Clinical Therapeutics
Volume 34, Issue 2 , Pages 305-313 , February 2012

Pharmacokinetic Comparison of 2 Formulations of Anastrozole (1 mg) in Healthy Korean Male Volunteers: A Randomized, Single-Dose, 2-Period, 2-Sequence, Crossover Study

  • Yook-Hwan Noh, MD

      Affiliations

    • Department of Clinical Pharmacology and Therapeutics, College of Medicine, University of Ulsan, Asan Medical Center, Seoul, Korea
  • ,
  • Young-Ju Ko, MD

      Affiliations

    • Department of Clinical Pharmacology and Therapeutics, College of Medicine, University of Ulsan, Asan Medical Center, Seoul, Korea
  • ,
  • Sang-Heon Cho, MD, PhD

      Affiliations

    • Department of Clinical Pharmacology and Therapeutics, College of Medicine, University of Ulsan, Asan Medical Center, Seoul, Korea
  • ,
  • Jong-Lyul Ghim, MD, PhD

      Affiliations

    • Department of Clinical Pharmacology, Busan Paik Hospital, Busan, Korea
  • ,
  • Sangmin Choe, MD, PhD

      Affiliations

    • Clinical Trials Center, Pusan National University Hospital, Busan, Korea
  • ,
  • Jin Ah Jung, MD, PhD

      Affiliations

    • Department of Clinical Pharmacology and Therapeutics, Samsung Medical Center, Seoul, Korea
  • ,
  • Un-Jib Kim, MD

      Affiliations

    • Department of Clinical Pharmacology and Therapeutics, College of Medicine, University of Ulsan, Asan Medical Center, Seoul, Korea
  • ,
  • Seok-Joon Jin, MD

      Affiliations

    • Department of Clinical Pharmacology and Therapeutics, College of Medicine, University of Ulsan, Asan Medical Center, Seoul, Korea
  • ,
  • Hyun-Jung Park

      Affiliations

    • Clinical Trial Center, Asan Medical Center, Seoul, Korea
  • ,
  • Geun-Seog Song, PhD

      Affiliations

    • Regulatory and Clinical Development Division, Pharmaceutical BU, CJ Cheiljedang Co., Ltd., Seoul, Korea
  • ,
  • Hyeong-Seok Lim, MD, PhD

      Affiliations

    • Department of Clinical Pharmacology and Therapeutics, College of Medicine, University of Ulsan, Asan Medical Center, Seoul, Korea
    • Corresponding Author InformationAddress correspondence to: Hyeong-Seok Lim, MD, PhD, 88, Olympic-ro 43-gil, Songpa-gu, Seoul, Korea, 138-736
  • ,
  • Kyun-Seop Bae, MD, PhD

      Affiliations

    • Department of Clinical Pharmacology and Therapeutics, College of Medicine, University of Ulsan, Asan Medical Center, Seoul, Korea

,Accepted 3 January 2012.

