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.

• Authors: A M Brodie
• Journal: Pharmacology & therapeutics (Pharmacol Ther) Vol. 60 Issue 3 Pg. 501-15 (Dec 1993) ISSN: 0163-7258 [Print] England
• PMID: 8073072 (Publication Type: Journal Article, Research Support, U.S. Gov't, P.H.S., Review)

Chemical References

• Antineoplastic Agents
• Aromatase Inhibitors
• Estrogens
• Aminoglutethimide
• Androstenedione
• Pargyline
• Aromatase
• plomestane
• formestane

Topics

• Aminoglutethimide (therapeutic use)
• Androstenedione (analogs & derivatives, blood, pharmacokinetics, therapeutic use)
• Antineoplastic Agents (blood, pharmacokinetics, therapeutic use)
• Aromatase (physiology)
• Aromatase Inhibitors
• Breast Neoplasms (drug therapy, etiology, metabolism)
• Estrogens (metabolism)
• Half-Life
• Humans
• Neoplasms, Hormone-Dependent (drug therapy, etiology, metabolism)
• Pargyline (analogs & derivatives, pharmacokinetics, therapeutic use)