, Volume 67, Issue 16, pp 2335–2353

Estrogen Receptor Modulators and Down Regulators

Optimal Use in Postmenopausal Women With Breast Cancer
Review Article

DOI: 10.2165/00003495-200767160-00004

Cite this article as:
Baumann, C.K. & Castiglione-Gertsch, M. Drugs (2007) 67: 2335. doi:10.2165/00003495-200767160-00004


Endocrine treatments have been used in breast cancer since 1896, when Beatson reported on the results of oophorectomy for advanced breast cancer. In the second half of the last century, different endocrine-based compounds were developed and, in this review, the role of the selective estrogen receptor modulators (SERMs) and selective estrogen receptor down regulators (SERDs) in the postmenopausal setting are discussed.

Tamoxifen is the most investigated and most widely used representative of these agents, and has been introduced in the advanced disease, in the neoadjuvant and adjuvant setting, and for the prevention of the disease. Its role has been challenged in recent years by the introduction of third-generation aromatase inhibitors that have proven higher activities than tamoxifen with different toxicity patterns.

Several other SERMs have been investigated, but none have been clearly superior to tamoxifen.

SERDs act as pure estrogen antagonists and should compare favourably to tamoxifen. For the time being, they have been used in the treatment of advanced breast cancers and their role in other settings still needs investigation.

The increased use of aromatase inhibitors as first-line endocrine therapy has resulted in new discussions regarding the role that tamoxifen and other SERMs or SERDs may play in breast cancer. The sequencing of endocrine therapies in hormone-sensitive breast cancer remains a very important research issue.

Copyright information

© Adis Data Information 2007

Authors and Affiliations

  • Christa K. Baumann
    • 1
  • Monica Castiglione-Gertsch
    • 1
    • 2
  1. 1.Clinic and Policlinic for Medical Oncology, InselspitalBernSwitzerland
  2. 2.International Breast Cancer Study Group Coordinating CenterBernSwitzerland

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