Effects of combined GnRH receptor antagonist linzagolix and hormonal add-back therapy on vaginal bleeding—delayed add-back onset does not improve bleeding pattern
Combined linzagolix and hormonal add-back therapy achieved better bleeding control and fewer hot flushes than delayed add-back in healthy premenopausal women.
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This single-center, open-label, parallel-group study in 32 premenopausal women evaluated high-dose linzagolix (200 mg) with hormonal add-back therapy (ABT) versus a delayed ABT onset, using 10 weeks of combined linzagolix/ABT or 4 weeks of linzagolix alone followed by ABT for 6 additional weeks. Linzagolix alone rapidly reduced bleeding, achieving amenorrhea in all women by week 5, with trough estradiol (E2) levels reaching median week 4 values of 4.1 pg/mL. When ABT was started at week 5, spotting and bleeding occurred, and bleeding was more frequent in the “Combined-ABT” group than in the “Delayed-ABT” group, with E2 medians of 24–32 pg/mL early in the combined group versus 35–42 pg/mL during weeks 5–10 in the delayed group; the paper reports that linzagolix was well tolerated, with headache and hot flushes as the most frequent adverse events. The main limitation is the small sample size and open-label design using healthy women rather than patients with sex-hormone-dependent disease. This paper is centrally about endometriosis — it evaluates linzagolix, a GnRH receptor antagonist developed for endometriosis, and characterizes how different add-back timing affects bleeding and estradiol relevant to endometriosis treatment regimens.
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Cited by (8)
- Linzagolix therapy versus a placebo in patients with endometriosis-associated pain: a prospective, randomized, double-blind, Phase 3 study (EDELWEISS 3) 2024
- An Efficient UPLC-MS/MS Method Established to Detect Relugolix Concentration in Rat Plasma 2022
- Gynecological uses of GnRH antagonists: review article 2022
- Comparing the pharmacokinetic and pharmacodynamic qualities of current and future therapies for uterine fibroids 2022
- A model‐based analysis to guide gonadotropin‐releasing hormone receptor antagonist use for management of endometriosis 2021
- Endometriosis and Medical Therapy: From Progestogens to Progesterone Resistance to GnRH Antagonists: A Review 2021
- Thromboembolic safety profile of low-dose estradiol (valerate) in combined hormonal preparations: Implications for the development of new hormonal endometriosis and uterine fibroid therapies 2021
- Neue Behandlungsoptionen mit GnRH-Antagonisten bei Endometriose und Uterus myomatosus 2020
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