Expert review of anticancer therapy

Role of fulvestrant in the management of postmenopausal breast cancer.

PMID 22050013


Fulvestrant is a form of endocrine therapy used in the treatment of postmenopausal breast cancer. It has a unique mechanism of action in that it causes the degradation of estrogen receptor and therefore has been labeled a selective estrogen receptor downregulator. Unlike the selective estrogen receptor modulator tamoxifen, it has no agonistic properties and is therefore a pure anti-estrogen. Given its low level of bioavailability and presystemic metabolism, it has been formulated as an intramuscular injection. A number of dosing regimens have been utilized - these include a dose of 250 mg monthly ('approved dose'), an initial 500 mg followed by 250 mg on days 14 and 28, and thereafter 250 mg every 28 days ('loading dose'), or 500 mg on days 0, 14 and 28, and thereafter every 28 days ('high dose'). This article will review its unique mode of action and preclinical data, as well as clinical data for different dosing regimens and data for its combination with aromatase inhibitors. Fulvestrant is a well-tolerated drug and its toxicities will also be reviewed. The optimal position of fulvestrant in sequential endocrine therapy has yet to be defined.