CAS No.: 737789-87-6
Category: Gonadotropin-Releasing Hormone (GnRH) Receptor Antagonist
Molecular Formula: C₂₉H₂₇F₂N₇O₅S
Molecular Weight: 623.63 g/mol
Synonyms: TAK-385, Relugolix
Relugolix is a nonpeptide, orally active gonadotropin-releasing hormone (GnRH) receptor antagonist. It acts directly on GnRH receptors in the pituitary gland, reducing the secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), which subsequently decreases sex hormone production.
Relugolix is an important compound in the development of hormone-dependent therapies and is clinically used in androgen-deprivation therapy for advanced prostate cancer. It is also used as a component of combination therapy for certain hormone-related conditions.
Relugolix is primarily used in hormone-dependent disease research and pharmaceutical development.
The FDA-approved ORGOVYX formulation contains relugolix and is indicated for adult patients with advanced prostate cancer.
Relugolix is a pharmacologically active hormonal compound and should be handled according to the applicable SDS and pharmaceutical safety procedures.
Clinical use of relugolix requires appropriate medical supervision. Hormonal suppression can produce clinically significant effects, and the approved product carries warnings including potential QT/QTc interval prolongation and hypersensitivity reactions.
Relugolix works by competitively blocking GnRH receptors in the pituitary gland.
Relugolix binds competitively to pituitary GnRH receptors and prevents endogenous GnRH from activating these receptors.
Blocking GnRH signaling reduces the release of:
The reduction in LH and FSH decreases gonadal production of sex hormones, particularly testosterone in males.
Relugolix → GnRH receptor blockade → ↓ LH/FSH → ↓ gonadal hormone production → androgen/sex-hormone suppression
Unlike GnRH agonists, GnRH antagonists such as relugolix can suppress the GnRH receptor pathway without requiring an initial stimulatory phase.
Relugolix is an orally active, nonpeptide GnRH receptor antagonist used to suppress pituitary gonadotropin secretion and downstream sex-hormone production.
The CAS number is 737789-87-6.
The molecular formula is C₂₉H₂₇F₂N₇O₅S.
The molecular weight is 623.63 g/mol.
Relugolix is used clinically as a GnRH receptor antagonist for androgen-deprivation therapy in advanced prostate cancer and is also relevant to hormone-related pharmaceutical research.
It competitively blocks pituitary GnRH receptors, reducing LH and FSH secretion and consequently reducing testosterone production.
The development code for Relugolix is TAK-385.
Relugolix is described as a white to off-white to slightly yellow solid
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