Figure 2. Differences in structure of antiaromatase agents.

stimulation in postmenopausal patients, but was only partly effective in competing with the high hormone levels in premenopausals.

Considering other SERMS currently available, toremifene has been found of similar efficacy and with a similar side-effect profile compared to tamoxifen (54-56); thus, the two treatment options are considered similar with respect to antitumour efficacy.

A novel class of estrogen receptor modifiers are the so-called SERDS (selective estrogen receptor downregulators), represented with fulvestrant (Fig. 3). Being a steroid derivative with a long aliphatic chain at its 7-position, fulvestrant has a chemical structure distinct from the SERMS. Importantly, fulvestrant is devoid of any intrinsic estrogen agonistic activity, and it seems to act by at least two distinct mechanisms: receptor blocking, but also receptor downregulation (57, 58).

Considering clinical trials, fulvestrant has been compared to anastrozole second-line (in patients failing tamoxifen) as well as to tamoxifen as first-line therapy for metastatic disease (59-61). Overall, results from these studies have suggested fulvestrant to be of similar clinical efficacy to anastrozole as well as tamoxifen. A major disadvantage with this compound is its need for parenteral administration.

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