References 

  1. Cole PA , Robinson CH . Mechanism and inhibition of cytochrome P-450 aromatase . J Med Chem . 1990;33:2933–2942
  2. Masamura S , Adlercreutz H , Harvey H , et al.  Aromatase inhibitor development for treatment of breast cancer . Breast Cancer Res Treat . 1995;33:19–26
  3. Longcope C , Pratt JH , Schneider SH , Fineberg SE . Aromatization of androgens by muscle and adipose tissue in vivo . J Clin Endocrinol Metab . 1978;46:146–152
  4. Miller WR . Aromatase activity in breast tissue . J Steroid Biochem Mol Biol . 1991;39:783–790
  5. Couzinet B , Meduri G , Lecce MG , et al.  The postmenopausal ovary is not a major androgen-producing gland . J Clin Endocrinol Metab . 2001;86:5060–5066
  6. Hemsell DL , Grodin JM , Brenner PF , et al.  Plasma precursors of estrogen (II. Correlation of the extent of conversion of plasma androstenedione to estrone with age) . J Clin Endocrinol Metab . 1974;38:476–479
  7. Ryan KJ . Biological aromatization of steroids . J Biol Chem . 1959;234:268–272
  8. Meigs RA , Ryan KJ . Cytochrome P-450 and steroid biosynthesis in the human placenta . Biochim Biophys Acta . 1968;165:476–482
  9. Fishman J , Raju MS . Mechanism of estrogen biosynthesis (Stereochemistry of C-1 hydrogen elimination in the aromatization of 2 beta-hydroxy-19-oxoandrostenedione) . J Biol Chem . 1981;256:4472–4477
  10. Lonning PE . Aromatase inhibitors in breast cancer . Endocr Relat Cancer . 2004;11:179–189
  11. Yu J , He J , Zhang Y , et al.  An ultraperformance liquid chromatography-tandem mass spectrometry method for determination of anastrozole in human plasma and its application to a pharmacokinetic study . Biomed Chromatogr . 2011;25:511–516
  12. Bonneterre J , Buzdar A , Nabholtz JM , et al.  Anastrozole is superior to tamoxifen as first-line therapy in hormone receptor positive advanced breast carcinoma . Cancer . 2001;92:2247–2258
  13. Milla-Santos A , Milla L , Portella J , et al.  Anastrozole versus tamoxifen as first-line therapy in postmenopausal patients with hormone-dependent advanced breast cancer: a prospective, randomized, phase III study . Am J Clin Oncol . 2003;26:317–322
  14. Howell A , Robertson JF , Vergote I . A review of the efficacy of anastrozole in postmenopausal women with advanced breast cancer with visceral metastases . Breast Cancer Res Treat . 2003;82:215–222
  15. Sanford M , Plosker GL . Anastrozole: a review of its use in postmenopausal women with early-stage breast cancer . Drugs . 2008;68:1319–1340
  16. Hiscox S , Davies EL , Barrett-Lee P . Aromatase inhibitors in breast cancer . Maturitas . 2009;63:275–279
  17. Korea Food and Drug Administration . Bioequivalence guideline in Korea [in Korean] . http://www.kfda.go.kr/index.kfda?mid=226&pageNo=1&seq=139&cmd=v Accessed December 9, 2011
  18. Korea good clinical practice (KGCP) guidelines [in Korean] . http://clinicaltrials.kfda.go.kr/guide/laws/board_list.jsp?category_seq=12 Accessed December 09, 2011
  19. Declaration of Helsinki, Ethical Principles for Medical Research Involving Human Subjects . http://www.wma.et/en/30publications/10policies/b3/ 2008; Accessed December 9, 2011
  20. Yates RA , Dowsett M , Fisher GV , et al.  Arimidex (ZD1033): a selective, potent inhibitor of aromatase in postmenopausal female volunteers . Br J Cancer . 1996;73:543–548
  21. Mendes GD , Hamamoto D , Ilha J , et al.  Anastrozole quantification in human plasma by high-performance liquid chromatography coupled to photospray tandem mass spectrometry applied to pharmacokinetic studies . J Chromatogr B Analyt Technol Biomed Life Sci . 2007;850:553–559
  22. Duan G , Liang J , Zuo M . Rapid determination of anastrozole in plasma by gas chromatography with electron capture detection and its application to an oral pharmacokinetic study in healthy volunteers . Biomed Chromatogr . 2002;16:400–403
  23. Malcolm Rowland  , Tozer TN . Clinical Pharmacoknetics and Pharmacodynamics: Concepts and Applications . In: 4th ed.. Philadelphia, Pa: WoltersKluwer/LippincottWilliams & Wilkins; 2011;p. 159–176 293–324, 687–689
  24. Apostolou C , Dotsikas Y , Kousoulos C , Loukas YL . Development and validation of an improved high-throughput method for the determination of anastrozole in human plasma by LC-MS/MS and atmospheric pressure chemical ionization . J Pharm Biomed Anal . 2008;48:853–859
  25. Tredway DR , Buraglio M , Hemsey G , Denton G . A phase I study of the pharmacokinetics, pharmacodynamics, and safety of single- and multiple-dose anastrozole in healthy, premenopausal female volunteers . Fertil Steril . 2004;82:1587–1593
  26. Plourde PV , Dyroff M , Dukes M . Arimidex: a potent and selective fourth-generation aromatase inhibitor . Breast Cancer Res Treat . 1994;30:103–111
  27. Diletti E , Hauschke D , Steinijans VW . Sample size determination for bioequivalence assessment by means of confidence intervals . Int J Clin Pharmacol Ther Toxicol . 1991;29:1–8
  28. Kutner MH , Nachtsheim CJ , Neter J , Li W . In: Applied Linear Statistical Models . 5th ed.. New York, NY: McGraw-Hill/Irwin; 2005;
  29. Yuan J , Wang PQ , Ge SR , et al.  Pharmacokinetics of anastrozole in Chinese male volunteers . Acta Pharmacol Sin . 2001;22:573–576
  30. Yates RA , Wong J , Seiberling M , et al.  The effect of anastrozole on the single-dose pharmacokinetics and anticoagulant activity of warfarin in healthy volunteers . Br J Clin Pharmacol . 2001;51:429–435
  31. Lorkowski G , Lucker PW , Petersen G , et al.  Bioequivalence of two commercially available tamoxifen tablet formulations in healthy male volunteers . Methods Find Exp Clin Pharmacol . 1994;16:443–447

PII: S0149-2918(12)00009-4

doi: 10.1016/j.clinthera.2012.01.008

Clinical Therapeutics
Volume 34, Issue 2 , Pages 305-313 , February 2012