Basic Information
ID DDInter1577
Drug Type small molecule
Molecular Formula C29H27F2N7O5S
Molecular Weight 623.640
CAS Number 737789-87-6
Description Relugolix is a gonadotropin-releasing hormone (GnRH) receptor antagonist used in the treatment of several hormone-responsive conditions. It was first approved in Japan in 2019, under the brand name Relumina, for the symptomatic treatment of uterine fibroids,[A225816] and more recently by the United States' FDA in 2020, under the brand name Orgovyx, for the treatment of advanced prostate cancer.[L27991,L27996] This branded product was later approved by the European Commission on April 29, 2022.[L42150] Relugolix has also been studied in the symptomatic treatment of endometriosis.[A225761] Relugolix is the first (and currently only) orally-administered GnRH receptor antagonist approved for the treatment of prostate cancer - similar therapies such as [degarelix] require subcutaneous administration - and therefore provides a less burdensome therapeutic option for patients who might otherwise require clinic visits for administration by healthcare professionals.[L27996] In addition to its relative ease-of-use, relugolix was shown to be superior in the depression of testosterone levels when compared to [leuprolide], another androgen deprivation therapy used in the treatment of prostate cancer.[A225926] In May 2021, the FDA approved the combination product made up of relugolix, [estradiol], and [norethindrone] under the market name Myfembree for the first once-daily treatment for the management of heavy menstrual bleeding associated with uterine fibroids in premenopausal women.[L34289]
ATC Classification H01CC54 L02BX04
IUPAC Name 1-(4-{1-[(2,6-difluorophenyl)methyl]-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxo-1H,2H,3H,4H-thieno[2,3-d]pyrimidin-6-yl}phenyl)-3-methoxyurea
InChI AOMXMOCNKJTRQP-UHFFFAOYSA-N
Canonical SMILES CONC(=O)NC1=CC=C(C=C1)C1=C(CN(C)C)C2=C(S1)N(CC1=C(F)C=CC=C1F)C(=O)N(C2=O)C1=CC=C(OC)N=N1
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