Aromatase, its inhibitors and their use in breast cancer treatment

Abstract

Aromatase, a cytochrome P450 enzyme, catalyses the rate-limiting step in the biosynthesis of estrogens. Many processes in male and female development and reproduction and especially in the growth of hormone-dependent cancers, are dependent on estrogens. Therefore, controlling estrogen production by inhibition of aromatase is a logical treatment strategy. Two classes of aromatase inhibitors, steroidal and non-steroidal compounds, are now coming into use. Among the steroid substrate analogs, 4-hydroxyandrostenedione has been shown to be effective in breast cancer patients with advanced disease and was recently approved for treatment in the United Kingdom. Several highly potent and selective non-steroidal inhibitors are now in clinical trials. The variety of compounds that act as aromatase inhibitors should provide breast cancer patients with a number of new treatment options.