linzagolix
{{Short description|Chemical compound}}
{{Use dmy dates|date=August 2022}}
{{Infobox drug
| image = Linzagolix.svg
| width = 250
| alt =
| image2 = Linzagolix molecule ball.png
| width2 = 250
| alt2 =
| caption =
| pronounce = {{IPAc-en|ˌ|l|ɪ|n|z|ə|ˈ|g|oʊ|l|ɪ|k|s}}
{{respell|LINZ|ə|GOH|liks}}
| tradename = Yselty
| Drugs.com =
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| pregnancy_AU =
| pregnancy_AU_comment =
| pregnancy_category=
| routes_of_administration = By mouth
| class = GnRH modulator; GnRH antagonist; Antigonadotropin
| ATC_prefix = H01
| ATC_suffix = CC04
| ATC_supplemental =
| legal_AU = S4
| legal_AU_comment = https://www.tga.gov.au/resources/prescription-medicines-registrations/yselty-theramex-australia-pty-ltd
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| legal_UK = POM
| legal_US =
| legal_US_comment =
| legal_EU = Rx-only
| legal_EU_comment = {{Cite web |date=14 December 2021 |title=Yselty EPAR |url=https://www.ema.europa.eu/en/medicines/human/EPAR/yselty |access-date=19 August 2022 |website=European Medicines Agency (EMA)}} Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
| legal_UN =
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| bioavailability =
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| index2_label = as choline
| CAS_number = 935283-04-8
| CAS_number2 = 1321816-57-2
| CAS_supplemental =
| PubChem = 16656889
| IUPHAR_ligand =
| DrugBank =
| ChemSpiderID = 17590169
| UNII = 7CDW97HUEX
| KEGG = D11608
| KEGG2 = D11609
| ChEBI =
| ChEMBL = 3668014
| ChEMBL2 = 4298171
| NIAID_ChemDB =
| PDB_ligand =
| synonyms = KLH-2109; OBE-2109
| IUPAC_name = 3-{5-[(2,3-difluoro-6-methoxyphenyl)methoxy]-2-fluoro-4-methoxyphenyl}-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid
| C=22 | H=15 | F=3 | N=2 | O=7 | S=1
| SMILES = COc1cc(F)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)cc1OCc1c(OC)ccc(F)c1F
| StdInChI_Ref =
| StdInChI = 1S/C22H15F3N2O7S/c1-32-14-4-3-10(23)18(25)9(14)7-34-16-6-13(11(24)5-15(16)33-2)27-20(28)17-12(26-22(27)31)8-35-19(17)21(29)30/h3-6,8H,7H2,1-2H3,(H,26,31)(H,29,30)
| StdInChI_comment =
| StdInChIKey_Ref =
| StdInChIKey = BMAAMIIYNNPHAB-UHFFFAOYSA-N
}}
Linzagolix, sold under the brand name Yselty, is a medication used in the treatment of uterine fibroids and endometriosis.{{Cite web |title=Yselty film-coated tablets |url=https://www.ema.europa.eu/en/documents/product-information/yselty-epar-product-information_en.pdf |website=Theramex Ireland Limited |publisher=European Medicines Agency}}{{Cite web |last=England |first=N. H. S. |date=2025-05-01 |title=NHS England » New endometriosis pill on the NHS could benefit more than 1,000 women a year |url=https://www.england.nhs.uk/2025/05/new-endometriosis-pill-on-the-nhs-could-benefit-more-than-1000-women-a-year/ |access-date=2025-05-22 |website=www.england.nhs.uk |language=en-US}} Linzagolix is a small-molecule, non-peptide, orally active gonadotropin-releasing hormone antagonist (GnRH antagonist) developed by Kissei Pharmaceutical and ObsEva.{{Cite web |title=Linzagolix - Kissei Pharmaceutical/ObsEva |url=http://adisinsight.springer.com/drugs/800032710 |website=AdisInsight |publisher=Springer Nature Switzerland AG}}{{Cite journal |vauthors=Chodankar R, Allison J |year=2018 |title=New Horizons in Fibroid Management |journal=Current Obstetrics and Gynecology Reports |volume=7 |issue=2 |pages=106–115 |doi=10.1007/s13669-018-0242-6 |issn=2161-3303 |doi-access=free}}{{Cite journal |vauthors=Ezzati M, Carr BR |date=January 2015 |title=Elagolix, a novel, orally bioavailable GnRH antagonist under investigation for the treatment of endometriosis-related pain |journal=Women's Health |volume=11 |issue=1 |pages=19–28 |doi=10.2217/whe.14.68 |pmid=25581052 |doi-access=free |title-link=doi}}
In June 2022, it was approved for medical use in the European Union and in the United Kingdom.{{Cite web |title=Yselty Product information |url=https://ec.europa.eu/health/documents/community-register/html/h1606.htm |access-date=24 June 2022 |publisher=European Commission |id=EU/1/21/1606}}
Medical uses
Linzagolix is indicated for treatment of moderate to severe symptoms of uterine fibroids in adult women of reproductive age and for treatment of intractable endometriosis.
