Relugonat — Relugolix 120 mg Tablets, 30 Tablets

Relugonat is supplied as film-coated tablets containing 120 mg of relugolix.

Qualitative and Quantitative Composition per Tablet:

• Active Ingredient: Relugolix — 120 mg.
• Excipients: Mannitol, sodium starch glycolate, hydroxypropyl cellulose, magnesium stearate, hypromellose, titanium dioxide, iron oxide red.

Packaging and Presentation: Light red to pink, round, biconvex film-coated tablets with debossing. 30 tablets packed in a plastic bottle sealed with a tamper-evident child-resistant cap. The bottle and prescribing information are enclosed in an outer carton displaying Relugonat (Relugolix Tablets) 120 mg and Natco Pharma corporate graphics.

Pharmacodynamics:
Relugolix is a non-peptide gonadotropin-releasing hormone (GnRH) receptor antagonist. It blocks GnRH receptors in the anterior pituitary gland, preventing endogenous stimulation of gonadotropin production (LH and FSH). This reduces testicular testosterone secretion in males to castrate levels (< 50 ng/dL). Testosterone suppression is maintained throughout the period of daily dosing.

Pharmacokinetics:

• Absorption: Relugolix is rapidly absorbed following oral administration. Peak plasma concentrations ($C_{max}$) are reached within 1.5 to 2.5 hours. Absolute bioavailability is approximately 12%.
• Distribution: Plasma protein binding is approximately 68% to 71%. Volume of distribution is large.
• Metabolism: Metabolized primarily in the liver via CYP3A and CYP2C8 enzymes, as well as P-glycoprotein (P-gp) transport. The majority is excreted unchanged.
• Elimination: Excreted predominantly via feces (~81% unchanged) and renally (~4.1%). Terminal elimination half-life ($T_{1/2}$) is approximately 25 hours.

Relugonat is indicated in adult males for:

• Prostate Cancer: Treatment of adult patients with advanced hormone-dependent prostate cancer.

Relugonat is administered orally once daily at the same time each day, regardless of food intake.

Dosing Regimen:

• Recommended Dose: A loading dose of 360 mg (three 120 mg tablets) is administered on the first day of treatment, followed by a maintenance dose of 120 mg once daily starting on the second day.
• Administration Instructions: Swallow tablets whole with water without chewing or crushing.
• Concurrent Therapy: Due to its antagonistic mechanism, co-prescribing antiandrogens to prevent a flare effect at therapy initiation is unnecessary.

Administration of Relugonat is contraindicated in:

• Hypersensitivity: Known hypersensitivity to relugolix or any excipient.
• Gender Restrictions: Intended exclusively for males (contraindicated in females, especially pregnant or nursing women).
• Pediatric Population: Safety and efficacy in individuals under 18 years of age have not been established.

Evaluated drug interactions for Relugonat include:

• P-gp and CYP3A Inhibitors (e.g., ketoconazole, amiodarone, verapamil): May significantly increase relugolix plasma concentrations. If co-administration is necessary, separate dosing schedules as recommended by a physician.
• P-gp and CYP3A Inducers (rifampicin, carbamazepine, St. John's wort): May significantly decrease relugolix efficacy. Concomitant use should be avoided.

Pregnancy and Lactation:
Relugonat is intended for use exclusively in males. The drug is contraindicated in women who are or may become pregnant or who are breastfeeding. Male patients with female partners of childbearing potential must use effective contraception during treatment and for 2 weeks after the final dose.

The most frequent and clinically significant adverse reactions associated with relugolix (resulting from androgen deprivation) include:

• Vascular & Thermoregulation (Very Common): Hot flashes, hyperhidrosis.
• Musculoskeletal System: Arthralgia, myalgia, fatigue, decreased bone mineral density.
• Gastrointestinal Tract: Diarrhea, constipation, abdominal pain.
• Metabolic Disorders: Weight gain, elevated cholesterol, triglycerides, and blood glucose.
• Cardiovascular System: Hypertension, rare cases of QT interval prolongation.
• Other: Decreased libido, erectile dysfunction.

Symptoms:
Acute overdose data for relugolix are limited. Clinical manifestations may correspond to an intensification of known adverse reactions (hot flashes, fatigue, dyspepsia).

Treatment:
No specific antidote exists. Supportive and symptomatic care should be initiated, with monitoring of vital organ functions.

Storage Requirements for Relugonat 120 mg:

• 🌡️ Temperature Range: Store in a dry place at temperatures not exceeding 25–30 °C.
• 💧 Moisture Protection: Keep in a tightly closed bottle to protect from moisture.
• 👶 Safety Precautions: Keep strictly out of reach of children.
• ⏳ Shelf Life: Stated on carton and bottle. Do not use past expiration date. Prescription-only medicine.

To verify authenticity of genuine Relugonat 120 mg manufactured by Natco Pharma, inspect the following features:

• ✅ Corporate Logo: Distinctive blue-green Natco Pharma corporate logo printed on the outer carton and bottle label.
• ✅ Packaging Markings: Clear factory printing displaying Batch No., Mfg. Date, Exp. Date, and product designation Relugonat (Relugolix Tablets) 120 mg.
• ✅ Bottle Quantity: Standard bottle contains exactly 30 tablets.
• ✅ Print Quality: High-grade packaging artwork without color fading or typography errors.