Linzagolix

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Linzagolix
File:Linzagolix.svg
File:Linzagolix molecule ball.png
Clinical data
Pronunciation/ˌlɪnzəˈɡoʊlɪks/
LINZ-ə-GOH-liks
Trade namesYselty
Other namesKLH-2109; OBE-2109
Routes of
administration		By mouth[1][2]
Drug classGnRH modulator; GnRH antagonist; Antigonadotropin
ATC code
Legal status
Legal status
Identifiers
  • 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
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
E number{{#property:P628}}
CompTox Dashboard (EPA)
  • {{#property:P3117}}Lua error in Module:EditAtWikidata at line 29: attempt to index field 'wikibase' (a nil value).
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Chemical and physical data
FormulaC22H15F3N2O7S
Molar mass508.42 g·mol−1
3D model (JSmol)
  • COc1cc(F)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)cc1OCc1c(OC)ccc(F)c1F
  • InChI=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)
  • Key:BMAAMIIYNNPHAB-UHFFFAOYSA-N

Linzagolix, sold under the brand name Yselty, is a medication used in the treatment of uterine fibroids and endometriosis.[1][6][7] Linzagolix is a small-molecule, non-peptide, orally active gonadotropin-releasing hormone antagonist (GnRH antagonist) developed by Kissei Pharmaceutical and ObsEva.[8][9][2]

In June 2022, it was approved for medical use in the European Union and in the United Kingdom.[1][5][10]

Medical uses

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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.[1][7]

Available forms

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Linzagolix is available as linzagolix choline, the choline salt of linzagolix, in the form of 100 and 200 mg film-coated oral tablets.[6]

Pharmacology

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Pharmacodynamics

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Linzagolix acts as a selective antagonist of the GnRH receptor, the biological target of GnRH.[6] 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.[6][11]

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.[6] Progesterone levels were also variably suppressed with these dosages.[6]

Pharmacokinetics

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The elimination half-life of linzagolix with repeated administration is approximately 15 hours.[6]

Society and culture

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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.[12] The applicant for this medicinal product is ObsEva Ireland Ltd.[12] Linzagolix was approved for medical use in the European Union in June 2022.[1][5]

Brand names

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Linzagolix is sold under the brand name Yselty.[6]

Availability

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Linzagolix is available in the European Union and in the United Kingdom.[6][10]

References

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  1. ^ a b c d e f Lua error in Module:Citation/CS1/Configuration at line 2172: attempt to index field '?' (a nil value). Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  2. ^ a b Lua error in Module:Citation/CS1/Configuration at line 2172: attempt to index field '?' (a nil value).
  3. ^ Lua error in Module:Citation/CS1/Configuration at line 2172: attempt to index field '?' (a nil value).
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  6. ^ a b c d e f g h i Lua error in Module:Citation/CS1/Configuration at line 2172: attempt to index field '?' (a nil value).
  7. ^ a b Lua error in Module:Citation/CS1/Configuration at line 2172: attempt to index field '?' (a nil value).
  8. ^ Lua error in Module:Citation/CS1/Configuration at line 2172: attempt to index field '?' (a nil value).
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  10. ^ a b Lua error in Module:Citation/CS1/Configuration at line 2172: attempt to index field '?' (a nil value).
  11. ^ Lua error in Module:Citation/CS1/Configuration at line 2172: attempt to index field '?' (a nil value).
  12. ^ a b Lua error in Module:Citation/CS1/Configuration at line 2172: attempt to index field '?' (a nil value). Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.

Further reading

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  • Lua error in Module:Citation/CS1/Configuration at line 2172: attempt to index field '?' (a nil value).
[edit | edit source]
  • Lua error in Module:Citation/CS1/Configuration at line 2172: attempt to index field '?' (a nil value).
  • Lua error in Module:Citation/CS1/Configuration at line 2172: attempt to index field '?' (a nil value).

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