relugolix/estradiol/norethindrone acetate

relugolix/estradiol/norethindrone acetate is a fixed-dose combination oral tablet containing relugolix 40 mg, estradiol 1 mg and norethindrone acetate 0.5 mg.

relugolix/estradiol/norethindrone acetate is a GnRH antagonist / Estrogen replacement / Progestin and is used to treat the following:

• Heavy menstrual bleeding related to uterine fibroids in women who haven’t reached menopause
• Moderate-to-severe pain related to endometriosis in women who haven’t reached menopause

relugolix/estradiol/norethindrone acetate is a combination of three medications. Relugolix is a gonadotropin-releasing hormone (GnRH) antagonist. GnRH is a natural hormone in the body that plays a role in making estrogen and progesterone hormones. These hormones all play a role in maintaining your reproductive system. Relugolix blocks the actions of GnRH, which lowers the estrogen and progesterone levels in your body. This lessens bleeding that happens with uterine fibroids and pain from endometriosis. Estradiol is an estrogen replacement. It replaces some of the estrogen in your body that’s lost from relugolix. Replacing estrogen might help prevent bone loss. Norethindrone is a progestin (a lab-made form of progesterone). It replaces some of the progesterone in your body that’s lost from relugolix. This might help protect the uterus from damage from the effects of estrogen alone, which might help prevent uterine (endometrial) cancer.

relugolix/estradiol/norethindrone acetate is typically taken as 1 tablet by mouth once a day around the same time each day, with or without food. It’s recommended to take the medication for a maximum of 2 years because of the risk for bone loss.

relugolix/estradiol/norethindrone acetate is a safe and effective treatment when used for FDA licensed indications. However, like all medications, they may give you unwanted side effects. You should always discuss potential side effects with your physician to ensure the medication is suitable and right for you. You should not use this medication in the following:

• High risk of arterial, venous thrombotic, or thromboembolic disorder
• Pregnancy
• Known osteoporosis
• Current or history of breast cancer or other hormone-sensitive malignancies
• Known hepatic impairment or disease
• Undiagnosed abnormal uterine bleeding
• Known hypersensitivity to components of relugolix/estradiol/norethindrone acetate

Common side effects of relugolix/estradiol/norethindrone acetate:

• New or worsening high blood pressure
• Unusual or irregular vaginal bleeding
• Hair loss or hair thinning
• Headache
• Hot flashes, a lot of sweating, or night sweats
• Mood problems or mood swings
• Unusual vaginal bleeding
• Nausea

Serious side effects are rare with relugolix/estradiol/norethindrone acetate. Contact your healthcare provider immediately if you experience any of the following.

• Blood clot: swelling or redness in the leg, shortness of breath, chest pain
• Heart attack: shortness of breath, arm or chest pain, sweating
• Stroke: slurred speech, vision changes, facial drooping, sudden weakness on one side of the body, sudden headache
• Liver or gallbladder problems: yellowing of your skin or eyes (jaundice), pain in the upper right part of your stomach, nausea, vomiting, dark urine
• Uterine fibroid that comes out into the vagina: heavy menstrual bleeding, severe cramping
• Suicidal thoughts or behavior
• Serious allergic reaction: swelling in the face, tongue, or throat; trouble breathing; hives

The following medications may interact with relugolix/estradiol/norethindrone acetate:

• Avoid use of relugolix/estradiol/norethindrone acetate with oral P-gp inhibitors
• Avoid use with combined P-gp and strong CYP3A inducers, as the exposure of the components of relugolix/estradiol/norethindrone acetate may be decreased

Various FDA-approved generic manufacturers

relugolix/estradiol/norethindrone acetate is contraindicated in pregnancy. Based on findings from animal studies and its mechanism of action, relugolix/estradiol/norethindrone acetate may cause early pregnancy loss. Discontinue relugolix/estradiol/norethindrone acetate if pregnancy occurs during treatmentThere is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to relugolix/estradiol/norethindrone acetate during pregnancy. Pregnant females exposed to relugolix/estradiol/norethindrone acetate and healthcare providers are encouraged to call the relugolix/estradiol/norethindrone acetate Pregnancy Exposure Registry at 1-855-428-0707.

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