Aromatase is a cytochrome P-450 exzyme complex which catalyzes the biosynthetic transformation of androgens to estrogens. Estrogen biosynthesis occurs not only in the female reproductive tissues, but also in such diverse sites as testes, adipose tissues and muscles.We review here evidences and advances in characterizing aromatase and its inhibitors. Topics of aromatase inhibitors are outlined by categorizing them in two classes ; competitive inhibitors and irreversible suicide inhibitors.Possible usefulness of selective and powerful aromatase inhibitors in the therapy of estrogen-dependent breast cancer promoted the research in this area.