title: Fulvestrant.
abstract: Fulvestrant, a novel oestrogen receptor (ER) downregulator, is a pure anti-oestrogen which completely blocks the trophic actions of oestrogens without exerting any partial agonist effects. It reduces expression of oestrogen receptor, progesterone receptor and proliferative and cell turnover indices. The drug is well-tolerated with minimal systemic side effects. Large randomised trials have demonstrated similar efficacy to anastrozole in the treatment of postmenopausal advanced breast cancer. While results of a Phase III trial comparing fulvestrant with tamoxifen as first-line endocrine therapy for postmenopausal advanced breast cancer are awaited, future studies on its role in adjuvant and neoadjuvant settings, as well as in premenopausal women are required. With the role of tamoxifen as the gold standard of first-line therapy being challenged by the third generation aromatase inhibitors, direct comparison of the latter with fulvestrant in the first-line setting may also be worthwhile.
authors.affiliation: Professorial Unit of Surgery, Nottingham City Hospital, Hucknall Road, Nottingham NG5 1PB, UK. kl.cheung@nottingham.ac.uk
authors.forename: Kwok Leung
authors.initials: KL
authors.lastname: Cheung
authors.forename: John F R
authors.initials: JF
authors.lastname: Robertson
mesh_terms: D000818:Animals; D018931:Antineoplastic Agents, Hormonal / Q000009:adverse effects / Q000494:pharmacology; D001943:Breast Neoplasms / Q000188:drug therapy; D000075202:Contraindications; D004305:Dose-Response Relationship, Drug; D004347:Drug Interactions; D004958:Estradiol / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000494:pharmacology; D020847:Estrogen Receptor Modulators / Q000009:adverse effects / Q000494:pharmacology; D005260:Female; D000077267:Fulvestrant; D006801:Humans; D016032:Randomized Controlled Trials as Topic; D013629:Tamoxifen / Q000627:therapeutic use
chemical_list: D018931:Antineoplastic Agents, Hormonal; D020847:Estrogen Receptor Modulators; D013629:Tamoxifen; D000077267:Fulvestrant; D004958:Estradiol