobiotica 45:10–18
  • Kim JH, Lee JH, Paik SH, et al. (2012a). Fimasartan, a novel angiotensin II receptor antagonist. Arch Pharm Res 35:1123–6
  • Kim HM, Oh SJ, Park SK, et al. (2008). In vitro metabolism of KBH-A40, a novel delta-lactam-based histone deacetylase (HDAC) inhibitor, in human liver microsomes and serum. Xenobiotica 38:281–93
  • Kim TH, Shin S, Bashir M, et al. (2014). Pharmacokinetics and metabolite profiling of fimasartan, a novel antihypertensive agent, in rats. Xenobiotica 44:913–25
  • Kim TW, Yoo BW, Lee JK, et al. (2012b). Synthesis and antihypertensive activity of pyrimidin-4(3)-one derivatives as losartan analogue for new angiotensin II receptor type 1 (AT1) antagonist. Bioorg Med Chem Lett 22:1649–54
  • Kuhnz W, Gieschen H. (1998). Predicting the oral bioavailability of 19-nortestosterone progestins in vivo from their metabolic stability in human liver microsomal preparations in vitro. Drug Metab Dispos 26:1120–7
  • Lee SE, Kim YJ, Lee HY, et al. (2012). Efficacy and tolerability of fimasartan, a new angiotensin receptor blocker, compared with losartan (50/100 mg): a 12-week, phase III, multicenter, prospective, randomized, double-blind, parallel-group, dose escalation clinical trial with an optional 12-week extension phase in adult Korean patients with mild-to-moderate hypertension. Clin Ther 34:552–68, 568.e1–9
  • Lee HW, Lim MS, Seong SJ, et al. (2011). Effect of age on the pharmacokinetics of fimasartan (BR-A-657). Expert Opin Drug Metab Toxicol 7:1337–44
  • Obach RS. (2001). The prediction of human clearance from hepatic microsomal metabolism data. Curr Opin Drug Discov Dev 4:36–44
  • Obach RS, Baxter JG, Liston TE, et al. (1997). The prediction of human pharmacokinetic parameters from preclinical and in vitro metabolism data. J Pharmacol Exp Ther 283:46–58
  • Pang KS, Rowland M. (1977). Hepatic clearance of drugs. I. Theoretical considerations of a ‘well-stirred’ model and a ‘parallel tube’ model: influence of hepatic blood flow, plasma and blood cell binding, and the hepatocellular enzymatic activity on hepatic drug clearance. J Pharmacokinet Biopharm 5:625–53
  • Park JB, Sung KC, Kang SM, Cho EJ. (2013). Safety and efficacy of fimasartan in patients with arterial hypertension (Safe-KanArb study): an open-label observational study. Am J Cardiovasc Drugs 13:47–56
  • Rousu T, Herttuainen J, Tolonen A. (2010). Comparison of triple quadrupole, hybrid linear ion trap triple quadrupole, time-of-flight and LTQ-Orbitrap mass spectrometers in drug discovery phase metabolite screening and identification in vitro – amitriptyline and verapamil as model compounds. Rapid Commun Mass Spectrom 24:939–57
  • Trunzer M, Faller B, Zimmerlin A. (2009). Metabolic soft spot identification and compound optimization in early discovery phases using MetaSite and LC–MS/MS validation. J Med Chem 52:329–35
  • Yao M, Ma L, Humphreys WG, Zhu M. (2008). Rapid screening and characterization of drug metabolites using a multiple ion monitoring-dependent MS/MS acquisition method on a hybrid triple quadrupole-linear ion trap mass spectrometer. J Mass Spectrom 43:1364–75
  • Yi S, Kim TE, Yoon SH, et al. (2011). Pharmacokinetic interaction of fimasartan, a new angiotensin II receptor antagonist, with amlodipine in healthy volunteers. J Cardiovasc Pharm 57:682–9

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