Antiestrogens are compounds that inhibit estrogen action by competing for its receptors. Estrogens are involved in the proliferation and differentiation of target cells and are among the main risk factors for breast and uterine cancer. Some antiestrogens, such as Tamoxifen, are used as adjuvant therapy against breast cancer, and have been proposed to be included in prevention programs for women at high risk of cancer. Antiestrogens are classified according to their action mechanisms into Type I or partial (agonistic/antagonistic), and Type II or pure (pure antagonistic). Advancements in the development of new antiestrogens and their clinical importance are reviewed in this paper, as well as their mechanism of action and clinical applications.