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Linzagolix in moderate to severe symptoms of uterine fibroids: a profile of its use

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Abstract

Linzagolix (Yselty®) is an orally administered gonadotropin-releasing hormone receptor antagonist approved in the EU for the treatment of moderate to severe symptoms of uterine fibroids in adult women of reproductive age and extends the treatment options in this indication. Linzagolix is available as different treatment regimens: for short-term use to reduce uterine and fibroid volumes; and for longer-term use to manage fibroid-associated symptoms. In two placebo-controlled phase 3 trials, linzagolix as a single agent or in combination with hormonal add-back therapy significantly reduced the proportion of patients with heavy menstrual bleeding, improved other symptoms associated with uterine fibroids (including anaemia and pain) and improved patient quality of life. Linzagolix was generally well tolerated, with hot flushes and headaches being the most common adverse events.

Plain Language Summary

Uterine fibroids occur in > 70% of women before menopause, and cause symptoms that require treatment in 25% of women of reproductive age. Uterine fibroids can cause heavy menstrual bleeding and lead to reduced fertility and complications during pregnancy. Linzagolix (Yselty®), a gonadotropin-releasing hormone receptor antagonist, is a new treatment option which suppresses the production of the ovarian steroids that drive fibroid growth. In two placebo-controlled phase 3 trials, linzagolix significantly reduced the proportion of patients who experienced heavy menstrual bleeding, improved other symptoms associated with uterine fibroids (anaemia, pain and fibroid growth) and improved patient quality of life. Linzagolix was generally well tolerated. Based on these results, linzagolix (with or without hormonal add-back therapy) has been approved in the EU for the treatment of moderate to severe symptoms of uterine fibroids in adult women of reproductive age and is available in different dosing regimens for reducing uterine and fibroid volume or to treat the symptoms associated with uterine fibroids. Thus, linzagolix extends the treatment options in this indication.

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Acknowledgements

The manuscript was reviewed by: M. A. Lumsden, School of Medicine, University of Glasgow, Glasgow, UK; S. Palacios, Palacios Institute of Women's Health, Madrid, Spain; N. Phillips, Obstetrics, Gynecology & Reproductive Sciences, Rutgers Robert Wood Johnson Medical School, New Brunswick, New Jersey, USA. During the peer review process, Kissei Pharmaceutical, the originator of linzagolix, was also offered an opportunity to provide a scientific accuracy review of their data. Changes resulting from comments received were made on the basis of scientific and editorial merit.

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    Simon Fung & Hannah A. Blair

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  1. Simon Fung
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Correspondence to Simon Fung.

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S. Fung and H. A. Blair are salaried employees of Adis International Ltd/Springer Nature and declare no relevant conflicts of interest. All authors contributed to this article and are responsible for its content.

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Fung, S., Blair, H.A. Linzagolix in moderate to severe symptoms of uterine fibroids: a profile of its use. Drugs Ther Perspect 39, 309–316 (2023). https://doi.org/10.1007/s40267-023-01019-8

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