Elagolix

Generic name: Elagolix
Brand name: Orilissa,
Dosage form: oral tablet
Drug class: Gonadotropin-releasing hormone antagonists

Medically reviewed by  A Ras MD.

What is elagolix?

Elagolix is a prescription medicine that is used to treat pain caused by endometriosis.

Description

Elagolix consists of two capsules: one to be taken orally in the morning (AM) and one to be taken orally in the evening (PM). The AM capsule is white and yellow and contains 300 mg elagolix (equivalent to 310.4 mg of elagolix sodium), 1 mg estradiol, and 0.5 mg norethindrone acetate. The PM capsule is white and light blue and contains 300 mg of elagolix (equivalent to 310 mg of elagolix sodium).

Elagolix

Elagolix sodium is the sodium salt of the active moiety elagolix, a nonpeptide small molecule, GnRH receptor antagonist. Elagolix sodium is chemically described as sodium 4-({(1R)-2-[5-(2-fluoro-3-methoxyphenyl)-3-{[2-fluoro-6-(trifluoromethyl)phenyl]methyl}-4-methyl-2,6-dioxo-3,6-dihydropyrimidin-1(2H)-yl]-1-phenylethyl}amino)butanoate. Elagolix sodium has a molecular formula of C32H29F5N3O5Na and a molecular weight of 653.58. Elagolix free acid has a molecular formula of C32H30F5N3O5 and a molecular weight of 631.60.

Elagolix sodium has the following structural formula:

Elagolix sodium is a white to off-white to light yellow powder and is freely soluble in water.

Estradiol

Estradiol (E2), an estrogen, is a white or almost white crystalline powder. Its chemical name is estra-1,3,5(10)-triene-3,17β-diol with the molecular formula of C18H24O2, and molecular weight of 272.38. The structural formula of E2 is as follows:

Norethindrone acetate

Norethindrone acetate (NETA), a progestin, is a white or yellowish white crystalline powder. Its chemical name is 17β-acetoxy-19-nor-17α-pregn-4-en-20-yn-3-one with the molecular formula of C22H28O3 and molecular weight of 340.46.

Elagolix  morning (AM) capsules contain the following inactive ingredients: anhydrous sodium carbonate, polyethylene glycol 3350, crospovidone, colloidal silicon dioxide, magnesium stearate, polyvinyl alcohol, titanium dioxide, polyethylene glycol, talc, purified water, lactose monohydrate, starch (corn), copovidone, talc, hypromellose, triacetin, and gelatin capsule shell. The capsule shell contains the following ingredients: FD&C Red #40, FD&C Yellow #5 [see Warnings and Precautions (5.12)], FD&C Yellow #6, titanium dioxide, gelatin, and printing ink (shellac, dehydrated alcohol, isopropyl alcohol, butyl alcohol, propylene glycol, strong ammonia solution, black iron oxide, potassium hydroxide, and purified water).

ORIAHNN evening (PM) capsules contain the following inactive ingredients: anhydrous sodium carbonate, polyethylene glycol 3350, crospovidone, colloidal silicon dioxide, magnesium stearate, polyvinyl alcohol, titanium dioxide, polyethylene glycol, talc, purified water, and gelatin capsule shell. The capsule shell contains the following ingredients: FD&C Blue #2, FDA/E172 yellow iron oxide, titanium dioxide, gelatin, and printing ink (shellac, dehydrated alcohol, isopropyl alcohol, butyl alcohol, propylene glycol, strong ammonia solution, black iron oxide, potassium hydroxide, and purified water).

 Mechanism of Action

Elagolix is a GnRH receptor antagonist that inhibits endogenous GnRH signaling by binding competitively to GnRH receptors in the pituitary gland. Administration of elagolix results in dose-dependent suppression of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), leading to decreased blood concentrations of the ovarian sex hormones estradiol and progesterone and reduces bleeding associated with uterine fibroids.

