About

Relugolix is an oral, non-peptide gonadotropin-releasing hormone (GnRH) receptor antagonist. It works by competitively binding to and blocking GnRH receptors in the anterior pituitary gland. This action leads to a rapid, dose-dependent, and reversible suppression of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) release. Consequently, it reduces the production of ovarian and testicular steroid hormones, including estrogen and testosterone. This mechanism makes relugolix effective in treating hormone-sensitive conditions that benefit from reduced sex hormone levels.

It is primarily indicated for the treatment of advanced prostate cancer and for the management of uterine fibroids. For prostate cancer, it offers a novel oral alternative to injectable GnRH agonists, providing rapid testosterone suppression without the initial testosterone flare associated with agonists. In uterine fibroids, it helps to reduce heavy menstrual bleeding and pain by lowering estrogen levels. Its oral administration and rapid onset of action are significant advantages.

Uses

Treatment of advanced prostate cancer.
Management of uterine fibroids (in combination with estradiol and norethindrone acetate).
Reduces levels of testosterone in men.
Reduces levels of estrogen in women.

Directions For Use

Take orally once daily, with or without food, at approximately the same time each day.

Benefits

Rapid and sustained suppression of sex hormones.
Oral administration for convenience.
Avoids initial testosterone flare in prostate cancer.
Effective in reducing symptoms of uterine fibroids.
Reversible effects on hormone levels.
Offers an alternative to injectable therapies.

Side Effects

Hot flashes
Diarrhea
Arthralgia
Fatigue
Nausea
Headache
Increased blood glucose
Increased triglycerides
Decreased bone mineral density (long-term use)
Anemia
Weight gain
Hypertension

Safety Measures

Alcohol - No specific contraindication, but alcohol may exacerbate hot flashes or gastrointestinal side effects.
Pregnancy - Contraindicated in pregnancy due to potential for fetal harm; use effective non-hormonal contraception.
Breastfeeding - Not recommended during breastfeeding as it may pass into breast milk and harm the infant.
Liver - Use with caution in patients with severe hepatic impairment; monitor liver function closely.
Kidney - No dose adjustment is required for mild to moderate renal impairment; use with caution in severe impairment.
Lung - No specific contraindications or concerns related to lung conditions; generally well-tolerated.

Disclaimer

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