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
MedlinePlus	a621006
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	AU: S4 (Prescription only); 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, uterine fibroids and endometriosis. It is taken by mouth.

Clinical data


Pronunciation	/ˌrɛlʊˈɡoʊlɪks/ RE-luu-GOH-liks
Trade names	Orgovyx, Relumina
Other names	RGX; RVT-601; TAK-385
AHFS/Drugs.com	Monograph
MedlinePlus	a621006
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	AU: S4 (Prescription only) 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