Linzagolix cholineProduct ingredient for Linzagolix
- Name
- Linzagolix choline
- Drug Entry
- Linzagolix
Linzagolix is a non-peptide, selective antagonist of the gonadotropin-releasing hormone (GnRH) receptor. It has been studied for the treatment of estrogen-dependent conditions such as uterine fibroids and endometriosis.1,2 It is similar to other GnRH receptor antagonists like cetrorelix, relugolix, and elagolix.
Uterine fibroids occur in >70% of women of reproductive age, and when symptomatic are associated with heavy menstrual bleeding, anemia, abdominal pain and pressure, bloating, increased urinary frequency, and reproductive dysfunction.5 As these fibroids are essentially estrogen-dependent phenomena, hormone therapies which suppress estrogen activity - including GnRH receptor antagonists like linzagolix - are thought to be beneficial by preventing intramyometrial growths in the endometrial glands.6
Linzagolix was approved for use in the European Union in June 2022 for the management of symptoms caused by uterine fibroids.7
- Accession Number
- DBSALT003262
- Structure
Structure for Linzagolix choline (DBSALT003262)
- Synonyms
- Not Available
- External IDs
- KLH-2109 choline / OBE2109 choline
- UNII
- VHS6SC660Q
- CAS Number
- 1321816-57-2
- Weight
- Average: 611.59
Monoisotopic: 611.154920537 - Chemical Formula
- C27H28F3N3O8S
- InChI Key
- IAIVRTFCYOGNBW-UHFFFAOYSA-M
- InChI
- InChI=1S/C22H15F3N2O7S.C5H14NO/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;1-6(2,3)4-5-7/h3-6,8H,7H2,1-2H3,(H,26,31)(H,29,30);7H,4-5H2,1-3H3/q;+1/p-1
- IUPAC Name
- (2-hydroxyethyl)trimethylazanium 3-{5-[(2,3-difluoro-6-methoxyphenyl)methoxy]-2-fluoro-4-methoxyphenyl}-2,4-dioxo-1H,2H,3H,4H-thieno[3,4-d]pyrimidine-5-carboxylate
- SMILES
- C[N+](C)(C)CCO.COC1=C(OCC2=C(OC)C=CC(F)=C2F)C=C(N2C(=O)NC3=CSC(C([O-])=O)=C3C2=O)C(F)=C1
- External Links
- ChemSpider
- 68007282
- ChEMBL
- CHEMBL4298171
- Wikipedia
- Linzagolix
- Predicted Properties
Property Value Source Water Solubility 0.00125 mg/mL ALOGPS logP 0.55 ALOGPS logP 3.88 Chemaxon logS -5.7 ALOGPS pKa (Strongest Acidic) 3.15 Chemaxon pKa (Strongest Basic) -3.5 Chemaxon Physiological Charge -1 Chemaxon Hydrogen Acceptor Count 7 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 117.23 Å2 Chemaxon Rotatable Bond Count 8 Chemaxon Refractivity 128.08 m3·mol-1 Chemaxon Polarizability 44.93 Å3 Chemaxon Number of Rings 4 Chemaxon Bioavailability 1 Chemaxon Rule of Five No Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule Yes Chemaxon