Aromatase inhibitors in the pharmacotherapy of endometriosis

ABSTRACT

Introduction

Endometriosis is a benign chronic inflammatory disease responsible for debilitating pain and decreased quality of life. The traditional treatment is based on estroprogestins, progestins, GnRH analogs, and surgery. Recently, aromatase inhibitors (AIs) demonstrated good efficacy in controlling symptoms and size of endometriotic implants, mostly because they suppress extraovarian estrogen synthesis, which can enhance the hypoestrogenic state ameliorating symptoms of endometriosis.

Areas covered

Phase I, II, III and IV trials, on the use of AIs used for the treatment of endometriosis, have been retrieved. The pharmacokinetics and pharmacodynamics of third-generation non-steroidal AIs have also been investigated. A MEDLINE search has been performed using the following MeSH keywords: ‘endometriosis,’ aromatase inhibitors,’ ‘therapy,’ and ‘treatment’. The timeframe was from 2010 up to November 2022 including reviews, systematic reviews, reports, case series, and retrospective or prospective trials.

Expert opinion

AIs have shown good clinical efficacy in combination with hormonal therapy in disease control, and they represent a promising second-line therapy in selected patients, yet more research is needed on alternative drug delivery systems and better control of adverse effects. In postmenopausal women in which surgery is contraindicated, AIs represent an excellent treatment option. Their application in routine clinical practice remains limited by adverse effects.

KEYWORDS:

• Aromatase inhibitors
• endometriosis
• pharmacotherapy
• pharmacology
• chronic pelvic pain

Article highlights

• Anastrozole and letrozole are the most investigated compounds in the treatment of endometriosis.

• Clinical trials showed that AIs are effective in combination with hormonal therapy but have more side effects.

• Use of AIs in postmenopausal patients is very promising.

• Topical administration may reduce the adverse effect burden while maintaining good disease control, but more studies are needed.

Acknowledgments

The authors want to thank Valeria Scotti (SSD Biostatistica e Clinical Trial Center, IRCCS Fondazione Policlinico San Matteo of Pavia) for the help in the research strategy design.

Declaration of interest

The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

Reviewer disclosures

Peer reviewers on this manuscript have no relevant financial or other relationships to disclose.

Additional information

Funding

This paper was not funded.