Merigolix

Merigolix (INNTooltip International Nonproprietary Name; developmental code names HS-10518, NCE-403, SKI-2670, TU-2670) is a gonadotropin releasing hormone (GnRH) antagonist which is under development for the treatment of endometriosis and uterine fibroids. It is taken by mouth. The drug is being developed by TiumBio, Daewon Pharmaceutical, and Jiangsu Hansoh Pharmaceutical. As of October 2024, it is in phase 2 clinical trials for both endometriosis and uterine fibroids.

Pharmaceutical compound

Merigolix

Clinical data
Other names	HS-10518; NCE-403; SKI-2670; TU-2670
Routes of administration	Oral[1]
Drug class	GnRH antagonist
Identifiers
IUPAC name 4-[[(1R)-2-[1-[[2-fluoro-6-(trifluoromethyl)phenyl]methyl]-2,4-dioxo-1'-[[5-(trifluoromethyl)furan-2-yl]methyl]spiro[7H-furo[3,4-d]pyrimidine-5,4'-piperidine]-3-yl]-1-phenylethyl]amino]butanoic acid
CAS Number	1454272-94-6
PubChem CID	71727383
ChemSpider	128922028
UNII	RS62JYV9LX
ChEMBL	ChEMBL5314469
Chemical and physical data
Formula	C36H35F7N4O6
Molar mass	752.687 g·mol−1
3D model (JSmol)	Interactive image
SMILES C1CN(CCC12C3=C(CO2)N(C(=O)N(C3=O)C[C@@H](C4=CC=CC=C4)NCCCC(=O)O)CC5=C(C=CC=C5F)C(F)(F)F)CC6=CC=C(O6)C(F)(F)F
InChI InChI=1S/C36H35F7N4O6/c37-26-9-4-8-25(35(38,39)40)24(26)19-46-28-21-52-34(13-16-45(17-14-34)18-23-11-12-29(53-23)36(41,42)43)31(28)32(50)47(33(46)51)20-27(22-6-2-1-3-7-22)44-15-5-10-30(48)49/h1-4,6-9,11-12,27,44H,5,10,13-21H2,(H,48,49)/t27-/m0/s1 Key:LJPSGSMPGVITHK-MHZLTWQESA-N

Merigolix (INNTooltip International Nonproprietary Name; developmental code names HS-10518, NCE-403, SKI-2670, TU-2670) is a gonadotropin releasing hormone (GnRH) antagonist which is under development for the treatment of endometriosis and uterine fibroids.^{[1][2][3][4][5]} It is taken by mouth.^[1] The drug is being developed by TiumBio, Daewon Pharmaceutical, and Jiangsu Hansoh Pharmaceutical.^[1][2] As of October 2024, it is in phase 2 clinical trials for both endometriosis and uterine fibroids.^[1][2]

See also

[edit]

• List of investigational sex-hormonal agents

References

[edit]

1. ^ ^{a b c d e} "Merigolix". AdisInsight. 28 October 2024. Retrieved 24 February 2025.
2. ^ ^{a b c} "Delving into the Latest Updates on Merigolix with Synapse". Synapse. 22 February 2025. Retrieved 24 February 2025.
3. ^ Tukun FL, Olberg DE, Riss PJ, Haraldsen I, Kaass A, Klaveness J (December 2017). "Recent Development of Non-Peptide GnRH Antagonists". Molecules. 22 (12): 2188. doi:10.3390/molecules22122188. PMC 6149776. PMID 29232843.
4. ^ Farris M, Bastianelli C, Rosato E, Brosens I, Benagiano G (2019). "Uterine fibroids: an update on current and emerging medical treatment options". Therapeutics and Clinical Risk Management. 15: 157–178. doi:10.2147/TCRM.S147318. PMC 6350833. PMID 30774352.
5. ^ Angioni S, D'Alterio MN, Daniilidis A (2021). "Highlights on Medical Treatment of Uterine Fibroids". Current Pharmaceutical Design. 27 (36): 3821–3832. doi:10.2174/1381612826666210101152820. PMID 33388011.

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