Relugolix/Estradiol/Norethindrone

DEA Class; Rx

Common Brand Names; Myfembree

Pregnancy

Osteoporosis

Current or history of breast cancer or other hormone-sensitive malignancies

Hepatic impairment or disease

Undiagnosed abnormal uterine bleeding

Hypersensitivity to drug or its components

Uterine fibroids

• Hot flush, hyperhidrosis, or night sweats (10.6%)
• Increased total cholesterol 130 to <160 mg/dL (9.3%)
• Abnormal uterine bleeding (6.3%)
• Alopecia (3.5%)
• Libido decreased (3.1%)
• Irritability (2-3%)
• Dyspepsia (2-3%)
• Breast cyst (2-3%)
• Depression (2.4%)
• Irritability (2.4%)
• Increased total cholesterol >240 mg/dL (1.7%)
• Increased total cholesterol 160 to <190 mg/dL (1.5%)
• Anxiety (1.2%)

Endometriosis pain

• Headache (33%)
• Increased total cholesterol (200 to <240 mg/dL) (13.6%)
• Vasomotor symptoms (13.2%)
• Mood disorders (9.1%)
• Abnormal uterine bleeding (6.7%)
• Nausea (6%)
• Back pain (4.8%)
• Decreased sexual desire and arousal (4.3%)
• Arthralgia (3.6%)
• Fatigue (3.1%)
• Dizziness (3.1%)
• Diarrhea (2.4%)
• Peripheral edema (2.2%)
• Vulvovaginal dryness (2.2%)

Immediately discontinue if a hypersensitivity reaction occurs

Studies among estrogen users suggest a small increased relative risk of developing gallbladder disease; discontinue therapy if signs or symptoms of gallbladder disease or jaundice occur; assess the risk-benefit of continuing therapy for women with a history of cholestatic jaundice associated with past estrogen use or with pregnancy

New or worsening hypertension occurred; continue to monitor blood pressure (BP) and stop therapy if BP rises significantly

Women may experience amenorrhea or a reduction in the amount, intensity, or duration of menstrual bleeding, which may delay the ability to recognize pregnancy; perform pregnancy testing if pregnancy is suspected and discontinue treatment if pregnancy is confirmed

Based on animal studies and mechanism of action, early pregnancy loss may occur

Uterine fibroid prolapse and uterine fibroid expulsion reported; advise women with known or suspected submucosal uterine fibroids about the possibility of uterine fibroid prolapse or expulsion and to contact their physician if severe bleeding and/or cramping occur during treatment

Discontinue therapy if a hormone-sensitive malignancy is diagnosed; surveillance measures in accordance with standard of care (eg, breast examinations, mammography) are recommended; use of estrogen alone or estrogen plus progestin has been reported to result in an increase in abnormal mammograms requiring further evaluation

Contraindicated

Based on findings from animal studies and its mechanism of action, early pregnancy loss may occur

Discontinue if pregnancy occurs during treatment

There are no data on presence of relugolix or its metabolites in human milk, effects on the breastfed children, or effects on milk production