Aromatase inhibitors: the next generation of therapeutics for endometriosis?

Objective and Design

To review the role of aromatase inhibitors (AIs) in the treatment of endometriosis.

Conclusion(s)

Endometriosis is a common estrogen-dependent disorder that can result in substantial morbidity, including pelvic pain, multiple operations, and infertility. Approximately only half of women with endometriosis get pain relief from existing medical or surgical treatments. Medical treatments usually are directed at inhibiting estrogen action or its production from the ovaries and do not address local estrogen biosynthesis by the aromatase enzyme in endometriotic lesions. A single gene encodes aromatase, which is the final enzyme in the estrogen biosynthesis pathway, and its inhibition effectively eliminates estrogen production. The recently introduced highly specific AIs have successfully treated pelvic pain and significantly reduced the lesion size. In premenopausal women, an AI alone may induce ovarian folliculogenesis, and thus AIs are combined with a progestin, a combination oral contraceptive, or a GnRH analogue. The side-effect profile of AIs administered in combination with an oral contraceptive or a progestin is remarkably benign. We review herein the published clinical evidence for the use of AIs in the treatment of endometriosis.

Key Words:  Endometriosis , aromatase , aromatase inhibitors , estrogen , oral contraceptive , progestin , norethindrone acetate , endometrium , GnRH agonist , GnRH analogue , letrozole , anastrozole , exemestane