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Relugolix: Drug information

Relugolix: Drug information
(For additional information see "Relugolix: Patient drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)
Brand Names: US
  • Orgovyx
Pharmacologic Category
  • Antineoplastic Agent, Gonadotropin-Releasing Hormone Antagonist;
  • Gonadotropin Releasing Hormone Antagonist
Dosing: Adult
Prostate cancer, advanced

Prostate cancer, advanced: Oral: Initial: 360 mg on day 1, followed by 120 mg once daily thereafter (Ref). Gonadotropin-releasing hormone receptor agonist or antagonist therapy is generally continued upon development of metastatic or nonmetastatic castration-resistant disease.

Missed dose: If a dose is missed, administer the missed dose as soon as possible. If the dose was missed by >12 hours, do not take the missed dose and resume with the next scheduled dose. If relugolix therapy is interrupted for >7 days, reinitiate therapy with a loading dose of 360 mg on day 1, followed by 120 mg once daily.

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Adult

CrCl 15 to 89 mL/minute: There are no dosage adjustments provided in the manufacturer's labeling; however, no clinically meaningful differences in relugolix pharmacokinetics were observed in mild to severe kidney impairment.

End-stage kidney disease (with or without hemodialysis): There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).

Dosing: Hepatic Impairment: Adult

Mild to moderate impairment (Child-Turcotte-Pugh class A, B): There are no dosage adjustments provided in the manufacturer's labeling; however, no clinically meaningful differences in relugolix pharmacokinetics were observed in mild to moderate hepatic impairment.

Severe impairment (Child-Turcotte-Pugh class C): There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).

Dosing: Adjustment for Toxicity: Adult

Hypersensitivity reactions, severe: Discontinue relugolix and manage as clinically indicated.

Dosing: Older Adult

Refer to adult dosing.

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Reported adverse reactions are for adults.

>10%:

Endocrine & metabolic: Hot flash (54%), increased serum glucose (44%), increased serum triglycerides (35%)

Gastrointestinal: Constipation (12%), diarrhea (12%, including colitis; grades 3/4: <1%)

Hematologic & oncologic: Decreased hemoglobin (28%; grades 3/4: <1%)

Hepatic: Increased serum alanine aminotransferase (27%), increased serum aspartate aminotransferase (18%)

Nervous system: Fatigue (26%; including asthenia)

Neuromuscular & skeletal: Musculoskeletal pain (30%)

1% to 10%:

Cardiovascular: Acute myocardial infarction (≤3%)

Dermatologic: Hyperhidrosis

Endocrine & metabolic: Decreased libido, gynecomastia, weight gain

Nervous system: Cerebrovascular accident (≤3%), depression, insomnia

<1%:

Cardiovascular: Cardiac arrhythmia (serious)

Genitourinary: Urinary tract infection (serious)

Hematologic & oncologic: Hemorrhage (serious)

Hypersensitivity: Angioedema

Renal: Acute kidney injury (serious)

Frequency not defined:

Cardiovascular: Atrioventricular block, heart failure

Endocrine & metabolic: Altered gonadal hormone levels (decreased)

Gastrointestinal: Abdominal pain

Respiratory: Pneumonia

Postmarketing: Hypersensitivity: Hypersensitivity reaction

Contraindications

Severe hypersensitivity to relugolix or any component of the formulation.

Warnings/Precautions

Concerns related to adverse effects:

• Hypersensitivity reactions: Hypersensitivity reactions (eg, severe angioedema, pharyngeal edema) have been reported.

• QT/QTc prolongation: Androgen deprivation therapy may prolong the QT/QTc interval. Consider risk versus benefit of androgen deprivation therapy in patients with congenital long QT syndrome, heart failure, frequent electrolyte abnormalities, and concomitant use of medications known to prolong QT interval. Correct electrolyte abnormalities prior to use.

Disease-related concerns:

• Cardiovascular disease: Androgen deprivation therapy may increase the risk for cardiovascular disease (Levine 2010).

• Diabetes: Androgen deprivation therapy may be associated with an increased risk for insulin resistance and diabetes (Keating 2006).

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Tablet, Oral:

Orgovyx: 120 mg

Generic Equivalent Available: US

No

Pricing: US

Tablets (Orgovyx Oral)

120 mg (per each): $107.28

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Administration: Adult

Oral: Administer at approximately the same time each day, with or without food. Swallow tablets whole; do not crush or chew.

Hazardous Drugs Handling Considerations

This medication is not on the NIOSH (2016) list; however, it may meet the criteria for a hazardous drug. Relugolix may cause reproductive toxicity, teratogenicity, and has a structural and/or toxicity profile similar to existing hazardous agents.

Use appropriate precautions for receiving, handling, storage, preparation, dispensing, transporting, administration, and disposal. Follow NIOSH and USP 800 recommendations and institution-specific policies/procedures for appropriate containment strategy (NIOSH 2016; USP-NF 2020).

