page_title: Steroidal aromatase inhibitor
section_title: 3rd generation
hierarchical_section_title: Steroidal aromatase inhibitor / Examples of agents / 3rd generation
caption_attribution_description: Structure of Testolactone
context_page_description: Steroidal aromatase inhibitors are a class of drugs that are mostly used for treating breast cancer in postmenopausal women. High levels of estrogen in breast tissue increases the risk of developing breast cancer and the enzyme aromatase is considered to be a good therapeutic target when treating breast cancer due to it being involved in the final step of estrogen biosynthetic pathway and also its inhibitation will not affect production of other steroids. Aromatase Inhibitors are classified into two categories based on their structure, nonsteroidal and steroidal; the latter resemble the structure of androstenedione. Steroidal aromatase inhibitors irreversibly inhibit the enzyme by binding covalently to the binding site of aromatase so the substrate can't access it.
context_section_description: Exemestane is the only steroidal 3rd generation aromatase inhibitor and it has the advantage over formestane in being more potent and can be administrated orally. Clinical studies have shown that 25 mg/day causes 97,9% suppression of aromatase.
caption: Figure 2: Structure of testolactone
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