Serms and Pure Anti-Oestrogens

Abstract

The oestrogen sensitivity of breast cancer was first recognised in 1836. Initially oestrogen levels were suppressed with surgical procedures such as oophorectomy, adrenalectomy and hypophysectomy. Recognition of the oestrogen receptor and development the first antioestrogens occurred in the 1960s. Since that time, tamoxifen has become one of the most widely prescribed antitumour agents across the world. Tamoxifen is not a pure antioestrogen, and it’s agonist actions produce clinically important effects on the endometrium, bone mineral density and the incidence of ischaemic heart disease. Hence the term Selective Estrogen Receptor Modulator (SERM) is a more accurate description for tamoxifen and related agents. Recently pure antieostrogens have now entered into clinical practice. SERMs were initially used for metastatic or locally advanced breast cancers, but are now widely employed as adjuvant therapy for early operable tumours. Concerns regarding the side-effects of SERMs have been compounded by recent data supporting new indications for these agents. These include the preventation of breast cancer in high risk women, and an expanded role as treatment for in situ breast cancer (DCIS). The number of women exposed to this expanding group of drugs is therefore set to dramatically increase.