Current approaches to overcome the side effects of GnRH analogs in the treatment of patients with uterine fibroids.

Abstract

INTRODUCTION:

Uterine fibroids (UFs) are the most prevalent benign neoplastic threat originating from myometria of reproductive age women, with a profound financial load valued in hundreds of billions of dollars. Unfortunately, there is no curative treatment so far except surgery and available pharmacological treatments are restricted for short-term treatment options. Thus, there is a large unmet need in the UF space for noninvasive therapeutics.

AREAS COVERED:

The authors reviewed the literature available for the utility of gonadotropin-releasing hormone (GnRH) analogs in women with UFs. We also focused on clinical studies exploring the therapeutic benefits of novel oral non-peptide GnRH antagonists that were recently approved by the U.S. Food and Drug Administration (FDA) in combination with estradiol/norethindrone acetate for the management of heavy menstrual bleeding associated with UFs in premenopausal women.

EXPERT OPINION:

The results regarding the efficacy of new-generation oral GnRH-antagonists, such as elagolix, relugolix and linzagolix, are promising and offer potential prospect for the future therapy of UFs. However, these antagonists must be combined with hormonal add-back therapy to minimize the resultant hypoestrogenic side effects such as bone loss.

• Authors: Mohamed Ali, Mohamed Raslan, Michał Ciebiera, Kornelia Zaręba, Ayman Al-Hendy
• Journal: Expert opinion on drug safety (Expert Opin Drug Saf) Vol. 21 Issue 4 Pg. 477-486 (Apr 2022) ISSN: 1744-764X [Electronic] England
• PMID: 34612122 (Publication Type: Journal Article, Review)

Chemical References

• Carboxylic Acids
• Pyrimidines
• Gonadotropin-Releasing Hormone
• linzagolix

Topics

• Carboxylic Acids (therapeutic use)
• Female
• Gonadotropin-Releasing Hormone (analogs & derivatives)
• Humans
• Leiomyoma (drug therapy)
• Pyrimidines
• Uterine Neoplasms (drug therapy)