Antioestrogens are a group of compounds which are at present attracting much attention both in scientific research and in clinical practice. The purpose of this article is to review the current understanding in both fields.Definitions of an antioestrogen. In the broadest sense, an antioestrogen is a substance which counteracts the activity of oestrogens (Terenius, 1974). For the purpose of this review, however, the definition will be restricted by the following considerations.(a) Direct eflect on oestrogen activity. Some substances do not counteract oestrogens directly but block subsequent events set in train by oestrogens. Hence substances which alter oestrogen response by interfering with protein or RNA synthesis in a target cell or with oestrogen metabolism in, say, the liver are not considered as antioestrogens in the context of this article. Neither is a substance which suppresses oestrogen secretion considered as an antioestrogen. Certain substances like androgens and progestogens can modify rather than counteract oestrogen effects. These substances do not interfere with oestrogen uptake by a target cell but modify the oestrogen response by stimulating other cell components (Terenius & Ljungkvist, 1972).(b) Blocking of oestrogen receptors. Antioestrogens have an affinity for the protein oestrogen-receptors in the target cell cytoplasm. Terenius (1970) has divided antioestrogens into two categories depending on the duration of receptor retention. The first group of antioestrogens is effective following systemic administration and has a sustained effect in blocking oestrogen stimulation : the second group is most effective when given locally, appears to be only transiently attached to the receptor but impedes the response to other oestrogens like oestradiol-17P (see Table 1).The scope of the review 1. Which oestrogen is blocked? Our interest is mainly in oestradiol-17P and to a lesser extent in oestradiol-17% and oestrone as these are the main gonadal oestrogens of the species