Note: This document contains side effect information about elagolix. Some dosage forms listed on this page may not apply to the brand name Orilissa.

Applies to elagolix: oral tablets.

Side effects include:

Hot flushes or night sweats, headache, nausea, insomnia, altered mood or mood swings, amenorrhea, depression-related adverse effects (i.e., depressed mood, depression, depressive symptoms, tearfulness), anxiety, arthralgia.

For Healthcare Professionals

Applies to elagolix: oral tablet.

General

The more commonly reported adverse reactions have included hot flushes and night sweats, headache, nausea, insomnia, amenorrhea, anxiety, arthralgia, depression-related adverse reactions, and mood changes.^[Ref]

Psychiatric

During clinical trials, a 44-year old woman completed suicide 2 days after finishing a course of 150 mg once a day for 31 days. She was reported to have no relevant past medical history; life stressors were noted. Of the 2090 patients exposed to this drug, there were 4 reports of suicidal ideation, 3 had a history of depression.

Common (1% to 10%): Insomnia, mood altered, mood swings, depressed mood, depression, depressive symptoms and/or tearfulness, anxiety, decreased libido, irritability

Uncommon (0.1% to 1%): Completed suicide, suicidal ideation

Genitourinary

Dose-dependent reduction in mean number of bleeding and spotting days and bleeding intensity was reported in electronic diaries. Amenorrhea was reported in 6% to 17% of patients receiving 150 mg/day and 13% to 52% of those receiving 200 mg twice a day during the first 6 months of therapy. During the second 6 months the incidence of amenorrhea was 11% to 15% and 46% to 57%, respectively. Six months after stopping therapy (150 mg/day), menses resumed in 59%, 87%, and 95% of women within 1, 2, and 6 months, respectively. After stopping therapy following 6 months at 200 mg twice a day, resumption of menses was reported in 60%, 88%, and 97% of women within 1, 2, and 6 months, respectively.

Very common (10% or more): Amenorrhea (up to 57%)

Frequency not reported: Reduction in mean number of bleeding and spotting days and bleeding intensity

Hepatic

Common (1% to 10%): ALT elevations

Dose-dependent asymptomatic elevations of serum ALT to 3 times the upper limit normal occurred at 0.2% and 1.1% of patients receiving 150 mg/day (n=450) and 200 mg twice a day (n=443) respectively; placebo 0.1% (n=696).

Metabolic

During clinical trials, dose dependent increases in total cholesterol, low-density lipoprotein (LDL) cholesterol, high density lipoprotein (HDL) cholesterol, and serum triglycerides occurred. Mean changes of LDL at 6 months were 5 and 13 mg/dL in patients receiving 150 mg/day and 200 mg twice a day, respectively. Mean change in HDL was 2 and 4 mg/dL in patients receiving 150 mg/day and 200 mg twice a day, respectively. Mean change in serum triglycerides was less than 1 and 11 mg/dL in patients receiving 150 mg/day and 200 mg twice a day, respectively. Placebo patients had mean changes of -3, 1 and -3 mg/dL for LDL, HDL, and serum triglycerides, respectively. Increases occurred within 1 to 2 months and remained stable after that.

Common (1% to 10%): Increases in total cholesterol, low-density lipoprotein cholesterol, high density lipoprotein cholesterol, and serum triglycerides

Nervous system

Very common (10% or more): Headache (up to 20%)

Common (1% to 10%): Dizziness

Cardiovascular

Very common (10% or more): Hot flush or night sweats (up to 46%)

Gastrointestinal

Very common (10% or more): Nausea (up to 16%)

Common (1% to 10%): Abdominal pain, diarrhea, constipation

Uncommon (0.1% to 1%): Appendicitis

Hypersensitivity

Common (1% to 10%): Non-serious reactions including rash

Postmarketing reports: Hypersensitivity reactions including anaphylaxis, angioedema, and urticaria

Non-serious hypersensitivity reactions including rash occurred in 5.8% of patients (placebo=6.1%). Study discontinuation occurred in 0.4% of drug treated patients (placebo=0.5%).

Musculoskeletal

Common (1% to 10%): Arthralgia, weight gain, bone loss

Uncommon (0.1% to 1%): Back pain

During clinical trials, bone loss was assessed by dual-energy X-ray absorptiometry (DXA). One study showed the percent of subjects with greater than an 8% decrease in bone mineral density in lumbar spine, total hip, or femoral neck at any point compared to placebo was 2% and 7% in patients dosed with 150 mg/day and 200 mg twice a day, respectively (placebo: less than 1%). In the blinded extension study in which patients continued treatment for 12 months, these numbers increased to 8% and 21%. In study 2, the percent of subjects with greater than an 8% decrease in BMD was less than 1%, 6%, and 0% in patients dosed with 150 mg/day, 200 mg twice a day, and placebo, respectively. Continued bone loss occurred in the extension study with up to 2% observed in patients receiving 150 mg/day and 21% in patients receiving 200 mg twice a day. Upon completing drug therapy, partial recovery of BMD was observed in those patients who were followed.