Relugolix NEW

Relugolix Cas 737789-87-6

Specification

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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

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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Spring Zhang

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Tel:   +86-27-59207892

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