elagolix (Rx)

Brand and Other Names:Orilissa
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Dosing & Uses


Dosage Forms & Strengths


  • 150mg
  • 200mg


Indicated for management of moderate-to-severe pain

Initiate with 150 mg PO qDay for up to 24 months

Coexisting conditions

  • Dyspareunia: Consider initiating with 200 mg BID for up to 6 months
  • Moderate hepatic impairment (Child-Pugh B): Initiate with 150 mg qDay for up to 6 months; 200 mg BID is not recommended

Dosage Modifications

Renal impairment

  • No dosage adjustment required with any degree of renal impairment or end-stage renal disease (including dialysis)

Hepatic impairment

  • Mild (Child-Pugh A): No dosage adjustment required
  • Moderate (Child-Pugh B): Only the 150-mg qDay regimen is recommended for women with moderate hepatic impairment, and the duration of treatment should be limited to 6 months
  • Severe (Child-Pugh C): Contraindicated

Dosing Considerations

Exclude pregnancy before initiating, or start elagolix within 7 days from the onset of menses

Use the lowest effective dose, taking into account the severity of symptoms and treatment objectives

Limit the duration of use because of bone loss

Safety and efficacy not established



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            Adverse Effects


            Hot flush or night sweats (24-46%)

            Headache (17-20%)

            Nausea (11-16%)


            Insomnia (6-9%)

            Mood altered, mood swings (5-6%)

            Amenorrhea (4-7%)

            Depressed mood, depression, depressive symptoms and/or tearfulness (3-6%)

            Hypersensitivity reactions (5.8%)

            Anxiety (3-5%)

            Arthralgia (3-5%)

            ≥3% to <5%

            • Decreased libido
            • Diarrhea
            • Abdominal pain
            • Weight gain
            • Dizziness
            • Constipation
            • Irritability





            Known osteoporosis

            Severe hepatic impairment

            Coadministration of strong organic anion transporting polypeptide (OATP) 1B1 inhibitors (eg, cyclosporine and gemfibrozil)


            May reduce the amount, intensity, or duration of menstrual bleeding, which may decrease the ability to recognize the occurrence of a pregnancy in a timely manner; perform pregnancy testing if pregnancy is suspected, and discontinue drug if pregnancy confirmed

            Dose-dependent elevations of ALT ≥3x ULN occurred with elagolix; use the lowest effective dose and instruct patients to promptly seek medical attention in case of symptoms or signs that may reflect liver injury

            Suicidal behavior and mood disorders

            • Suicidal ideation and behavior, including 1 completed suicide, occurred in subjects treated with elagolix in the endometriosis clinical trials
            • Patients taking elagolix had a higher incidence of depression and mood changes compared with placebo
            • Patients with a history of suicidality or depression had a higher incidence of depression compared with subjects without such a history
            • Promptly evaluate patients with depressive symptoms to determine whether the risks of continued therapy outweigh the benefits
            • Patients with new or worsening depression, anxiety, or other mood changes should be referred to a mental health professional, as appropriate
            • Advise patients to seek immediate medical attention for suicidal ideation and behavior
            • Reevaluate the benefits and risks of continuing elagolix if such events occur

            Bone mineral density

            • Dose-dependent decrease in bone mineral density (BMD) reported
            • BMD loss is greater with increasing duration of use and may not be completely reversible after stopping treatment
            • The impact of these BMD decreases on long-term bone health and future fracture risk are unknown
            • Consider assessing BMD with a history of a low-trauma fracture or other risk factors for osteoporosis or bone loss, and do not use in women with known osteoporosis
            • Limit the duration of use to reduce the extent of bone loss

