The evaluation of pharmacotherapy in endometriosis: changes, challenges and difficulties

Monika Kopec, Kopec M, Monika Ruszała, Monika Kopeć, Wankowicz A, Agnieszka Wańkowicz, Agnieszka Wankowicz, Ivan Golubka, Golubka I, Kotarski J, Jan Kotarski, Marek Gogacz, Gogacz M
Ginekologia polska · 2026 · vol. 97(9) , pp. 751–760 · doi:10.5603/gpl.111016 · PMID:42383477 · W7166804256
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This review discusses pharmacotherapy for endometriosis, highlighting GnRH antagonists/agonists and new combination therapies like relugolix and linzagolix for pain relief and adherence, while noting potential side effects and the need for bone health monitoring.

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This review evaluates recent advancements in pharmacotherapy for endometriosis, focusing on the shift from traditional GnRH agonists to oral GnRH antagonists like relugolix and linzagolix. The authors highlight that combining active substances into single tablets improves patient adherence while maintaining efficacy in alleviating pain symptoms. Key findings indicate that two years of monotherapy with linzagolix did not significantly impact bone health compared to placebo, whereas relugolix combination therapy effectively managed pain and preserved bone mineral density over a similar period. Despite potential side effects, these treatments are described as promising and well-tolerated, though individualized dosing and long-term bone health monitoring remain necessary considerations. This paper is centrally about endometriosis — specifically evaluating oral GnRH antagonist therapies for pain management and their impact on bone health.

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Abstract

OBJECTIVES: Endometriosis presents a multitude of challenges for individuals. Current treatment of the disease is based on pharmacotherapy that aims to relieve pain, improves future fertility, potentially slows disease progression and lessen the likelihood of recurrence. The present review outlines recent reports on the importance of Gonadotropin-Releasing Hormone antagonists/antagonists and a new prospective as a significant second-line treatment option. MATERIAL AND METHODS: A review of the literature from the last 5 years was conducted. The search included the following medical subject: "endometriosis", "GnRh agonists", "GnRh antagonists", "pharmacotherapy". The articles published in English were included. Publications without full text access and duplicates were rejected. RESULTS: Current research no longer focuse exclusively on finding new GnRH agonists/antagonists, but rather on maximizing their usage, in favour of the latter ones. Multiple active substances are now being combined into one tablet, which makes it easier for patients to take their medication and improves their adherence to treatment recommendations. 24 months monotherapy of linzagolix did not indicate any clinically relevant impact on overall bone condition in comparison to placebo group. Relugolix combination therapy-maintained bone mass density over two years while effectively alleviating pain symptoms. CONCLUSIONS: Despite being effective, all treatments may have additional negative effects. The best approach to pharmacotherapy depends on the individual patient's needs and circumstances. Taking into consideretion potential effects, an appropriate dose or a combination of the above options should be performed. The treatment options of Relugolix and Linzagolix are both promising and well-tolerated. Further research should focuse on long-term bone health monitoring strategies and its safety profile.
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Abstract

Objectives: Endometriosis presents a multitude of challenges for individuals. Current treatment of the disease is based on pharmacotherapy that aims to relieve pain, improves future fertility, potentially slows disease progression and lessen the likelihood of recurrence. The present review outlines recent reports on the importance of Gonadotropin-Releasing Hormone antagonists/antagonists and a new prospective as a significant second-line treatment option.

Material and methods

A review of the literature from the last 5 years was conducted. The search included the following medical subject: “endometriosis”, “GnRh agonists”, “GnRh antagonists”, "pharmacotherapy”. The articles published in English were included. Publications without full text access and duplicates were rejected.

Results

Current research no longer focuse exclusively on finding new GnRH agonists/antagonists, but rather on maximizing their usage, in favour of the latter ones. Multiple active substances are now being combined into one tablet, which makes it easier for patients to take their medication and improves their adherence to treatment recommendations. 24 months monotherapy of linzagolix did not indicate any clinically relevant impact on overall bone condition in comparison to placebo group. Relugolix combination therapy-maintained bone mass density over two years while effectively alleviating pain symptoms.

Conclusions

Despite being effective, all treatments may have additional negative effects. The best approach to pharmacotherapy depends on the individual patient’s needs and circumstances. Taking into consideretion potential effects, an appropriate dose or a combination of the above options should be performed. The treatment options of Relugolix and Linzagolix are both promising and well-tolerated. Further research should focuse on long-term bone health monitoring strategies and its safety profile.

Keywords

endometriosispharmacotherapyGnRh agonistshormonal treatmentGnRh antagonists

References

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Endometriosis Endometriosis Endometriosis Endometriosis Endometriosis Endometriosis Endometriosis Endometriosis Endometriosis Endometriosis Endometriosis Endometriosis Endometriosis Endometriosis Endometriosis Endometriosis Endometriosis Endometriosis Endometriosis Endometriosis

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