Note: Facilities may perform risk assessment of some hazardous drugs to determine if appropriate for alternative handling and containment strategies (USP-NF 2020). Refer to institution-specific handling policies/procedures.

Use: Labeled Indications

Prostate cancer, advanced: Treatment of advanced prostate cancer.

Metabolism/Transport Effects

Substrate of CYP2C8 (minor), CYP3A4 (minor), P-glycoprotein/ABCB1 (major); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.

Asciminib: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor therapy

Elacestrant: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor therapy

Erdafitinib: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Management: If coadministration with these narrow therapeutic index/sensitive P-gp substrates is unavoidable, separate erdafitinib administration by at least 6 hours before or after administration of these P-gp substrates. Risk D: Consider therapy modification

Flotufolastat F18: Androgen Deprivation Therapy Agents may diminish the diagnostic effect of Flotufolastat F18. Management: Androgen deprivation therapy (ADT) may result in changes in the uptake of flotufolastat F18 in prostate cancer. The impact of ADT on the performance of flotufolastat F18 is unknown, but use of alternative agents should be considered. Risk D: Consider therapy modification

Futibatinib: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor therapy

Gallium Ga 68 PSMA-11: Androgen Deprivation Therapy Agents may diminish the therapeutic effect of Gallium Ga 68 PSMA-11. Management: Androgen deprivation therapy (ADT) may result in changes in the uptake of gallium Ga 68 PSMA-11 (gozetotide) in prostate cancer. The impact of ADT on the performance of gallium Ga 68 PSMA-11 is unknown, but use of alternative agents should be considered. Risk D: Consider therapy modification

Gilteritinib: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor therapy

Haloperidol: QT-prolonging Agents (Indeterminate Risk - Caution) may enhance the QTc-prolonging effect of Haloperidol. Risk C: Monitor therapy

Indium 111 Capromab Pendetide: Antigonadotropic Agents may diminish the diagnostic effect of Indium 111 Capromab Pendetide. Risk X: Avoid combination

Inducers of CYP3A4 (Moderate) and P-glycoprotein: May decrease the serum concentration of Relugolix. Risk C: Monitor therapy

Inducers of CYP3A4 (Strong) and P-glycoprotein: May decrease the serum concentration of Relugolix. Management: Avoid use of relugolix with drugs that are both strong CYP3A4 and P-glycoprotein (P-gp) inducer. If combined, increase the dose of relugolix to 240 mg once daily. Reduce back to 120 mg daily once the combined inducer is discontinued. Risk D: Consider therapy modification

Lasmiditan: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk X: Avoid combination

Lumacaftor and Ivacaftor: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates (High risk with Inhibitors or Inducers). Lumacaftor and Ivacaftor may decrease the serum concentration of P-glycoprotein/ABCB1 Substrates (High risk with Inhibitors or Inducers). Risk C: Monitor therapy

Mitapivat: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor therapy

Pacritinib: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk X: Avoid combination

P-glycoprotein/ABCB1 Inhibitors: May increase the serum concentration of Relugolix. Management: Avoid coadministration of relugolix with oral P-gp inhibitors whenever possible. If combined, take relugolix at least 6 hours prior to the P-gp inhibitor and monitor patients more frequently for adverse reactions. Risk D: Consider therapy modification

Piflufolastat F18: Androgen Deprivation Therapy Agents may diminish the diagnostic effect of Piflufolastat F18. Management: Androgen deprivation therapy (ADT) may result in changes in the uptake of piflufolastat F18 in prostate cancer. The impact of ADT on the performance of piflufolastat F18 is unknown, but use of alternative agents should be considered. Risk D: Consider therapy modification

Pretomanid: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor therapy

QT-prolonging Agents (Highest Risk): QT-prolonging Agents (Indeterminate Risk - Caution) may enhance the QTc-prolonging effect of QT-prolonging Agents (Highest Risk). Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk C: Monitor therapy

Sotorasib: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Management: Consider avoiding use of sotorasib and narrow therapeutic index/sensitive P-gp substrates. If combined use is unavoidable, monitor for increased toxicities of the substrate and consider a decrease in the substrate dosage. Risk D: Consider therapy modification

Sparsentan: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk X: Avoid combination

Taurursodiol: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk X: Avoid combination

Reproductive Considerations

Patients with partners who could become pregnant should use effective contraception during therapy and for 2 weeks after the last dose of relugolix. Based on the mechanism of action, male fertility may be impaired.

Pregnancy Considerations

Based on the mechanism of action and data from animal reproduction studies, in utero exposure to relugolix may cause fetal harm and loss of pregnancy.

Breastfeeding Considerations

It is unknown if relugolix is present in breast milk.

