relugolix (Rx)

Brand and Other Names:Orgovyx
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 120mg

Prostate Cancer

Indicated for advanced prostate cancer

Day 1 loading dose: 360 mg PO

Maintenance dose: 120 mg PO qDay

Dosage Modifications

Renal impairment

  • Mild-to-severe (CrCl 15-89 mL/min): No dosage adjustment required
  • End-stage renal disease with or without hemodialysis: Not studied

Hepatic impairment

  • Mild-to-moderate (Child-Pugh A or B): No dosage adjustment required
  • Severe (Child-Pugh C): Not studied

P-gp inhibitors

  • Avoid coadministration; if unable to avoid, take relugolix first and separate dosing by at least 6 hr
  • May briefly interrupt relugolix treatment for up to 2 weeks if a short course of treatment with a P-gp inhibitor is required
  • If treatment interrupted for >7 days, resume relugolix with 360 mg loading dose on the first day, followed by 120 mg/day

Combined P-gp and strong CYP3A inducers

  • Avoid coadministration; if unable to avoid, increase relugolix dose to 240 mg qDay; resume 120 mg qDay after discontinuing the strong P-gp/CYP3A inducer

Dosing Considerations

Correct electrolyte abnormalities

Consider periodic ECG and electrolyte monitoring

Males with female partners of reproductive potential should use effective contraception

Not indicated

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Interactions

Interaction Checker

and relugolix

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            All grades

            • Hot flush (54%)
            • Glucose increased (44%)
            • Triglycerides increased (35%)
            • Musculoskeletal pain (30%)
            • Hemoglobin decreased (28%)
            • ALT increased (27%)
            • Fatigue (26%)
            • AST increased (18%)
            • Diarrhea (12%)
            • Constipation (12%)

            1-10%

            All grades

            • Increased weight (<10%)
            • Insomnia (<10%)
            • Gynecomastia (<10%)
            • Hyperhidrosis (<10%)
            • Depression (<10%)
            • Decreased libido (<10%)

            Grade 3-4

            • Glucose increased (2.9%)
            • Triglycerides increased (2%)
            • Musculoskeletal pain (1.1%)

            <1%

            Grade 3-4

            • Hot flush
            • Fatigue
            • Diarrhea
            • ALT increased
            • Hemoglobin increased
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            Warnings

            Contraindications

            None

            Cautions

            Based animal studies and mechanism of action, fetal harm may occur

            Therapy suppresses pituitary gonadal system; results of diagnostic tests conducted during and after treatment may be affected; monitor therapeutic effect of relugolix by measuring serum concentrations of prostate specific antigen (PSA) periodically; if PSA increases, measure serum testosterone concentrations

            QT/QTc interval prolongation

            • Androgen deprivation therapy may prolong QT/QTc interval
            • Consider benefits and risks in patients with congenital long QT syndrome, congestive heart failure, or frequent electrolyte abnormalities, and those taking drugs known to prolong QT interval
            • Correct electrolyte abnormalities
            • Consider periodic ECG and electrolyte monitoring

            Drug interaction overview

            • CYP enzymes: Substrate of CYP3A (primarily) and CYP2C8 (minor)
            • Transporter systems: Substrate of P-gp; inhibitor of BCRP and P-gp
            • P-gp inhibitors
              • Avoid coadministration
              • Coadministration increases relugolix AUC and peak plasma concentration; if unable to avoid, adjust time between dosing relugolix and the P-gp inhibitor
            • Combined P-gp and strong CYP3A inducers
              • Avoid coadministration
              • Coadministration decreases relugolix AUC and peak plasma concentration; if unable to avoid, adjust relugolix dose
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            Pregnancy & Lactation

            Pregnancy

            Based on findings in animals and mechanism of action, can cause fetal harm and loss of pregnancy when administered to pregnant females

            Human data are unavailable

            Animal studies

            • Administration to pregnant rabbits during organogenesis caused embryofetal lethality at maternal exposures that were 0.3 times the human exposure at the recommended dose of 120 mg daily based on AUC

            Contraception

            • Males with female partners of reproductive potential: Use effective contraception during treatment and for 2 weeks after last dose

            Infertility

            • Based on findings in animals and mechanism of action, may impair fertility in males of reproductive potential

            Lactation

            Data are unavailable on presence in human milk, effects on breastfed children, or effects on milk production

            Relugolix and/or its metabolites were present in milk of lactating rats at concentrations up to 10-fold higher than in plasma at 2 hr post dose

            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.

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            Pharmacology

            Mechanism of Action

            Gonadotropin-releasing hormone (GnRH) receptor antagonist; binds to and blocks GnRH receptors in the anterior pituitary gland

            Blocking GnRH receptors decreases the release of gonadotropins (ie, luteinizing hormone, follicle stimulating hormone), thereby decreasing the downstream production of testosterone by the testes in men

            Absorption

            Absolute bioavailability: ~12%

            Peak plasma time: 2.25 hr

            Peak plasma concentration

            • 360 mg: 215 ng/mL
            • 120 mg: 70 ng/mL

            AUC

            • 360 mg: 985 nghr/mL
            • 120 mg: 407 nghr/mL

            Distribution

            Protein bound: 68-71%; albumin (primarily), alpha1-acid glycoprotein (less extent)

            Blood/plasma ratio: 0.78

            Metabolism

            Metabolized primarily by CYP3A and to lesser extent by CYP2C8 in vitro

            Elimination

            Half-life: 25 hr; terminal half-life 60.8 hr

            Total clearance: 29.4 L/hr

            Renal clearance: 8 L/hr

            Excretion: Feces (81%; 4.2 unchanged); urine (4.1%; 2.2 unchanged)

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            Administration

            Oral Administration

            Take at approximately the same time each day

            May take with or without food

            Swallow tablets whole; do not crush or chew

            Patients treated with GnRH receptor agonists and antagonists for prostate cancer is usually continued upon development of nonmetastatic or metastatic castration-resistant prostate cancer

            Missed dose

            • Take missed dose as soon as remembered
            • Dose missed by >12 hours: Do not take missed dose; resume with next scheduled dose
            • Treatment interrupted for >7 days: Restart with 360-mg loading dose on first day, and then continue 120 mg qDay

            Storage

            Store at room temperature; not to exceed 30ºC (86ºF)

            Dispense in original container only

            For bottles, keep container tightly closed after first opening

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            Formulary

            FormularyPatient Discounts

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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            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
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
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            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
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            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.