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.
With medicine: 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; consider increasing their doses. May be antagonized by CYP3A inducers. Reduced efficacy with estrogen-containing contraceptives.
With food and others: No known food interaction.
It is contraindicated in pregnant women because exposure to Elagolix early in pregnancy may increase the risk of early pregnancy loss. With known osteoporosis, it can increase the risk of further bone loss. It is also contraindicated for severe hepatic impairment and also with concomitant use of strong organic anion transporting polypeptide OATP1B1 inhibitors (e.g. cyclosporine and gemfibrozil).
Common: The most common side effects include hot flushes, night sweats, headache, nausea, amenorrhea, , arthralgia, mood changes & bone loss. Rare: Insomnia, anxiety & elevated hepatic transaminase.
The limited human data with the use of Elagolix in pregnant women are insufficient to determine whether there is a risk for major birth defects or miscarriage. Exposure to Elagolix early in pregnancy may increase the risk of early pregnancy loss. Use of it is contraindicated in pregnant women. Elagolix has to be discontinued if pregnancy occurs during treatment. There is no information on the presence of elagolix or its metabolites in human milk, the effects on the breastfed child or the effects on milk production.
Bone Loss: Dose and duration-dependent decreases in bone mineral density (BMD) that may not be completely reversible. Assess BMD in women with additional risk factors for bone loss.
Reduced Ability to Recognize Pregnancy: Elagolix may alter menstrual bleeding, which may reduce the ability to recognize pregnancy. Perform testing if pregnancy is suspected. Discontinue if pregnancy is confirmed.
Suicidal Ideation and Mood Disorders: Advise patients to seek medical attention for suicidal ideation, suicidal behavior, new onset or worsening depression, anxiety, or other mood changes.
Hepatic Transaminase Elevations: Dose-dependent elevations in serum alanine aminotransferase (ALT). Counsel patients on signs and symptoms of liver injury.
Potential for Reduced Efficacy with Estrogen-Containing Contraceptives: Use non-hormonal contraception during treatment and for one week after discontinuing Elagolix.
No dose adjustment of Elagolix is required in women with any degree of renal impairment or end-stage renal disease (including women on dialysis)
No dosage adjustment of Elagolix is required in women with mild hepatic impairment.
Safety and effectiveness of Elagolix in patients less than 18 years of age have not been established.
In case of overdose, patients should be monitored for any signs or symptoms of adverse reactions and initiate appropriate symptomatic treatment, as needed.
