Golixter 120mg – Barter & Marcin Pharma

GOLIXTER 120 MG

Product Overview

Golixter 120 mg Tablet contains Relugolix, an oral Gonadotropin-Releasing Hormone (GnRH) receptor antagonist used in the management of advanced prostate cancer. It works by blocking GnRH receptors in the anterior pituitary gland, which suppresses the production of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), ultimately reducing testosterone levels in men.

Lowering testosterone levels helps slow the growth and progression of prostate cancer.

Golixter offers the convenience of once-daily oral therapy and is designed to provide effective androgen deprivation without the need for injectable treatment.

Composition

Each film-coated tablet contains:

Ingredient
Relugolix 120 mg

Dosage form: Oral Tablet

Therapeutic Class

Antineoplastic Agent
GnRH Receptor Antagonist
Hormonal Therapy for Prostate Cancer

Indications

Golixter 120 mg is indicated for:

Treatment of adult patients with advanced prostate cancer

The medication suppresses testosterone production, which is necessary for the growth of prostate cancer cells.

Dosage & Administration

Standard Adult Dosing

Day 1 (Loading Dose): 360 mg orally
Maintenance Dose: 120 mg once daily thereafter

Administration Instructions

Take once daily at approximately the same time each day
May be taken with or without food
Swallow tablet whole; do not crush or chew

Missed Dose

If remembered within 12 hours, take the missed dose immediately
If more than 12 hours have passed, skip the missed dose and continue the regular schedule
If treatment is interrupted for more than 7 days, restart with 360 mg loading dose, followed by 120 mg daily

Dose Adjustments

Renal Impairment

Condition	Recommendation
Mild to Severe (CrCl 15–89 mL/min)	No dosage adjustment required
End-stage renal disease	Not studied

Hepatic Impairment

Condition	Recommendation
Mild to Moderate (Child-Pugh A or B)	No dosage adjustment required
Severe (Child-Pugh C)	Not studied

Drug Interactions

P-glycoprotein (P-gp) Inhibitors

Avoid coadministration of Relugolix with P-gp inhibitors where possible.
If concomitant use cannot be avoided, take Relugolix first and separate dosing by at least 6 hours.
For short-term treatment with a P-gp inhibitor, Relugolix therapy may be temporarily interrupted for up to 2 weeks.
If treatment interruption exceeds 7 days, restart therapy with a 360 mg loading dose followed by 120 mg once daily.

Combined P-gp and Strong CYP3A Inducers

Coadministration with combined P-gp and strong CYP3A inducers should be avoided.
If concomitant therapy cannot be avoided, increase the Relugolix dose to 240 mg orally once daily.
After discontinuation of the inducer, resume the standard maintenance dose of 120 mg once daily.

Warnings and Precautions

QT Interval Prolongation

Androgen deprivation therapy may prolong the QT/QTc interval. Use caution in patients with:

Congenital long QT syndrome
Congestive heart failure
Electrolyte abnormalities
Concomitant QT-prolonging medications

Hypersensitivity Reactions

Hypersensitivity reactions including:

Angioedema
Urticaria
Pharyngeal edema

Patients experiencing symptoms should stop treatment immediately and seek medical attention.

Diagnostic Test Interference

Suppression of the pituitary-gonadal axis may affect hormone-related diagnostic tests.

Regular monitoring of:

Prostate-Specific Antigen (PSA)
Serum testosterone levels

is recommended.

Electrolyte Monitoring

Electrolyte abnormalities should be corrected before initiating therapy.

Adverse Effects

Common Adverse Effects (>10%)

Hot flush (54%)
Increased blood glucose (44%)
Increased triglycerides (35%)
Musculoskeletal pain (30%)
Decreased hemoglobin (28%)
Increased ALT (27%)
Fatigue (26%)
Increased AST (18%)
Diarrhea (12%)
Constipation (12%)

Less Common (1–10%)

Weight gain
Insomnia
Gynecomastia
Hyperhidrosis
Depression
Decreased libido

Serious Reactions (Rare)

Severe hot flush
Severe fatigue
Elevated liver enzymes
Severe diarrhea

Post-Marketing Reports

Hypersensitivity reactions
Angioedema
Urticaria

Use in Pregnancy and Lactation

Pregnancy

Based on animal studies and mechanism of action, Relugolix may cause fetal harm and pregnancy loss.

Human data are not available.

Contraception

Men with partners of reproductive potential should use effective contraception during treatment and for 2 weeks after the last dose.

Fertility

Relugolix may impair fertility in males.

Lactation

Data regarding presence in human milk are unavailable.

Pharmacology

Mechanism of Action

Relugolix is a GnRH receptor antagonist that binds to receptors in the anterior pituitary gland, blocking GnRH signaling. This suppresses the release of LH and FSH, reducing testosterone production in the testes.

Lower testosterone levels help slow the growth of testosterone-dependent prostate cancer cells.

Pharmacokinetics

Absorption

Absolute bioavailability: ~12%
Peak plasma time: 2.25 hours

Peak Plasma Concentration

Dose: 360 mg; Concentration: 215 ng/mL
Dose: 120 mg; Concentration: 70 ng/mL

Distribution

Protein binding: 68–71%
Blood/plasma ratio: 0.78

Metabolism

Primarily via CYP3A
Minor metabolism via CYP2C8

Elimination

Half-life: ~25 hours
Terminal half-life: ~60.8 hours
Total clearance: 29.4 L/hr

Excretion

Feces: 81%
Urine: 4.1%

Storage

Store at room temperature below 30°C
Keep tablets in original container
Ensure container remains tightly closed after opening

Packaging

Available as Golixter 120 mg tablets in pharmaceutical packaging suitable for prescription use.