E2 acts by binding to nuclear receptors that are expressed in estrogen-responsive tissues. As a component of ORIAHNN, the addition of exogenous estradiol may reduce the increase in bone resorption and resultant bone loss that can occur due to a decrease in circulating estrogen from elagolix alone.

Progestins such as NETA act by binding to nuclear receptors that are expressed in progesterone-responsive tissues. As a component of ORIAHNN, NETA may protect the uterus from the potential adverse endometrial effects of unopposed estrogen.

Before taking elagolix, tell your doctor:

• If you are allergic to elagolix; any part of this medicine; or any other drugs, foods, or substances. Tell your doctor about the allergy and what signs you had.
• If you have any of these health problems: Liver disease or soft, brittle bones (osteoporosis).
• If you are taking any of these drugs: Cyclosporine or gemfibrozil.
• If you are pregnant or may be pregnant. Do not take elagolix if you are pregnant.

This is not a list of all drugs or health problems that interact with elagolix.

Tell your doctor and pharmacist about all of your drugs (prescription or OTC, natural products, vitamins) and health problems. You must check to make sure that it is safe for you to take elagolix with all of your drugs and health problems. Do not start, stop, or change the dose of any drug without checking with your doctor.

What are some things I need to know or do while I take elagolix?

• Tell all of your health care providers that you take elagolix. This includes your doctors, nurses, pharmacists, and dentists.
• This medicine may cause bones to weaken. This effect is greater the longer you take elagolix and may not go back to normal when elagolix is stopped. If you have questions, talk with your doctor.
• Take calcium and vitamin D as you were told by your doctor.
• Have blood work checked as you have been told by the doctor. Talk with the doctor.
• Birth control pills and other hormone-based birth control may not work as well to prevent pregnancy. Use some other kind of birth control, like a condom, while you are taking elagolix and for 7 days after stopping it.
• This medicine may cause harm to the unborn baby or loss of the unborn baby if you take it while you are pregnant.
• This medicine may cause menstrual period changes like abnormal bleeding or spotting, less bleeding, or no bleeding. This may make it hard to know if you are pregnant. Call your doctor if you have other signs of pregnancy like tender breasts, weight gain, or upset stomach.
• If you are a woman and you miss a period, have unprotected sex, or think that your birth control has not worked, call your doctor right away.
• Tell your doctor if you are breast-feeding. You will need to talk about any risks to your baby.

How is elagolix best taken?

Use elagolix as ordered by your doctor. Read all information given to you. Follow all instructions closely.

• Take with or without food.
• Take elagolix at the same time of day.
• Have a pregnancy test before starting elagolix, or start taking it within 7 days of when your menstrual period starts. Talk with your doctor if you are not sure how to start elagolix.

What do I do if I miss a dose?

• Take a missed dose as soon as you think about it.
• If it is close to the time for your next dose, skip the missed dose and go back to your normal time.
• Do not take 2 doses at the same time or extra doses.

What are the side effects of elagolix that I need to call my doctor about immediately?

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
• Signs of liver problems like dark urine, feeling tired, not hungry, upset stomach or stomach pain, light-colored stools, throwing up, or yellow skin or eyes.
• New or worse behavior or mood changes like depression or thoughts of killing yourself.
• Anxiety.

What are some other side effects of elagolix?

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Period (menstrual) changes.
• Hot flashes.
• Night sweats.
• Headache.
• Upset stomach.
• Not able to sleep.
• Joint pain.

These are not all of the side effects that may occur. If you have questions about side effects, call your doctor. Call your doctor for medical advice about side effects.

You may report side effects to the FDA at 1-800-332-1088. You may also report side effects at https://www.fda.gov/medwatch.

If overdose is suspected:

If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

How do I store and/or throw out elagolix?

• Store in a refrigerator or at room temperature.
• Store in a dry place. Do not store in a bathroom.
• Keep all drugs in a safe place. Keep all drugs out of the reach of children and pets.
• Throw away unused or expired drugs. Do not flush down a toilet or pour down a drain unless you are told to do so. Check with your pharmacist if you have questions about the best way to throw out drugs. There may be drug take-back programs in your area.