The oral GnRH antagonists, a new class of drugs in gynecology: from pharmacokinetics to possible clinical applications.

Autor:	Barretta M; Department of Clinical Sciences and Community Health, University of Milan, Milan, Italy., Vignali M; Department of Clinical Sciences and Community Health, University of Milan, Milan, Italy., La Marca A; Department of Medical and Surgical Sciences for Mother, Child and Adult, University of Modena and Reggio Emilia, Azienda Ospedaliero-Universitaria di Modena, Modena, Italy., Grandi G; Department of Medical and Surgical Sciences for Mother, Child and Adult, University of Modena and Reggio Emilia, Azienda Ospedaliero-Universitaria di Modena, Modena, Italy.
Jazyk:	angličtina
Zdroj:	Expert opinion on drug metabolism & toxicology [Expert Opin Drug Metab Toxicol] 2024 Dec 12. Date of Electronic Publication: 2024 Dec 12.
DOI:	10.1080/17425255.2024.2441981
Abstrakt:	Introduction: In ovarian steroid-dependent diseases such as uterine fibroids, endometriosis and adenomyosis, oral GnRH antagonists have emerged as new therapeutic alternatives. These oral GnRH antagonists offer key advantages, including oral administration, dose-dependent estrogen suppression and rapid reversibility. Areas Covered: This review examines the pharmacological, clinical and therapeutic profiles of the latest non-peptide oral GnRH antagonists, through an analysis of clinical evidence and randomized clinical trials, to provide a comprehensive and up-to-date overview of their clinical applications and potential benefits. Expert Opinion: The clinical trials examined demonstrated significant efficacy in reducing heavy menstrual bleeding in women with fibroids and pelvic pain in women with endometriosis, with more than 70% of patients achieving primary endpoints. The use of add-back therapy minimized bone mass density loss, ensuring long-term safety. Adverse events were dose-dependent but generally well tolerated. In our opinion, the strength of oral GnRH antagonists lies in their pharmacological properties. Oral administration increases convenience, allows adjustable dosing and ensures a dose-dependent effect. These drugs provide an immediate antagonistic effect without the flare-up phenomenon. Furthermore, they are expected to act on ectopic endometrial and smooth muscle cell receptors, potentially providing additional anti-proliferative effects. However, further research is needed: long term clinical trials must compare them with existing treatments.
Databáze:	MEDLINE
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