Buy Relugolix (Orgovyx) online

Price: 3,129 UAH

Known as original brand(s)

Orgovyx

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Relugolix is an oral, non-peptide gonadotropin-releasing hormone (GnRH) receptor antagonist originally marketed under the brand name Orgovyx. It is indicated in uro-oncology for the treatment of advanced prostate cancer, and in gynecology (in combination with estradiol and norethindrone acetate) for the management of uterine fibroids and endometriosis symptoms.

The mechanism of action of relugolix involves competitive and reversible binding to pituitary GnRH receptors. This results in rapid and dose-dependent suppression of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), leading to a profound reduction in testosterone levels in men (to castration levels) or estrogen/progesterone in women without an initial testosterone surge ("flare effect") typical of GnRH agonists.

Clinical utilization of relugolix provides convenient once-daily oral administration for reliable hormone suppression with faster recovery kinetics upon discontinuation.

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Relugolix (Orgovyx)

Indications

Relugolix is indicated in clinical practice for the following conditions:

  • Prostate Cancer: Treatment of adult patients with advanced hormone-sensitive prostate cancer.
  • Uterine Fibroids (Combination): Management of heavy menstrual bleeding associated with uterine fibroids in premenopausal women (as a fixed-dose combination therapy).
  • Endometriosis (Combination): Management of moderate to severe pain associated with endometriosis.

Dosage and administration

Relugolix is formulated for once-daily oral administration:

  • For Prostate Cancer (Orgovyx): Initiate with a loading dose of 360 mg (three 120 mg tablets) on the first day, followed by a maintenance dose of 120 mg taken orally once daily at approximately the same time, with or without food.
  • Administration Method: Swallow tablets whole with water without crushing or chewing.
  • Missed Dose: If a dose is missed, take it as soon as remembered on the same day. If more than 12 hours have passed, skip the missed dose and resume the normal schedule.
  • Monitoring: Regular monitoring of serum testosterone, prostate-specific antigen (PSA), liver function tests, and bone mineral density.

Relugolix is contraindicated in the following cases:

  • Hypersensitivity: Known hypersensitivity to relugolix or any formulation excipients.
  • Pregnancy and Lactation: Pregnancy and breastfeeding periods (teratogenic risks in females).
  • Severe Hepatic Impairment: Severe hepatic dysfunction.
  • Drug Interactions: Concomitant use with strong P-glycoprotein (P-gp) inducers (e.g., rifampin) that significantly lower systemic exposure.

Treatment with relugolix may cause the following adverse reactions:

  • Vascular & General: Hot flashes, fatigue, asthenia, and peripheral edema.
  • Metabolic & Musculoskeletal: Weight gain, arthralgia, myalgia, and decreased bone mineral density leading to osteopenia or osteoporosis risk.
  • Gastrointestinal: Diarrhea, constipation, abdominal pain, and transient elevations in liver transaminases (ALT, AST).
  • Cardiovascular: Hypertension and rare instances of QT interval prolongation.
  • Laboratory Abnormalities: Hypercholesterolemia and hypertriglyceridemia.

Frequently Asked Questions

Relugolix is an oral gonadotropin-releasing hormone (GnRH) receptor antagonist that competitively and reversibly binds to GnRH receptors in the anterior pituitary gland. This blocks interaction with the endogenous hormone and leads to a rapid, dose-dependent suppression of the secretion of luteinizing and follicle-stimulating hormones. As a result of this action, testosterone production by the testes is suppressed to castration levels in men, while estrogen and progesterone synthesis by the ovaries is reduced in women. The drug exhibits high bioavailability when taken orally and begins to act within the first day after the start of administration. This pharmacodynamics provides reliable control of hormone-dependent pathological processes without an initial surge in hormone levels.
The main indication for the use of Relugolix is the treatment of adult patients with advanced hormone-dependent prostate cancer requiring androgen deprivation therapy. In combined dosage forms, the drug is also widely used in gynecological practice for the symptomatic treatment of moderate to severe pain associated with uterine fibroids in women of reproductive age. In addition, this active substance is used for the treatment of endometriosis accompanied by severe pain and deterioration of the patient's quality of life. The drug effectively suppresses pathological cell proliferation and reduces symptom severity through deep regulation of sex hormones. The prescription of the medication is carried out exclusively by a specialized physician after performing all necessary diagnostic procedures.
For prostate cancer, Relugolix is typically taken as monotherapy at a fixed dose of one hundred and twenty milligrams once daily at the same time. Tablets should be swallowed whole with water, regardless of food intake. In gynecological practice for the treatment of uterine fibroids or endometriosis, the drug is used in combination with estradiol and norethisterone acetate according to a specific schedule once daily. In case of an accidental missed dose, the tablet should be taken as soon as possible on the same day, and the regular schedule resumed the next day. Taking a double dose of the drug to compensate for a missed dose is strictly prohibited. The duration of treatment is determined individually by the attending physician depending on the nature of the disease and therapy tolerability.
During treatment with Relugolix, hot flashes, fatigue, diarrhea, constipation, and joint or muscle pain are frequently observed. In men undergoing long-term androgen deprivation therapy, decreased libido, weight gain, and reduced bone mineral density may occur. To prevent bone mass loss, patients may require additional skeletal mineralization monitoring and intake of appropriate mineral supplements. Cardiovascular risks include an increased likelihood of arterial hypertension and heart rhythm changes, which require regular blood pressure measurement and ECG monitoring. If prominent adverse reactions occur, it is necessary to consult a physician to evaluate the benefit-risk ratio of continuing treatment.
Relugolix is a substrate of P-glycoprotein and cytochrome P450 enzymes, therefore concurrent administration with strong P-glycoprotein or CYP3A inducers can significantly reduce its blood concentration. Patients should avoid co-administration with potent inducers such as rifampin to prevent the loss of therapeutic efficacy. Regular monitoring of blood parameters, liver enzymes, and sex hormone levels in the body is required before and during therapy. The drug is contraindicated in case of hypersensitivity to the active substance, severe hepatic impairment, as well as in pregnant and breastfeeding women. Driving a vehicle and operating machinery require caution if dizziness or general weakness occurs during treatment.

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