Elagolix

Endometriosis Pain

Elagolix is used to treat moderate to severe pain associated with endometriosis. This condition occurs when tissue similar to the lining of the uterus grows in other parts of the body, often leading to chronic pelvic pain, painful periods, and pain during intercourse.

Uterine Fibroids

This medication is also indicated for the management of heavy menstrual bleeding caused by uterine fibroids. For this use, it is typically prescribed to women who have not yet gone through menopause. In these cases, elagolix is often used in combination with other hormones, such as estradiol and norethindrone, to help manage symptoms while protecting bone health.

Treatment Considerations

Healthcare providers typically prescribe elagolix for patients who require medical management of these symptoms. The use of this medication is generally limited to specific periods of time, as long-term use may affect bone mineral density. It is intended for use only in premenopausal women.

Mechanism of Action

Elagolix belongs to a class of medications known as gonadotropin-releasing hormone (GnRH) receptor antagonists. It works by blocking the GnRH receptors located in the pituitary gland, which is a small gland at the base of the brain.

Under normal conditions, the pituitary gland releases hormones that signal the ovaries to produce estrogen. By blocking these signals, elagolix causes a decrease in the production of:

• Luteinizing hormone (LH)
• Follicle-stimulating hormone (FSH)

When the levels of these hormones drop, the ovaries produce less estrogen. Because estrogen can stimulate the growth of endometrial tissue and contribute to heavy menstrual bleeding, reducing its levels helps to decrease pain and bleeding associated with conditions like endometriosis and uterine fibroids.

The effect of elagolix is dose-dependent, meaning that higher doses lead to a greater reduction in hormone levels. This allows the medication to be adjusted based on the specific condition being treated and the severity of the symptoms.

Common Side Effects

The most frequently reported side effects of elagolix include:

• Hot flashes or night sweats
• Headache
• Nausea
• Difficulty sleeping
• Changes in menstrual periods, such as irregular bleeding, spotting, or a total stop in menstruation
• Joint pain
• Anxiety

Serious Side Effects

Some side effects can be serious. Seek medical attention immediately if you experience any of the following:

• New or worsening depression, anxiety, or suicidal thoughts and behaviors
• Signs of liver problems, including yellowing of the skin or eyes (jaundice), dark urine, or pain in the upper right stomach area
• Bone loss, which may increase the risk of fractures and may not be fully reversible after stopping the medication
• Severe allergic reactions, such as a rash, hives, or swelling of the face, lips, or throat

Bone Mineral Density Loss

Elagolix causes a dose-dependent decrease in bone mineral density (BMD). This loss may not be completely reversible after stopping the medication. Because of this risk, the duration of use is limited based on the dosage prescribed. Assessment of bone density may be recommended for those with additional risk factors for bone loss, such as a history of low-impact fractures.

Suicidal Ideation and Mood Changes

Some individuals taking this medication have reported suicidal thoughts or behavior, as well as new or worsening depression and anxiety. Monitoring for changes in mood, behavior, or signs of depression is important during treatment.

Liver Health

Elevations in liver enzymes have been observed in clinical trials. This medication is not recommended for individuals with severe liver impairment. Signs of potential liver injury, such as yellowing of the skin or eyes, dark urine, or upper right-sided abdominal pain, require medical evaluation.

Pregnancy and Contraception

Elagolix is contraindicated in pregnancy because it may increase the risk of early pregnancy loss. It is not a contraceptive. Effective non-hormonal birth control, such as condoms or a diaphragm, must be used during treatment and for one week after the last dose. Because the medication often reduces or stops menstrual bleeding, it may be difficult to recognize a pregnancy.

Contraindications

• Known osteoporosis.
• Severe liver impairment.
• Concurrent use of strong OATP1B1 inhibitors, such as cyclosporine or gemfibrozil, which can significantly increase elagolix levels in the body.

Pregnancy

Elagolix is contraindicated for use during pregnancy. Research suggests that the medication may cause early pregnancy loss. Because elagolix often changes menstrual bleeding patterns, it can be difficult to recognize the early signs of pregnancy. A negative pregnancy test is typically required before starting treatment.

Individuals who can become pregnant should use effective non-hormonal contraception, such as condoms or a diaphragm, while taking elagolix and for at least one week after the final dose. Hormonal contraceptives, such as birth control pills, may be less effective during treatment. If pregnancy occurs or is suspected, the medication should be discontinued immediately and a healthcare provider should be consulted.

Breastfeeding

It is currently unknown if elagolix passes into human breast milk, how it affects milk production, or if it has any effect on a breastfed child. Because data are limited, the benefits of breastfeeding should be weighed against the clinical need for the medication. Patients are encouraged to discuss these factors with a healthcare professional to make an informed decision.

Available Forms

Elagolix is provided for oral use in the following forms:

• Tablets: These are film-coated oral tablets containing elagolix.
• Co-packaged Capsules: This format consists of a treatment pack containing different types of capsules. A capsule contains elagolix, while another capsule contains a combination of elagolix, estradiol, and norethindrone acetate.

FDA Approval Status

Elagolix was first approved by the U.S. Food and Drug Administration (FDA) in July 2018 for the management of moderate to severe pain associated with endometriosis. In May 2020, the FDA approved a combination therapy containing elagolix, estradiol, and norethindrone acetate for the treatment of heavy menstrual bleeding associated with uterine fibroids in premenopausal women.

Regulatory Warnings

The combination product containing elagolix, estradiol, and norethindrone acetate includes a boxed warning regarding the risk of serious vascular events, such as blood clots, heart attack, and stroke. This risk is higher in women who smoke or are over the age of 35.

The FDA has also identified several significant safety concerns for elagolix, including:

• Bone Mineral Density Loss: Use of elagolix is associated with a dose-dependent decrease in bone mineral density, which may not be completely reversible. Because of this, the duration of treatment is typically limited.
• Suicidal Ideation: Regulatory labeling includes warnings about suicidal thoughts and behavior, as well as the development or worsening of mood disorders.
• Hepatic Impairment: The medication is contraindicated in patients with severe liver disease due to the risk of drug-induced liver injury.

Factors Influencing Cost

The amount a patient pays for elagolix can vary significantly based on their individual circumstances. Key factors include:

• Insurance Coverage: Many commercial insurance plans and Medicare Part D provide coverage for elagolix, but the out-of-pocket cost will depend on the plan's specific formulary, deductible, and copayment or coinsurance requirements.
• Pharmacy Selection: Prices may differ between local retail pharmacies and mail-order pharmacy services.
• Prescription Type: Elagolix is available as a standalone medication and as part of a combination product. The specific formulation prescribed may affect the price.

Financial Assistance and Savings

Because elagolix is currently available only as a brand-name medication and does not have a generic equivalent, the cost may be higher for those without insurance. There are several options that may help reduce the cost:

• Manufacturer Savings Programs: The manufacturer may offer savings cards or copay assistance for patients with commercial insurance to help lower monthly out-of-pocket expenses.
• Patient Assistance Programs: For individuals who are uninsured or meet certain income criteria, assistance programs may be available to provide the medication at a lower cost or for free.

Patients are encouraged to contact their insurance provider or speak with a pharmacist to obtain the most accurate pricing information for their specific situation.