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SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS › PITUITARY AND HYPOTHALAMIC HORMONES AND ANALOGUES › HYPOTHALAMIC HORMONES › Anti-gonadotropin-releasing hormones
relugolix, estradiol and norethisterone
H01CC54
Forms & Strengths
- Combination tablet: relugolix 40 mg, estradiol 1 mg, and norethisterone acetate 0.5 mg
Adult Dosing
- Uterine fibroids: 1 tablet orally once daily with or without food for up to 24 months
- Endometriosis: 1 tablet orally once daily with or without food for up to 24 months
Pediatric Dosing
- Safety and efficacy not established in pediatric patients post-menarche
- Not indicated for use in premenarchal pediatric patients
Indications
- Management of heavy menstrual bleeding associated with uterine leiomyomas (fibroids) in premenopausal women
- Management of moderate to severe pain associated with endometriosis in premenopausal women
Mechanism of Action
- Relugolix is a non-peptide gonadotropin-releasing hormone (GnRH) receptor antagonist that decreases LH and FSH secretion
- Estradiol (an estrogen) is added to reduce bone loss and hypoestrogenic symptoms
- Norethisterone acetate (a progestin) is added to protect the endometrium from estrogen-induced hyperplasia
Contraindications
- High risk of arterial or venous thrombotic disorders
- Known or suspected pregnancy
- Known osteoporosis or baseline bone mineral density significantly below the mean
- Known or suspected estrogen- or progestin-sensitive malignancies
- Undiagnosed abnormal uterine bleeding
- Known hepatic impairment or disease
- History of known hypersensitivity to the active substances or excipients
Adverse Reactions
- Vasomotor symptoms (hot flushes)
- Hyperhidrosis and night sweats
- Uterine bleeding changes
- Alopecia
- Decreased libido
- Bone mineral density decrease
- Depression and mood changes
- Headache
Drug Interactions
- P-glycoprotein (P-gp) inhibitors: Co-administration may increase relugolix exposure; administer relugolix at least 6 hours before or after P-gp inhibitors if co-administration is unavoidable
- Combined P-gp and strong CYP3A inducers: May decrease relugolix exposure, leading to reduced efficacy; avoid concomitant use
- Hormonal contraceptives: Concomitant use with other hormonal contraceptives is contraindicated
Curated Content: Needs Vetting Before Put to Clinical Use