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

            All Interactions Sort By:
             activity indicator 

            Contraindicated (0)

              Serious - Use Alternative (0)

                Monitor Closely (1)

                • gallium Ga 68 PSMA-11

                  relugolix will decrease the level or effect of gallium Ga 68 PSMA-11 by unspecified interaction mechanism. Modify Therapy/Monitor Closely. Androgen deprivation therapy and other therapies targeting the androgen pathway may result in changes in the uptake of gallium Ga 68 PSMA-11 in prostate cancer. The effect of ADT on the performance of gallium Ga 68 PSMA-11 is unknown.

                Minor (0)

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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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                  Images

                  No images available for this drug.
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                  Patient Handout

                  A Patient Handout is not currently available for this monograph.
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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.
                  QL Quantity Limits
                  Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
                  ST Step Therapy
                  Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
                  OR Other Restrictions
                  Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each 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.