Selective oestrogen receptor modulators (SERMs) are compounds with a mixed agonist/antagonist activity on oestrogen receptors. An ideal SERM is a compound with an oestrogen antagonist effect on the breast and uterus but oestrogen agonist effect on bone. Beside tamoxifen, a group of well-investigated SERMs is represented by raloxifene, LY-353381 (SERM3), EM-800 and CP-336156. On an empirical basis, tamoxifen has been used to pharmacologically treat desmoid tumours. Recently, raloxifene, a second-generation SERM, has been used in the treatment of familial adenomatous polyposis patients affected by desmoid tumour. The mechanisms through which these molecules affect desmoid tumour growth appear to be due, in part, to the fact that SERMs may act independently of oestrogen receptors. The knowledge of the molecular basis of SERM action will make the development of novel synthetic compounds with engineered tissue selectivity possible.