=Available forms=
Linzagolix is available as linzagolix choline, the choline salt of linzagolix, in the form of 100 and 200{{nbsp}}mg film-coated oral tablets.
Pharmacology
=Pharmacodynamics=
Linzagolix acts as a selective antagonist of the GnRH receptor, the biological target of GnRH. 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.{{Cite journal |vauthors=Kotlyar AM, Pal L, Taylor HS |date=December 2021 |title=Eliminating Hormones With Orally Active Gonadotropin-releasing Hormone Antagonists |journal=Clinical Obstetrics and Gynecology |volume=64 |issue=4 |pages=837–849 |doi=10.1097/GRF.0000000000000664 |pmid=34668887 |s2cid=239034628}}
In clinical studies, linzagolix fully suppressed estradiol levels (median <20{{nbsp}}pg/mL) in women at a dosage of 200{{nbsp}}mg/day, whereas partial suppression of estradiol levels (median 20–60{{nbsp}}pg/mL) occurred at a dosage 100{{nbsp}}mg/day. Progesterone levels were also variably suppressed with these dosages.
=Pharmacokinetics=
The elimination half-life of linzagolix with repeated administration is approximately 15{{nbsp}}hours.
Society and culture
= Legal status =
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. The applicant for this medicinal product is ObsEva Ireland Ltd.{{Cite web |date=16 December 2021 |title=Yselty: Pending EC decision |url=https://www.ema.europa.eu/en/medicines/human/summaries-opinion/yselty |access-date=18 December 2021 |website=European Medicines Agency |archive-date=18 December 2021 |archive-url=https://web.archive.org/web/20211218215204/https://www.ema.europa.eu/en/medicines/human/summaries-opinion/yselty |url-status=dead }} Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged. Linzagolix was approved for medical use in the European Union in June 2022.
=Brand names=
=Availability=
Linzagolix is available in the European Union and in the United Kingdom.{{Cite press release |title=ObsEva Announces UK MHRA Marketing Authorization for Yselty (linzagolix), an Oral GnRH Antagonist, for the Treatment of Uterine Fibroids |date=28 June 2022 |publisher=ObsEva |url=https://www.globenewswire.com/news-release/2022/06/28/2470795/0/en/ObsEva-Announces-UK-MHRA-Marketing-Authorization-for-Yselty-linzagolix-an-Oral-GnRH-Antagonist-for-the-Treatment-of-Uterine-Fibroids.html |via=GlobeNewswire |access-date=24 August 2022}}
References
{{Reflist}}
Further reading
{{refbegin}}
- {{Cite journal |display-authors=6 |vauthors=Dababou S, Garzon S, Laganà AS, Ferrero S, Evangelisti G, Noventa M, D'Alterio MN, Palomba S, Uccella S, Franchi M, Barra F |date=September 2021 |title=Linzagolix: a new GnRH-antagonist under investigation for the treatment of endometriosis and uterine myomas |journal=Expert Opinion on Investigational Drugs |volume=30 |issue=9 |pages=903–911 |doi=10.1080/13543784.2021.1957830 |pmid=34278887 |s2cid=236091261}}
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External links
- {{Cite web |title=Linzagolix |url=https://druginfo.nlm.nih.gov/drugportal/name/linzagolix |website=Drug Information Portal |publisher=U.S. National Library of Medicine}}
- {{Cite web |title=Linzagolix choline |url=https://druginfo.nlm.nih.gov/drugportal/name/linzagolix%20choline |website=Drug Information Portal |publisher=U.S. National Library of Medicine}}
{{GnRH and gonadotropins}}
{{GnRH and gonadotropin receptor modulators}}
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