Elagolix sodium

Elagolix is a GnRH receptor antagonist that inhibits endogenous GnRH signaling by competitively binding to GnRH receptors in the pituitary gland. It suppresses LH and FSH, decreasing estradiol and progesterone levels. Used for moderate to severe pain associated with endometriosis. Recommended dose: 150 mg once daily (up to 24 months) or 200 mg twice daily (up to 6 months with dyspareunia). Exclude pregnancy before starting treatment. Contraindicated in pregnancy, osteoporosis, severe hepatic impairment and with strong OATP1B1 inhibitors.

• Management of moderate to severe pain associated with endometriosis

Elagolix is a GnRH receptor antagonist that competitively binds to GnRH receptors in the pituitary gland, inhibiting endogenous GnRH signaling. Administration results in dose-dependent suppression of LH and FSH, leading to decreased blood concentrations of estradiol and progesterone.

Elagolix competitively binds to GnRH receptors in the pituitary gland, suppressing LH and FSH secretion, decreasing estradiol and progesterone levels, and reducing endometriosis pain.

Adult Dose:

• 150 mg: Once daily, up to 24 months (up to 6 months in moderate hepatic impairment).
• 200 mg: Twice daily, up to 6 months (with coexisting dyspareunia). 200 mg dose should not exceed 6 months (may decrease BMD).

Exclude pregnancy before starting treatment and start Elagolix within 7 days from onset of menses.

Oral tablet. Take in the dose and duration as advised by your doctor. May be taken with or without food.

If you miss a dose of Elagolix, take it as soon as possible. If it is almost time for your next dose, skip the missed dose and go back to your regular schedule.

Common Side Effects:

• Hot flushes
• Night sweats
• Headache
• Nausea
• Amenorrhea
• Arthralgia
• Mood changes
• Bone loss (decreased BMD)

Rare Side Effects:

• Insomnia
• Anxiety
• Elevated hepatic transaminase

• Bone Loss: Dose and duration-dependent decreases in BMD that may not be completely reversible. Assess BMD in women with additional risk factors.
• Reduced Ability to Recognize Pregnancy: Elagolix may alter menstrual bleeding. Perform testing if pregnancy is suspected.
• Suicidal Ideation and Mood Disorders: Advise patients to seek medical attention for suicidal thoughts, new or worsening depression, anxiety or mood changes.
• Hepatic Transaminase Elevations: Dose-dependent elevations in serum ALT. Counsel patients on signs/symptoms of liver injury.

• Pregnancy (exposure early in pregnancy may increase risk of early pregnancy loss)
• Osteoporosis (increases risk of further bone loss)
• Severe hepatic impairment
• Concomitant use with strong OATP1B1 inhibitors (e.g., cyclosporine and gemfibrozil)

May potentiate P-gp substrates (e.g., digoxin), CYP2C19 substrates (e.g., omeprazole; limit doses to <40 mg daily). May antagonize CYP3A substrates. Antagonizes oral midazolam, rosuvastatin. May be antagonized by CYP3A inducers. Reduced efficacy with estrogen-containing contraceptives.

No known food interactions.

Limited human data on use in pregnancy. Exposure early in pregnancy may increase risk of early pregnancy loss. Contraindicated in pregnancy.

No information on presence of elagolix or its metabolites in human milk, effects on breastfed child or milk production.

Safety and effectiveness in patients less than 18 years have not been established.

Limited information available regarding dose adjustment for elderly patients.

Renal impairment: No dose adjustment required in any degree of renal impairment.

Hepatic impairment: No dose adjustment required in mild hepatic impairment. 200 mg dose not recommended in moderate to severe hepatic impairment.

In case of overdose, monitor patients for signs/symptoms of adverse reactions and initiate appropriate symptomatic treatment.

Store in a cool & dry place, protect from light & moisture. Keep out of reach of children.

Elagolix sodium