Comparing the pharmacokinetic and pharmacodynamic qualities of current and future therapies for uterine fibroids. (3rd August 2022)

• Record Type: Journal Article
• Authors: Evangelisti, Giulio; Barra, Fabio; Perrone, Umberto; Di Donato, Nadine; Bogliolo, Stefano; Ceccaroni, Marcello; Ferrero, Simone
• Is Part Of: Expert opinion on drug metabolism and toxicology. Volume 18:Number 7/8(2022)
• Page Start: 441
• Page End: 457
• Publication Date: 2022-08-03
• Subjects: Drug pharmacology -- elagolix -- levonorgestrel releasing intrauterine device -- linzagolix -- relugolix -- ulipristal acetate -- uterine fibroid -- vilaprisan -- GnRH-agonists -- leuprolide -- aromatase inhibitors; Drugs -- Toxicology -- Periodicals; Drugs -- Metabolism -- Periodicals; 615.7
• DOI: 10.1080/17425255.2022.2113381
• Languages: English
• ISSNs: 1742-5255

Abstract

ABSTRACT: Introduction: Uterine fibroids are the most common benign gynecological tumors affecting women of reproductive ages. Although surgery is the definitive treatment choice, several medical approaches have been investigated to control their symptoms. The main issue of currently employed drugs for uterine fibroids is the long-term safety and tolerability profile. Today, new emerging options represent hopeful alternatives that could potentially overcome these limitations. Areas covered: This manuscript aims to give an updated overview of the pharmacodynamic and pharmacokinetic properties of current and new investigational medical drugs for the treatment of symptomatic uterine fibroids. The bibliographic research was conducted by searching alone or combined keywords on the following electronic databases: Medline, PubMed, Embase, Science Citation Index via Web of Science. Expert opinion: The most recent therapeutic strategies for uterine fibroids are represented by gonadotropin-releasing hormone antagonists (GnRH-ants; elagolix and relugolix) and selective progesterone receptor modulators (SPRM; ulipristal acetate). After early promising results, studies on innovative drugs, such as linzagolix (GnRH-ant) and vilaprisan (SPRM) are demanding. In the near future, a deeper knowledge of biological mechanisms at the basis of the genesis and growth of uterine fibroids could pave the way for the development of innovative targeted therapies.