Pharmacokinetics of third-generation aromatase inhibitors

作者: Per Lønning , Christian Pfister , Andrea Martoni , Claudio Zamagni

DOI: 10.1016/S0093-7754(03)00305-1

关键词:

摘要: The latest generation of nonsteroidal aromatase inhibitors (anastrozole and letrozole) has been approved by the US Food Drug Administration for use in first- second-line treatment postmenopausal women with hormone receptor-positive (or unknown) breast cancer. steroidal agent exemestane is currently being evaluated first line. In addition, these agents are adjuvant neoadjuvant settings. Because preclinical studies have suggested some differences efficacy to inhibit aromatase, it important evaluate whether properties actually translate into meaningful clinical setting. pharmacokinetic each inhibitor influences their ability perform effectively. Examination data suggests uptake rates, half-life elimination, metabolism, clearance rates that could influence efficacy. However, significance effectiveness over long-term remains be determined.

参考文章(74)
Per Eystein Lønning, Jürgen Geisler, Dag Clement Johannessen, Hans-Peter Gschwind, Felix Waldmeier, Werner Schneider, Bruno Galli, Tammo Winkler, Wolfgang Blum, Hans-Peter Kriemler, William Russell Miller, Johann Werner Faigle, None, Pharmacokinetics and metabolism of formestane in breast cancer patients The Journal of Steroid Biochemistry and Molecular Biology. ,vol. 77, pp. 39- 47 ,(2001) , 10.1016/S0960-0760(01)00029-2
Hironobu Sasano, Hiroshi Nagura, Nobuhiro Harada, Yuji Goukon, Michio Kimura, Immunolocalization of aromatase and other steroidogenic enzymes in human breast disorders Human Pathology. ,vol. 25, pp. 530- 535 ,(1994) , 10.1016/0046-8177(94)90127-9
F. A. MacNeill, S. Jacobs, M. Dowsett, P. E. Lonning, T. J. Powles, The effects of oral 4-hydroxyandrostenedione on peripheral aromatisation in post-menopausal breast cancer patients. Cancer Chemotherapy and Pharmacology. ,vol. 36, pp. 249- 254 ,(1995) , 10.1007/BF00685855
M. A. Blankenstein, J. Szymczak, J. Daroszewski, A. Milenncz, J. H. H. Thijssen, Estrogens in plasma and fatty tissue from breast cancer patients and women undergoing surgery for non-oncological reasons. Gynecological Endocrinology. ,vol. 6, pp. 13- 17 ,(1992) , 10.3109/09513599209081001
J.H.H. Thijssen, M.A. Blankenstein, W.R. Miller, A. Milewicz, Estrogens in tissues: uptake from the peripheral circulation or local production. Steroids. ,vol. 50, pp. 297- 306 ,(1987) , 10.1016/0039-128X(83)90079-X
Paul C. MacDonald, Clare D. Edman, Irwin J. Kerber, Pentti K. Siiteri, Plasma Precursors of Estrogen Gynecologic and Obstetric Investigation. ,vol. 7, pp. 165- 175 ,(1976) , 10.1159/000301332
Danielle M. Colussi, Carole Y. Parisot, Gilbert Y. Lefèvre, Plasma protein binding of letrozole, a new nonsteroidal aromatase enzyme inhibitor. The Journal of Clinical Pharmacology. ,vol. 38, pp. 727- 735 ,(1998) , 10.1002/J.1552-4604.1998.TB04813.X
A.L. Jones, F. MacNeill, S. Jacobs, P.E. Lonning, M. Dowsett, T.J. Powles, The influence of intramuscular 4-hydroxyandrostenedione on peripheral aromatisation in breast cancer patients. European Journal of Cancer. ,vol. 28, pp. 1712- 1716 ,(1992) , 10.1016/0959-8049(92)90074-C
RA Yates, M Dowsett, GV Fisher, A Selen, PJ Wyld, Arimidex (ZD1033): a selective, potent inhibitor of aromatase in postmenopausal female volunteers. British Journal of Cancer. ,vol. 73, pp. 543- 548 ,(1996) , 10.1038/BJC.1996.94