Relugolix

Relugolix

Clinical data
Routes of administration	Oral
ATC code	none
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
Synonyms	TAK-385
CAS Number	737789-87-6
PubChem CID	10348973
ChemSpider	8524431
UNII	P76B05O5V6
Chemical and physical data
Formula	C29H27F2N7O5S
Molar mass	623.630386 g/mol
3D model (Jmol)	Interactive image
SMILES CN(C)CC1=C(SC2=C1C(=O)N(C(=O)N2CC3=C(C=CC=C3F)F)C4=NN=C(C=C4)OC)C5=CC=C(C=C5)NC(=O)NOC
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 (INN) (developmental code name TAK-385) is a non-peptide, orally-active, selective antagonist of the gonadotropin-releasing hormone receptor (GnRHR) (IC₅₀ = 0.12 nM) that is under development for clinical use by Takeda. It is currently in phase II clinical trials for the treatment of endometriosis, uterine leiomyoma, and prostate cancer.

A single oral administration of relugolix at a dose of 3 mg/kg has been found to suppress luteinizing hormone levels for more than 24 hours in castrated cynomolgus monkeys, indicating a long duration of action. The drug (80–160 mg/day) has been found to reduce testosterone levels to sustained castrate levels in men with once-daily chronic administration. Lower dosages (10–40 mg/day) are being studied in the treatment of endometriosis and uterine leiomyoma to achieve partial sex hormone suppression. The reasoning behind partial suppression for these conditions is to reduce the incidence and severity of menopausal symptoms such as hot flushes and to avoid bone mineral density changes caused by estrogen deficiency that can eventually lead to osteoporosis.