Relugolix

Relugolix
Clinical data
Pronunciation	/ˌrɛlʊˈɡoʊlɪks/; RE-luu-GOH-liks
Trade names	Orgovyx, Relumina
Other names	RGX; RVT-601; TAK-385
AHFS/Drugs.com	Monograph
License data	US DailyMed: Relugolix;
Routes of; administration	By mouth
Drug class	GnRH antagonist
ATC code	L02BX04 (WHO) ; H01CC54 (WHO) (combination with estradiol and norethisterone);
Legal status
Legal status	CA: ℞-only; US: ℞-only; EU: Rx-only;
Pharmacokinetic data
Protein binding	68–71%
Elimination half-life	36 to 65 hours
Excretion	Feces: 82%; Urine: 4%
Identifiers
	IUPAC name 1-[4-[1-[(2,6-difluorophenyl)methyl]-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxothieno[2,3-d]pyrimidin-6-yl]phenyl]-3-methoxyurea;
CAS Number	737789-87-6;
PubChem CID	10348973;
IUPHAR/BPS	5586;
DrugBank	DB11853;
ChemSpider	8524431;
UNII	P76B05O5V6;
KEGG	D10888;
ChEMBL	ChEMBL1800159;
CompTox Dashboard (EPA)	DTXSID40224167 ;
Chemical and physical data
Formula	C29H27F2N7O5S
Molar mass	623.64 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)C)c(=O)n(-c2ccc(OC)nn2)c(=O)n3Cc2c(F)cccc2F)cc1;
	InChI InChI=1S/C29H27F2N7O5S/c1-36(2)14-19-24-26(39)38(22-12-13-23(42-3)34-33-22)29(41)37(15-18-20(30)6-5-7-21(18)31)27(24)44-25(19)16-8-10-17(11-9-16)32-28(40)35-43-4/h5-13H,14-15H2,1-4H3,(H2,32,35,40); Key:AOMXMOCNKJTRQP-UHFFFAOYSA-N;

Relugolix, sold under the brand names Orgovyx and Relumina among others, is a gonadotropin-releasing hormone antagonist (GnRH receptor antagonist) medication which is used in the treatment of prostate cancer in men and uterine fibroids in women. It is also under development for use in the treatment of endometriosis. It is taken by mouth once per day.

Side effects of relugolix include menstrual abnormalities, hot flashes, excessive sweating, headache, and decreased bone mineral density. Relugolix is a GnRH antagonist, or an antagonist of the gonadotropin-releasing hormone receptor. Unlike most other GnRH modulators, but similarly to elagolix (brand name Orilissa), relugolix is a non-peptide, small-molecule compound and is orally active. It suppresses sex hormone levels to the postmenopausal or castrate range in both women and men with administration once per day.

Relugolix was approved for use for the treatment of uterine fibroids in Japan in January 2019, and for the treatment of prostate cancer in the United States in December 2020.

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