Hormone therapy for breast cancer, with an emphasis on the pure antiestrogen fulvestrant: mode of action, antitumor efficacy and effects on bone health

Abstract

Breast cancer is a major health problem in women of developed Western countries. Whereas estrogen receptor (ER) may be involved in many cases in breast carcinogenesis, its expression in breast tumors may predict a favorable response to hormone therapy. In this review, we report the role played by ER in breast cancer and compare the effects and mechanisms of action of partial (tamoxifen) and pure (fulvestrant) antiestrogens, as well as of aromatase inhibitors. Moreover, as ER also has a critical role in bone metabolism, we review the beneficial and adverse effects of breast cancer hormone therapy on bone health, with a particular emphasis on fulvestrant, the only pure antiestrogen recently approved by the FDA for Phase III clinical trials. We conclude that, because of its therapeutic efficacy and its seemingly minimal effect on bone integrity, fulvestrant represents a new option for the hormonal treatment of breast cancer that deserves further clinical evaluation.