| Drug Name |
Relugolix |
| Drug ID |
BADD_D02587 |
| 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] 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] |
| Indications and Usage |
Relugolix is indicated for the treatment of adult patients with advanced prostate cancer.[L27991] In a combination product with [estradiol] and [norethindrone], relugolix is indicated for the once-daily treatment for the management of heavy menstrual bleeding associated with uterine fibroids in premenopausal women.[L34289] |
| Marketing Status |
approved; investigational |
| ATC Code |
L02BX04 |
| DrugBank ID |
DB11853
|
| KEGG ID |
D10888
|
| MeSH ID |
C561634
|
| PubChem ID |
10348973
|
| TTD Drug ID |
D0F2WP
|
| NDC Product Code |
46014-1130; 72974-120; 83137-0009; 51148-013 |
| UNII |
P76B05O5V6
|
| Synonyms |
relugolix | orgovyx | TAK 385 | TAK385 | TAK-385 | 1-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxypyridazin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno(2,3-d)pyrimidin-6-yl)phenyl)-3-methoxyurea |
