Arzoxifene: the evidence for its development in the management of breast cancer
Authors Jackson L, Cheung KL, Buzdar AU, Robertson JFR
Published 15 December 2007 Volume 2007:2(4)
Lee R. Jackson1, Kwok L. Cheung1, Aman U. Buzdar2, John F. R. Robertson1
1Professorial Unit of Surgery, Nottingham City Hospital, Nottingham, UK; 2The University of Texas, M.D. Anderson Cancer Center, Houston, Texas, USA
Introduction: Endocrine therapy is an important and integral part of breast cancer management. Selective estrogen receptor modulators (SERMs), such as tamoxifen, remain a vital component in the endocrine therapy armamentarium. However the “ideal SERM”, which has antagonist effects on the breast and endometrium but beneficial agonistic effects on bone and lipid profile, remains to be found.
Aim: The aim of this review is to examine the evidence for arzoxifene as the “ideal SERM.”
Evidence review: Arzoxifene showed initial promise as the “ideal SERM” in preclinical, phase I, and phase II clinical studies. It appeared to have powerful antiestrogenic effects on breast cancer and endometrium, with equally strong favorable estrogenic effects on bone and lipid profile, minimal side effects, and good oral bioavailability. However, phase III trial data found it to be inferior to tamoxifen, bringing an apparent end to its investigation as a breast cancer treatment.
Clinical potential: Despite early promise as the “ideal SERM”, results from a phase III trial have relegated arzoxifene to research in breast cancer prevention and osteoporosis treatment.
Key words: arzoxifene, selective estrogen receptor modulators (SERM), breast cancer
This work is published and licensed by Dove Medical Press Limited. The full terms of this license are available at https://www.dovepress.com/terms.php and incorporate the Creative Commons Attribution - Non Commercial (unported, v3.0) License. By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed. For permission for commercial use of this work, please see paragraphs 4.2 and 5 of our Terms.Download Article [PDF]