Rexilo(Relugolix)

Therapeutic Group: Others

Presentation

Rexilo 120: Each tablet contains Relugolix 120 mg.

Description

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

Indications

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

Dosage & Administration

Recommended Dosage: A loading dose of 360 mg on the first day of treatment followed by 120 mg taken orally once daily, at approximately the same time each day
Relugolix can be taken with or without food. Patients should be instructed to swallow tablets whole and not to crush or chew tablets

Side Effects

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

Precautions

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.

Use in 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
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 these subjects and younger subjects.

Drug Interaction

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 RELUGOLIX dose to 240 mg once daily

Storage

Do not Store above 30 C. Keep out of the reach of children and light.

Commercial Pack

Rexilo 120: Each box contains 1 blister of 10 Tablets.