Monitoring Parameters

Prostate-specific antigen at baseline and periodically; serum testosterone levels (if clinically necessary). Consider periodic monitoring of ECGs and electrolytes. Monitor adherence.

Cardiovascular monitoring for patients with prostate cancer: Comprehensive assessment prior to treatment including a history and physical examination, screening for cardiovascular disease risk factors such as hypertension, diabetes, dyslipidemia, obesity, and smoking; baseline and serial ECGs are recommended in patients at risk of QTc prolongation during androgen deprivation therapy (ADT); estimate 10-year cardiovascular disease risk in patients without cardiovascular disease at baseline; assess cardiovascular risk annually during ADT (ASCO [Armenian 2017]; ESC [Lyon 2022]).

Mechanism of Action

Relugolix is a nonpeptide gonadotropin-releasing hormone (GnRH) antagonist that competitively binds to pituitary GnRH receptors, blocking the receptor and decreasing secretion of luteinizing hormone and follicle stimulation hormone, resulting in decreased testosterone levels.

Pharmacokinetics (Adult Data Unless Noted)

Onset: Testosterone concentrations at castrate levels (<50 ng/dL) were observed by day 4 in over half of patients; almost all maintained castrate testosterone levels through 48 weeks.

Protein binding: 68% to 71% (primarily to albumin, lesser extent to α1-acid glycoprotein).

Metabolism: Primarily hepatic via CYP3A and to a lesser extent by CYP2C8.

Bioavailability: ~12%.

Half-life elimination: Mean effective half-life: 25 hours; Mean terminal elimination half-life: ~61 hours.

Time to peak: 2.25 hours (range: 0.5 to 5 hours).

Excretion: Feces: ~81% (4.2% unchanged); Urine: ~4% (2.2% unchanged).

Clearance: Mean: 29.4 L/hour; renal: 8 L/hour.

Brand Names: International
International Brand Names by Country
For country code abbreviations (show table)

  • (AR) Argentina: Orgovyx;
  • (AT) Austria: Orgovyx;
  • (CZ) Czech Republic: Orgovyx;
  • (DE) Germany: Orgovyx;
  • (IE) Ireland: Orgovyx;
  • (JP) Japan: Relumina;
  • (PR) Puerto Rico: Orgovyx
  1. <800> Hazardous Drugs—Handling in Healthcare Settings. United States Pharmacopeia and National Formulary (USP 43-NF 38). Rockville, MD: United States Pharmacopeia Convention; 2020:74-92.
  2. Armenian SH, Lacchetti C, Barac A, et al. Prevention and monitoring of cardiac dysfunction in survivors of adult cancers: American Society of Clinical Oncology clinical practice guideline. J Clin Oncol. 2017;35(8):893-911. doi:10.1200/JCO.2016.70.5400 [PubMed 27918725]
  3. Keating NL, O'Malley AJ, Smith MR. Diabetes and cardiovascular disease during androgen deprivation therapy for prostate cancer. J Clin Oncol. 2006;24(27):4448-4456. doi:10.1200/JCO.2006.06.2497 [PubMed 16983113]
  4. Levine GN, D’Amico AV, Berger P, et al; American Heart Association Council on Clinical Cardiology and Council on Epidemiology and Prevention, the American Cancer Society, and the American Urological Association. Androgen-deprivation therapy in prostate cancer and cardiovascular risk. A science advisory from the American Heart Association, American Cancer Society, and American Urological Association: endorsed by the American Society for Radiation Oncology. Circulation. 2010;121(6):833-840. doi:10.1161/CIRCULATIONAHA.109.192695 [PubMed 20124128]
  5. Lyon AR, López-Fernández T, Couch LS, et al; ESC Scientific Document Group. 2022 ESC guidelines on cardio-oncology developed in collaboration with the European Hematology Association (EHA), the European Society for Therapeutic Radiology and Oncology (ESTRO) and the International Cardio-Oncology Society (IC-OS). Eur Heart J. 2022;43(41):4229-4361. doi:10.1093/eurheartj/ehac244 [PubMed 36017568]
  6. Orgovyx (relugolix) [prescribing information]. Brisbane, CA: Myovant Sciences Inc; August 2023.
  7. Shore ND, Saad F, Cookson MS, et al; HERO Study Investigators. Oral relugolix for androgen-deprivation therapy in advanced prostate cancer. N Engl J Med. 2020;382(23):2187-2196. doi:10.1056/NEJMoa2004325 [PubMed 32469183]
  8. US Department of Health and Human Services; Centers for Disease Control and Prevention; National Institute for Occupational Safety and Health. NIOSH list of antineoplastic and other hazardous drugs in healthcare settings 2016. https://www.cdc.gov/niosh/docs/2016-161/. Updated September 2016. Accessed December 22, 2020.
Topic 130388 Version 52.0

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