Elagolix

ORILISSA is a GnRH receptor antagonist that inhibits endogenous GnRH signaling by binding competitively to GnRH receptors in the pituitary gland. Administration of ORILISSA 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.

• ORILISSA is indicated for the management of moderate to severe pain associated with endometriosis. Limitation s of Use: Limit the duration of use based on the dose and coexisting condition (see Table 1 ) [see D osage and Administration ( 2.1 ) and Warnings and Precautions ( 5.1 ) ] .ICD-10: N80.9

• ORILISSA is contraindicated in women: Who are pregnant [see Use in Specific Populations ( 8.1 )] . Exposure to ORILISSA early in pregnancy may increase the risk of early pregnancy loss.contraindicated

Normal liver function or mild hepatic impairment : 150 mg once daily for up to 24 months or 200 mg twice daily for up to 6 months. ( 2.1 ) Moderate hepatic impairment : 150 mg once daily for up to 6 months. ( 2.1 ) 2.1 Important Dosing Information Exclude pregnancy before starting ORILISSA or start ORILISSA within 7 days from the onset of menses. Take ORILISSA at approximately the same time each day, with or without food. Use the lowest effective dose, taking into account the severity of symptoms and treatment objectives [see Warnings and Precautions ( 5.1 , 5.3 , 5.4 ) and Clinical Studies ( 14 )] . Limit the duration of use because of bone loss ( Table 1 ) [see Warnings and Precautions ( 5.1 )] . Table 1. Recommended Dosage and Duration of Use Dosing Regimen Maximum Treatment Duration Coexisting Condition Initiate treatment with ORILISSA 150 mg once daily 24 months None Consider initiating treatment with ORILISSA 200 mg twice daily 6 months Dyspareunia Initiate treatment with ORILISSA 150 mg once daily. Use of 200 mg twice daily is not recommended. 6 months Moderate hepatic impairment (Child-Pugh Class B) 2.2 Hepatic Impairment No dosage adjustment of ORILISSA is required in women with mild hepatic impairment (Child-Pugh A). Compared to women with normal liver function, those with moderate hepatic impairment had approximately 3-fold higher elagolix exposures and those with severe hepatic impairment had approximately 7-fold higher elagolix exposures.

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 ( 5.1 ) Reduced Ability to Recognize Pregnancy : ORILISSA may alter menstrual bleeding, which may reduce the ability to recognize pregnancy. Perform testing if pregnancy is suspected. Discontinue if pregnancy is confirmed ( 5.2 ) 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 ( 5.3 ) Hepatic Transaminase Elevations : Dose-dependent elevations in serum alanine aminotransferase (ALT). Counsel patients on signs and symptoms of liver injury ( 5.4 ) Interactions with Hormonal Contraceptives : Use non-hormonal contraception during treatment and for 28 days after discontinuing ORILISSA. Coadministration of ORILISSA 200 mg twice daily with an estrogen-containing contraceptive is not recommended because of the potential for increased estrogen-associated risks. Coadministration of ORILISSA with an estrogen-containing contraceptive may reduce the efficacy of ORILISSA. Coadministration with progestin-containing oral contraceptives may reduce the efficacy of the contraceptive. ( 5.5 ) 5.1 Bone Loss ORILISSA causes a dose-dependent decrease in bone mineral density (BMD). BMD loss is greater with increasing duration of use and may not be completely reversible after stopping treatment [see Adverse Reactions ( 6.1 )] .

The following serious adverse reactions are discussed elsewhere in labeling: Bone loss [see Warnings and Precautions ( 5.1 )] Change in menstrual bleeding pattern and reduced ability to recognize pregnancy [see Warnings and Precautions ( 5.2 )] Suicidal ideation, suicidal behavior, and exacerbation of mood disorders [see Warnings and Precautions ( 5.3 )] Hepatic transaminase elevations [see Warnings and Precautions ( 5.4 )] Most common adverse reactions (>5%) in clinical trials included hot flushes and night sweats, headache, nausea, insomnia, amenorrhea, anxiety, arthralgia, depression-related adverse reactions and mood changes ( 6.1 ). To report SUSPECTED ADVERSE REACTIONS, contact AbbVie Inc. at 1-800-633-9110 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch Figure 1. Percent Change from Baseline in Lumbar Spine BMD in Subjects Who Received 12 Months of ORILISSA and Had Follow-up BMD 6 Months off Therapy in Studies EM-2/EM-4 Figure 2. Percent Change from Baseline in Lumbar Spine BMD in Subjects Who Received 12 Months of ORILISSA and Had Follow-up BMD 12 Months off Therapy in Studies EM-2/EM-4 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice.

8.1 Pregnancy Risk Summary Use of ORILISSA is contraindicated in pregnant women. Exposure to ORILISSA early in pregnancy may increase the risk of early pregnancy loss. Discontinue ORILISSA if pregnancy occurs during treatment. The limited human data with the use of ORILISSA in pregnant women are insufficient to determine whether there is a risk for major birth defects or miscarriage. Although two cases of congenital malformations were reported in clinical trials with ORILISSA, no pattern was identified and miscarriages were reported at a similar incidence across treatment groups (see Data ) . When pregnant rats and rabbits were orally dosed with elagolix during the period of organogenesis, postimplantation loss was observed in pregnant rats at doses 20 times the maximum recommended human dose (MRHD). Spontaneous abortion and total litter loss was observed in rabbits at doses 7 and 12 times the MRHD. There were no structural abnormalities in the fetuses at exposures up to 40 and 12 times the MRHD for the rat and rabbit, respectively (see Data ) . Data Human Data There were 49 pregnancies reported in clinical trials of more than 3,500 women (of whom more than 2,000 had endometriosis) treated with ORILISSA for up to 12 months. These pregnancies occurred while the women were receiving ORILISSA or within 30 days after stopping ORILISSA.

