Relugolix tablet is a gonadotropin-releasing hormone (GnRH) receptor antagonist indicated for the treatment of adult patients with advanced prostate cancer.


Relugolix is a non-peptide small molecule, GnRH receptor antagonist. Relugolix competitively binds to pituitary GnRH receptors, thereby, reducing the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), and consequently testosterone.

Absorption: Relugolix is a substrate for intestinal P-gp. The mean (CV%) absolute bioavailability of Relugolix is approximately 12%. The median (range) Tmax of Relugolix is 2.25 hours.

Effect of Food: No clinically meaningful differences in the pharmacokinetics of Relugolix were observed following consumption of a high-calorie, high-fat meal.

Distribution: Plasma protein binding of Relugolix is 68 to 71%, primarily to albumin and to a lesser extent to α1- acid glycoprotein. The mean blood-to-plasma ratio is 0.78.

Elimination: The mean effective half-life of Relugolix is 25 hours and the mean (CV %) terminal elimination half-life is 60.8 (11%) hours. The mean (CV %) total clearance of Relugolix is 29.4 (15%) L/h and the renal clearance is 8 L/h.

Metabolism: Relugolix is metabolized primarily by CYP3A and to a lesser extent by CYP2C8 in vitro.

Excretion: After oral administration of a single 80mg radiolabeled dose of Relugolix, approximately 81% of the radioactivity was recovered in feces (4.2% as unchanged) and 4.1% in urine (2.2% as unchanged).

Dosage & Administration

A loading dose of 360 mg on the first day of treatment followed by 120 mg taken once daily, at approximately the same time each day. Relugolix Tablet can be taken with or without food. Advise patients to take a missed dose of Relugolix as soon as they remember. If the dose was missed by more than 12 hours, patients should not take the missed dose and resume with the next scheduled dose. If treatment with Relugolix is interrupted for greater than 7 days, restart Relugolix with a loading dose of 360 mg on the first day, and continue with a dose of 120 mg once daily.

Pediatric Use: The safety and efficacy of Relugolix in pediatric patients have not been established.

Geriatric Use: No overall differences in safety or effectiveness were observed between older and younger subjects.


P-gp Inhibitors: Avoid co-administration. If unavoidable, take Relugolix first, separate dosing by at least 6 hours, and monitor patients more frequently for adverse reactions. Combined P-gp and

Strong CYP3A Inducers: Avoid co-administration. If unavoidable, increase the Relupros ® dose to 240 mg once daily.

Side Effects

Adverse Reactions: The most common adverse reactions (≥10%) and laboratory abnormalities (≥15%) were hot flushes, glucose increased, triglycerides increased, musculoskeletal pain, haemoglobin decreased, alanine aminotransferase (ALT) increased, fatigue, aspartate aminotransferase (AST) increased, constipation, and diarrhea.

Common Side Effects
: Hot flushes, Increased blood sugar levels, Increased blood fat (triglyceride) levels, Muscle and joint pain, Decreased hemoglobin levels, Increased liver enzymes, Tiredness, Constipation, Diarrhoea

Rare Side Effects: Relugolix may cause rare side effects, including Changes in the electrical activity of your heart (QT prolongation), Dizziness, Fainting, Feeling that your heart is pounding or racing (palpitations), Chest pain. Other side effects include weight gain, decreased sex drive, and erectile function problems.

Pregnancy & Lactation

The safety and efficacy of Relugolix at the recommended dose of 120 mg daily have not been established in females. Females and Males of Reproductive Potential. Based on findings in animals and mechanism of action, Relugolix may impair fertility in males of reproductive potential.

Precautions & Warnings

QT/QTc Interval Prolongation: Androgen deprivation therapy may prolong the QT interval.

Embryo-Fetal Toxicity: Relugolix can cause fetal harm. Advise males with female partners of reproductive potential to use effective contraception.

Overdose Effects

There is no specific experience in the management of Relugolix overdose in patients.

Therapeutic Class

Gonadotropin-releasing hormone (GnRH) antagonist

Storage Conditions

Store in a cool and dry place, protect from light & moisture. Keep all medicines out of the reach of children.