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Pronunciation |
/ˌlɪnzəˈɡoʊlɪks/ LINZ-ə-GOH-liks |
Trade names | Yselty |
Other names | KLH-2109; OBE-2109 |
Routes of administration | By mouth [1] [2] |
Drug class | GnRH modulator; GnRH antagonist; Antigonadotropin |
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Chemical and physical data | |
Formula | C22H15F3N2O7S |
Molar mass | 508.42 g·mol−1 |
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Linzagolix, sold under the brand name Yselty, is a medication used in the treatment of uterine fibroids. [1] [5] Linzagolix is a small-molecule, non-peptide, orally active gonadotropin-releasing hormone antagonist (GnRH antagonist) developed by Kissei Pharmaceutical and ObsEva. [6] [7] [2]
In June 2022, it was approved for medical use in the European Union and in the United Kingdom. [1] [4] [8]
Linzagolix is indicated for treatment of moderate to severe symptoms of uterine fibroids in adult women of reproductive age. [1]
Linzagolix is available as linzagolix choline, the choline salt of linzagolix, in the form of 100 and 200 mg film-coated oral tablets. [5]
Linzagolix acts as a selective antagonist of the GnRH receptor, the biological target of GnRH. [5] By blocking this receptor, linzagolix prevents GnRH-mediated secretion of the gonadotropins, luteinizing hormone (LH) and follicle-stimulating hormone (FSH), and prevents them from signaling the gonads to produce sex hormones including estrogens, progesterone, and androgens. [5] [9]
In clinical studies, linzagolix fully suppressed estradiol levels (median <20 pg/mL) in women at a dosage of 200 mg/day, whereas partial suppression of estradiol levels (median 20–60 pg/mL) occurred at a dosage 100 mg/day. [5] Progesterone levels were also variably suppressed with these dosages. [5]
The elimination half-life of linzagolix with repeated administration is approximately 15 hours. [5]
On 16 December 2021, and on 22 April 2022, the Committee for Medicinal Products for Human Use (CHMP) of the European Medicines Agency (EMA) adopted a positive opinion, recommending the granting of a marketing authorization for the medicinal product Yselty, intended for the treatment of symptoms of uterine fibroids. [10] The applicant for this medicinal product is ObsEva Ireland Ltd. [10] Linzagolix was approved for medical use in the European Union in June 2022. [1] [4]
Linzagolix is sold under the brand name Yselty. [5]
Linzagolix is available in the European Union and in the United Kingdom. [5] [8]