            Drug interaction overview

            • Also see Contraindications
            • OATP1B1 inhibitors
              • Coadministration with drugs that inhibit OATP1B1 may increase elagolix plasma concentrations
              • Concomitant use with strong OATP1B1 inhibitors (eg, cyclosporine, gemfibrozil) is contraindicated
            • CYP3A inhibitors and inducers
              • Elagolix is a CYP3A substrate
              • Coadministration of elagolix 200 mg BID with strong CYP3A inhibitors for >1 month is not recommended; limit coadministration of elagolix 150 mg qDay and strong CYP3A inhibitors to 6 months
              • Coadministration with drugs that induce CYP3A may decrease elagolix plasma concentrations
            • P-gp inhibitors and inducers
              • The effect of concomitant use of P-gp inhibitors or inducers on the pharmacokinetics of elagolix is unknown
            • Estrogen-containing contraceptive
              • Based on elagolix’s mechanism of action, estrogen-containing contraceptives are expected to reduce elagolix efficacy
              • The effect of progestin-only contraceptives on elagolix efficacy is unknown
              • Advise women to use nonhormonal contraceptives during treatment and for 28 days after discontinuing elagolix
              • Increases estrogen exposure and associated risks when 200 mg twice daily dose taken with combined hormonal contraceptives
              • Dose of 200 mg twice daily co-administered with a combined oral contraceptive (COC) containing ethinyl estradiol may lead to increased risk of ethinyl estradiol-related adverse events including thromboembolic disorders and vascular events; not recommended
            • Effect of elagolix on other drugs
              • Elagolix is a weak-to-moderate CYP3A inducer; coadministration may decrease plasma concentration of CYP3A substrates
              • Elagolix inhibits efflux transporter P-glycoprotein (P-gp); coadministration may increase plasma concentration of P-gp substrates (eg, digoxin)
              • Elagolix is a weak inhibitor of CYP2C19; coadministration may increase plasma concentrations of CYP2C19 substrates (eg, omeprazole)



            Contraindicated in pregnant women

            May delay ability to recognize occurrence of pregnancy as it may reduce intensity, duration, and amount of menstrual bleeding

            Drug exposure early in pregnancy may increase the risk of early pregnancy loss

            Discontinue elagolix if pregnancy occurs during treatment

            There is a pregnancy registry that monitors outcomes in women who become pregnant while treated with elagolix; enroll by calling 1-833-782-7241

            The limited human data with use in pregnant women are insufficient in determining whether there is a risk for major birth defects or miscarriage; although 2 cases of congenital malformations were reported in clinical trials with elagolix, no pattern was identified and miscarriages were reported at a similar incidence across treatment groups

            Animal 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

            Pregnancy testing

            • Exclude pregnancy before initiating treatment
            • Perform pregnancy testing if pregnancy is suspected during treatment


            • Advise women to use effective non-hormonal contraceptives during treatment and for 28 days after discontinuing therapy


            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

            There are no adequate animal data on the excretion of elagolix in milk

            The developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for elagolix and any potential adverse effects on the breastfed child from elagolix

            Pregnancy Categories

            A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA: Information not available.



            Mechanism of Action

            Oral gonadotropin-releasing hormone (GnRH) receptor antagonist; 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


            Peak plasma time: 1 hr

            Peak plasma concentration: 574 ng/mL (150-mg dose); 774 ng/mL (200-mg dose)

            AUC: 1292 ng·hr/mL (150-mg dose); 1725 ng·hr/mL (200-mg dose)

            Effect of high-fat meal (relative to fasting): AUC decreases by 24%; peak plasma concentration decreases by 36%


            Vd (steady-state): 1674 L (150-mg dose); 881 L (200-mg dose)

            Protein binding: 80%

            Blood-to-plasma ratio: 0.6


            Hepatically metabolized by CYP3A4 (major)

            Minor pathways include: CYP2D6, CYP2C8, and uridine glucuronosyl transferases (UGTs)


            Half-life: 4-6 hr

            Oral clearance: 123 L/hr (150-mg dose); 144 L/hr (200-mg dose)

            Excretion: Urine (<3%); feces (90%)


            Disposition of elagolix involves the OATP1B1 transporter protein

            Higher plasma concentrations of elagolix observed in individuals who have 2 reduced function alleles of the gene that encodes OATP1B1 (SLCO1B1 521T>C)

            The frequency of this SLCO1B1 521 C/C genotype is generally <5% in most racial/ethnic groups

            Individuals with this genotype are expected to have a 78% mean increase in elagolix concentrations compared with individuals with normal transporter function (ie, SLCO1B1 521T/T genotype)



            Oral Administration

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

            Missed dose

            • Administer missed dose on the same day as soon as possible and then resume the regular dosing schedule
            • 150 mg qDay: Take no more than 1 tablet each day
            • 200 mg BID: Take no more than 2 tablets each day


            Store at 2-30°C (36-86°F)





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            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
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