Metabolism

The pharmacokinetic properties of ORILISSA in healthy subjects are summarized in Table 8 . The steady state pharmacokinetic parameters under fasting conditions are summarized in Table 9 .

In case of overdose, monitor the patient for any signs or symptoms of adverse reactions and initiate appropriate symptomatic treatment, as needed.

• Jul 23, 2018NDANDA210450Abbvie
• May 29, 2020NDANDA213388Abbvie

1. 1Hot Flush50112%
2. 2Pain45311%
3. 3Nausea3768.8%
4. 4Headache3297.7%
5. 5Endometriosis3047.1%
6. 6Drug Ineffective2726.3%
7. 7Depression2325.4%
8. 8Arthralgia2054.8%
9. 9Anxiety1663.9%
10. 10Surgery1643.8%
11. 11Alopecia1633.8%
12. 12Fatigue1633.8%
13. 13Insomnia1543.6%
14. 14Suicidal Ideation1523.5%
15. 15Adverse Drug Reaction1473.4%

The 10 most recently updated of 39 ClinicalTrials.gov registrations naming Elagolix as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Study Of Oral Elagolix Tablets In Combination With Combined Oral Contraceptive Capsules/Tablets To Assess Dysmenorrhea Response In Adult Female Participants With Endometriosis And Associated Moderate To Severe Pain
  Active not recruiting · Phase 3 · Interventional · 800 enrolled · AbbVie
  NCT04333576updated 2026-06-12
• Pre-IVF Treatment With a GnRH Antagonist in Women With Endometriosis
  Completed · Phase 3 · Interventional · 103 enrolled · Yale University
  NCT04173169updated 2026-06-12
• Pre-IVF Treatment With a GnRH Antagonist in Women With endometriosis_temp
  Active not recruiting · Phase 3 · Interventional · 97 enrolled · Yale University
  NCT06375811updated 2026-06-05
• Comparison of Elagolix and OCPs in Reducing Endometriosis Associated Pelvic Pain
  Enrolling by invitation · Phase 4 · Interventional · 90 enrolled · Pak Emirates Military Hospital
  NCT07532876updated 2026-04-16
• Role of Menopause in Thermoregulation
  Recruiting · Phase 4 · Interventional · 24 enrolled · Penn State University
  NCT06798571updated 2026-04-06
• A Clinical Trial to Evaluate Efficacy and Safety of Elagolix Tablets in Women With Moderate or Severe Endometriosis-associated Pain
  Completed · Phase 3 · Interventional · 202 enrolled · Nanjing Chia-tai Tianqing Pharmaceutical
  NCT06076486updated 2025-09-23
• A Study to Evaluate Changes in Hair in Adult Participants Taking Oral Oriahnn Capsules With Heavy Menstrual Bleeding (HMB) Associated With Uterine Fibroids (UF)
  Withdrawn · Observational · 0 enrolled · AbbVie
  NCT06058728updated 2025-09-17
• A Study to Evaluate Pregnancy Outcomes in Females Treated With Oral Elagolix Tablets and Capsules
  Terminated · Observational · 173 enrolled · AbbVie
  NCT04464187updated 2025-09-15
• Long-Term Safety Study of Elagolix in Combination With Estradiol/Norethindrone Acetate for the Management of Heavy Menstrual Bleeding Associated With Uterine Fibroids in Premenopausal Women
  Completed · Phase 3 · Interventional · 478 enrolled · AbbVie
  NCT03271489updated 2025-07-22
• Brain Blood Flow Responses to Stress: Sex Differences
  Completed · Phase 4 · Interventional · 22 enrolled · University of Wisconsin, Madison
  NCT06253702updated 2025-07-18

CPIC-curated drug–gene pairs for Elagolix. Levels describe the strength of curated evidence and guideline status — never a recommendation to test or to adjust therapy.

• SLCO1B1CPIC B/C (provisional)FDA label: Informative PGx

Frequently asked questions

How does Elagolix work?

ORILISSA is a GnRH receptor antagonist that inhibits endogenous GnRH signaling by binding competitively to GnRH receptors in the pituitary gland. Administration of ORILISSA 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.

What is Elagolix used for?

According to FDA labeling, Elagolix carries indications including: ORILISSA is indicated for the management of moderate to severe pain associated with endometriosis. Limitation s of Use: Limit the duration of use based on the dose and coexisting condition (see Table 1 ) [see D osage and Administration ( 2.1 ) and Warnings and Precautions ( 5.1 ) ] .. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Elagolix?

Elagolix is classified as Anti-gonadotropin-releasing hormones, Gonadotropin Releasing Hormone Receptor Antagonist, Cytochrome P450 2C19 Inhibitors, Cytochrome P450 3A Inducers, Gonadotropin Releasing Hormone Receptor Antagonists, Organic Anion Transporting Polypeptide 1B1 Inhibitors, P-Glycoprotein Inhibitors, Decreased Follicle Stimulating Hormone Secretion, Decreased GnRH Activity, Decreased GnRH Secretion, Decreased Luteinizing Hormone Secretion.

What are the brand names for Elagolix?

Elagolix is marketed under brand names including Orilissa.

What are the contraindications for Elagolix?

Elagolix labeling lists contraindications including: ORILISSA is contraindicated in women: Who are pregnant [see Use in Specific Populations ( 8.1 )] . Exposure to ORILISSA early in pregnancy may increase the risk of early pregnancy loss.. Always consult the full prescribing information and a clinician.