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Relugolix

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Relugolix

relugolix

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

Description:

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.

Applications

Relugolix is primarily used in hormone-dependent disease research and pharmaceutical development.

Key Applications

  • Prostate Cancer: Used as an androgen-deprivation therapy for adult patients with advanced prostate cancer.
  • GnRH Antagonist Research: Used for investigating pituitary-gonadal hormone regulation.
  • Androgen Deprivation Therapy: Studied for suppression of testosterone production.
  • Hormonal Disorder Research: Investigated in hormone-dependent reproductive and gynecological conditions.
  • Pharmaceutical Development: Used as an active pharmaceutical ingredient and reference compound in formulation and analytical research.
  • Endocrine Research: Useful for studying LH, FSH and sex-hormone regulation.

The FDA-approved ORGOVYX formulation contains relugolix and is indicated for adult patients with advanced prostate cancer.

Product Specifications

Relugolix is a pharmacologically active hormonal compound and should be handled according to the applicable SDS and pharmaceutical safety procedures.

Handling Precautions

  • Avoid inhalation of dust or powder.
  • Avoid contact with eyes and skin.
  • Wear suitable gloves, protective clothing and safety eyewear.
  • Handle in an adequately ventilated environment.
  • Avoid unnecessary generation of airborne particles.
  • Wash hands thoroughly after handling.
  • Keep the container tightly closed.
  • Do not eat, drink or smoke while handling the material.

Pharmaceutical Safety

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.

Mechanism of Actions

Relugolix works by competitively blocking GnRH receptors in the pituitary gland.

1. GnRH Receptor Antagonism

Relugolix binds competitively to pituitary GnRH receptors and prevents endogenous GnRH from activating these receptors.

2. Reduction of LH and FSH

Blocking GnRH signaling reduces the release of:

  • Luteinizing hormone (LH)
  • Follicle-stimulating hormone (FSH)

3. Suppression of Sex Hormones

The reduction in LH and FSH decreases gonadal production of sex hormones, particularly testosterone in males.

Simplified pathway:

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.

FAQs

1. What is Relugolix?

Relugolix is an orally active, nonpeptide GnRH receptor antagonist used to suppress pituitary gonadotropin secretion and downstream sex-hormone production.

2. What is the CAS number of Relugolix?

The CAS number is 737789-87-6.

3. What is the molecular formula of Relugolix?

The molecular formula is C₂₉H₂₇F₂N₇O₅S.

4. What is the molecular weight of Relugolix?

The molecular weight is 623.63 g/mol.

5. What is Relugolix used for?

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.

6. How does Relugolix work?

It competitively blocks pituitary GnRH receptors, reducing LH and FSH secretion and consequently reducing testosterone production.

7. What is the development code for Relugolix?

The development code for Relugolix is TAK-385.

8. What is the physical form of Relugolix?

Relugolix is described as a white to off-white to slightly yellow solid

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