Aromatase inhibitors

Abstract

Oestrogens play an active role in the development of numerous hormone-related disorders, most notably hormone-dependent carcinomas, such as those associated with breast and endometrial tissues. A decrease in oestrogen levels can be achieved by inhibition of aromatase, a key enzyme responsible for oestrogen biosynthesis. A third generation of effective and selective aromatase inhibitors (AIs) has recently been developed for clinical use in postmenopausal breast cancer. The patents discussed in this review describe the synthesis and activities of some novel AIs and the use of AIs for the treatment of hormone-dependent disorders.

• aromatase
• breast cancer
• non-steroidal inhibitors
• steroidal inhibitors