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Relugolix

Generic Name
Relugolix
Brand Names
Myfembree, Orgovyx
Drug Type
Small Molecule
Chemical Formula
C29H27F2N7O5S
CAS Number
737789-87-6
Unique Ingredient Identifier
P76B05O5V6
Background

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, and more recently by the United States' FDA in 2020, under the brand name Orgovyx, for the treatment of advanced prostate cancer. This branded product was later approved by the European Commission on April 29, 2022. Relugolix has also been studied in the symptomatic treatment of endometriosis.

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. 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. 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.

Indication

适用于治疗成年晚期前列腺癌症患者。

Associated Conditions
Advanced Hormone Sensitive Prostate Cancer, Advanced Prostate Cancer, Heavy Menstrual Bleeding, Severe Pain
Associated Therapies
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urologytimes.com
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