Drug information of elagolix


Elagolix binds to the same receptors in the body as a certain hormone that stimulates the production of sex hormones. Elagolix works by lowering blood levels of estradiol and progesterone (female sex hormones).

Elagolix is used to treat moderate to severe pain caused by endometriosis.

Mechanism of effect

Elagolix is a short-acting, nonpeptide, gonadotropin-releasing hormone antagonist that suppresses pituitary and ovarian hormone function in a dose-dependent manner. Concentrations of LH, FSH, and estradiol are decreased during therapy and rapidly return to previous levels once treatment is discontinued. In patients with endometriosis, these actions reduce dysmenorrhea and nonmenstrual pelvic pain .



Hepatic via CYP3A (major pathway) and CYP2D6, CYP2C8, and UGTs

Feces 90%; urine <3%

Onset of Action:
FSH, LH, and estradiol suppression: Within hours of day 1 (initial) administration 

Time to Peak:
1 hour

Duration of Action:
FSH, LH, and estradiol concentrations return to baseline or higher within 24 to 48 hours after discontinuation

Half-Life Elimination:
4 to 6 hours

Protein Binding:
80%; to human plasma proteins

Drug indications

Endomtosiris: Management of moderate to severe pain associated with endometriosis.


Usual Adult Dose for Endometriosis:
150 mg orally once a day for 24 months

For Women with Dyspareunia:
-Consider 200 mg orally twice a day for 6 months

-Exclude pregnancy before starting or start therapy within 7 days from onset of menses.
-Use lowest effective dose, considering the severity of symptoms and treatment objectives.
-The duration of treatment is limited because of bone loss.

Use: For the management of moderate to severe pain associated with endometriosis.

Drug contraindications

Pregnancy; known osteoporosis; severe hepatic impairment (Child-Pugh class C); concomitant use of strong organic anion transporting polypeptide (OATP) 1B1 inhibitors (eg, cyclosporine, gemfibrozil)
Canadian labeling: Additional contraindications (not in US labeling): Hypersensitivity to elagolix or any component of the formulation; undiagnosed vaginal bleeding

Side effects

Side effects requiring immediate medical attention
Along with its needed effects, elagolix may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.
Check with your doctor immediately if any of the following side effects occur while taking elagolix:
More common
Absent, missed, or irregular menstrual periods
bone loss
fast heartbeat
hives, itching, skin rash
joint pain, stiffness, or swelling
mood swings
redness of the skin
stopping of menstrual bleeding
swelling of the eyelids, face, lips, hands, or feet
tightness in the chest
troubled breathing or swallowing
Less common
bleeding between periods
change in pattern of monthly periods
change in the amount of bleeding during periods
feeling sad or empty
lack of appetite
loss of interest or pleasure
trouble concentrating
trouble sleeping
Back pain
severe cramping
stomach or lower abdominal pain
thoughts or attempts at killing oneself
Side effects not requiring immediate medical attention
Some side effects of elagolix may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects.
Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:
More common
Feeling of warmth
night sweats
Less common
decreased interest in sexual intercourse
difficulty in moving
muscle pain or stiffness
weight gain

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Concerns related to adverse effects:
• Bleeding irregularities: Menstrual bleeding patterns may change, causing a decrease in the amount, intensity, or duration of bleeding. Changes in bleeding patterns may alter the ability to detect pregnancy. Pregnancy testing should be conducted if pregnancy is suspected; discontinue use if pregnancy is confirmed.
• BMD loss: A dose-dependent decrease in BMD is associated with elagolix exposure. The risk of BMD loss is increased with duration of use and may not be completely reversible following discontinuation of elagolix. Evaluate patients for osteoporosis risk factors (including a history of low-trauma fracture) prior to therapy. Consider supplementation with calcium and vitamin D. Duration of treatment should be limited to prevent BMD loss. Do not use in patients with known osteoporosis.
• Depression: Elagolix may increase the risk of depression and mood changes; risk may be increased in patients with a history of suicidality or depression. Suicidal ideation/behavior has been reported. Promptly evaluate new or worsening psychiatric symptoms and refer to a mental health care professional if appropriate. Patients should seek immediate medical attention for suicidal ideation and behavior. Consider risks and benefits of therapy if mood disturbances occur.
• Hepatic impairment: Dose-dependent elevations of ALT ≥3 times the upper limit of normal may occur; the lowest effective dose should be used. Promptly evaluate elevations in transaminases to assess risks versus benefits of continuing therapy. Dose adjustment is required in patients with moderate hepatic impairment; do not use in severe hepatic impairment.
Concurrent drug therapy issues:
• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

Do not use if you are pregnant. Elagolix may cause miscarriage.

Hormonal birth control methods (birth control pills, injections, implants) could make elagolix less effective. Use a condom or diaphragm with spermicide while you are taking elagolix and for at least 1 week after your last dose.

Elagolix can lower your estrogen levels, which may cause bone loss (osteoporosis). Talk with your doctor about ways to keep your bones healthy during and after treatment with elagolix.

Points of recommendation

Before taking this medicine:
- You should not use elagolix if you are allergic to it, or if:
-you have osteoporosis;
-you are pregnant or may become pregnant;
-you have severe liver disease; or
-you also use certain other medicines such as cyclosporine, gemfibrozil, or rifampin.

You may need to have a negative pregnancy test before starting this treatment. 

Do not use elagolix if you are pregnant, and tell your doctor right away if you become pregnant. This medicine may cause miscarriage.

Elagolix may change your menstrual periods, making it harder for you to know if you are pregnant. Other signs of pregnancy could include breast tenderness, nausea, and weight gain. 

Birth control pills can make elagolix less effective. Use a condom or diaphragm with spermicide to prevent pregnancy while using elagolix and for at least 1 week after your last dose. 

Tell your doctor if you have ever had:
- a broken bone;
-low bone mineral density;
-depression or a mood disorder; or
- suicidal thoughts or actions.

Elagolix can lower your estrogen levels, which may cause bone loss (osteoporosis). Talk with your doctor about ways to keep your bones healthy during and after treatment with this medicine. 

It may not be safe to breast-feed while using this medicine. Ask your doctor about any risk.

Take the medicine at the same time each day, with or without food.

Your dosing schedule may change if you switch to a different strength of elagolix. Follow your doctor's dosing instructions very carefully.

Store at room temperature away from moisture and heat.

ake the missed dose if you remember it later in the day. Otherwise, skip the missed dose and go back to your regular schedule. Do not take two doses at one time.

Store at 2°C to 30°C (36°F to 86°F).

Pregnancy level



US FDA pregnancy category: Not Assigned

Risk Summary: Exposure to this drug early in pregnancy may increase the risk of early pregnancy loss; limited human data are insufficient to determine if there is a risk for major birth defects or miscarriage.

-Pregnancy must be excluded before starting therapy or therapy must start within 7 days from onset of menses.
-Advise women to use effective non-hormonal contraception during therapy and for 1 week following discontinuation.
-This drug should be discontinued if pregnancy occurs.

Breast feeding warning

Benefit should outweigh risk

Excreted into human milk: Unknown
Excreted into animal milk: Unknown

-There are no data on the effects of this drug on the breastfed infant or its effects on milk production.
-The developmental and health benefits of breastfeeding should be considered along with the mother's clinical need for this drug and any potential adverse effects to the breastfed infant from the drug or from the underlying maternal condition.

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