China Manufacturer High Quality Wholesale Price Relugolix CAS 737789-87-6 for sale
China Manufacturer High Quality Wholesale Price Relugolix CAS 737789-87-6 for sale
China Manufacturer High Quality Wholesale Price Relugolix CAS 737789-87-6 for sale
China Manufacturer High Quality Wholesale Price Relugolix CAS 737789-87-6 for sale
China Manufacturer High Quality Wholesale Price Relugolix CAS 737789-87-6 for sale

China Manufacturer High Quality Wholesale Price Relugolix CAS 737789-87-6 Wholesale & Bulk

Relugolix is a prescription medication known as a GnRH receptor antagonist. It works by blocking the hormone signals that tell the body to produce testosterone or estrogen. It is primarily used in two ways: as Orgovyx to treat advanced prostate cancer in men by lowering testosterone, and as Myfembree (combined with other hormones) to manage uterine fibroids and endometriosis in women by reducing estrogen. It is an oral tablet taken once daily.

Items

Specifications

Results

Appearance

White to tinted   powder

Light   yellow

powder

Solubility

Freely soluble in DMSO, slightly   soluble in methanol and

acetonitrile, and shows pH   dependent solubility in aqueous media

Conforms

Identification

IR:   The IR absorption spectrum of the sample must be concordant

with   test standard.

Conforms

HPLC:   The HPLC spectrum of the sample must be concordant

with   the standard substance.

Conforms

Water

Not   more than 1.0%

0.16%

Residue   on Ignition

Not   more than 0.1%

Conforms

Heavy   Metals

Not   more than 20ppm

Conforms

Related   Substances

Any   other impurity: Not more than 0.3%

Total   impurities: Not more than 1.0%


0.11%

0.38%

Residual Solvents

Methanol: Not   more than 0.3%

Acetonitrile:   Not more than 0.041%

Dichloromethane:   Not more than 0.06%

Ethanol: Not   more than 0.5%

DMSO: Not more   than 0.5%

N.D.

N.D.

N.D.

0.16%

0.10%

Assay

(on anhydrous basis)

98.0%~102.0%

99.9%

Conclusion

The result conform with standard

Relugolix is a prescription medication classified as a GnRH (Gonadotropin-Releasing Hormone) receptor antagonist. In simpler terms, it is a hormone therapy that blocks the body's signal that tells the testes or ovaries to produce sex hormones (testosterone and estrogen).

It is known by the brand name Orgovyx when used for prostate cancer and Myfembree (in combination with estradiol and norethindrone acetate) for uterine fibroids and endometriosis.

How It Works: The Mechanism of Action

To understand Relugolix, it's helpful to know the natural hormone chain reaction it interrupts:

  1. Normal Process: Your brain's pituitary gland releases GnRH. This hormone signals the pituitary gland to release two other hormones: Luteinizing Hormone (LH) and Follicle-Stimulating Hormone (FSH).

  2. Result: LH and FSH then travel through the blood to tell the testes (in men) to produce testosterone, or the ovaries (in women) to produce estrogen.

  3. Relugolix's Action: Relugolix works by directly blocking the GnRH receptors on the pituitary gland. It acts like a "key" that fits into the lock but doesn't turn it, preventing the actual GnRH from binding.

  4. Final Effect: This quickly and dramatically reduces the production of LH and FSH. Consequently, the production of testosterone in men or estrogen in women plummets to very low levels. This is known as "chemical castration" or "medical menopause."

Primary Uses and Indications

Relugolix is used in two main contexts, with different formulations:

1. For Men: Advanced Prostate Cancer (Brand: Orgovyx™)

  • Purpose: It is used to treat advanced forms of prostate cancer that are hormone-sensitive. Prostate cancer cells often rely on testosterone to grow.

    Benefit: By rapidly reducing testosterone to very low levels ("androgen deprivation therapy" or ADT), Relugolix starves the cancer cells, slowing or stopping the disease's progression.

    Advantage over older therapies: Traditional GnRH agonists (like leuprolide) cause an initial surge in testosterone before suppressing it, which can lead to a "clinical flare" of symptoms. As an antagonist, Relugolix suppresses testosterone quickly without an initial surge, avoiding this problem.

2. For Women: Uterine Fibroids & Endometriosis (Brand: Myfembree®)

  • Important: For these conditions, Relugolix is combined with low-dose hormones (estradiol and norethindrone acetate).

    Purpose: While Relugolix alone suppresses estrogen (which can shrink fibroids and reduce endometriosis pain), causing very low estrogen levels long-term leads to menopausal side effects like bone loss.

    The "Add-Back" Therapy: The added estradiol and norethindrone acetate are "add-back" therapies. They provide just enough hormone to alleviate the severe symptoms of low estrogen (e.g., hot flashes, bone density loss) while maintaining the therapeutic benefit of a lower overall estrogen environment for treating the fibroids or endometriosis.

Key Considerations: Side Effects, Warnings, and Dosage

  • Common Side Effects:

    • In Men (Prostate Cancer): Hot flashes, increased blood sugar, increased triglycerides, muscle and joint pain, constipation, diarrhea, fatigue.

      In Women (Fibroids/Endometriosis): The add-back therapy mitigates many side effects, but can include headache, hot flashes, night sweats, and mood changes.

  • Important Warnings:

    • QT Prolongation: Relugolix can prolong the QT interval (an electrical measurement of the heart), which could increase the risk for irregular heart rhythms. Doctors may monitor heart health.

      Pregnancy Contraindication: It can cause fetal harm. Pregnancy must be excluded before starting and avoided during treatment.

      Bone Loss (Osteoporosis): Significant testosterone or estrogen suppression can lead to decreased bone mineral density. This risk is managed in women with the "add-back" therapy in Myfembree.

  • Administration:

    • It is an oral tablet, taken once daily. This is a major advantage over traditional GnRH therapies, which often require monthly or quarterly injections.

Summary

AspectDescription
What it isA prescription GnRH receptor antagonist (oral tablet).
Brand NamesOrgovyx (for men), Myfembree (for women, combo pill).
Primary FunctionRapidly suppresses the production of sex hormones (testosterone/estrogen).
Key UsesMen: Advanced prostate cancer. Women: Uterine fibroids & endometriosis (with add-back therapy).
Main AdvantageRapid action without the initial hormone surge caused by older agonist therapies. Oral administration.

Disclaimer: This information is for educational purposes only. Relugolix is a powerful prescription medication that must be used under the strict supervision of a qualified healthcare professional who can evaluate its risks and benefits for an individual's specific condition.


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