Orgovyx
(relugolix)Dosage & Administration
Orgovyx Prescribing Information
ORGOVYX is indicated for the treatment of adult patients with advanced prostate cancer.
Recommended Dosage
Initiate treatment of ORGOVYX with a loading dose of 360 mg on the first day and continue treatment with a 120 mg dose taken orally once daily at approximately the same time each day.
ORGOVYX can be taken with or without food [see Clinical Pharmacology (12.3)] . Instruct patients to swallow tablets whole and not to crush or chew tablets.
Advise patients to take a missed dose of ORGOVYX as soon as they remember. If the dose was missed by more than 12 hours, patients should not take the missed dose and resume with the next scheduled dose.
If treatment with ORGOVYX is interrupted for greater than 7 days, restart ORGOVYX with a loading dose of 360 mg on the first day, and continue with a dose of 120 mg once daily.
In patients treated with GnRH receptor agonists and antagonists for prostate cancer, treatment is usually continued upon development of nonmetastatic or metastatic castration-resistant prostate cancer.
Dose Modification for Use with P-gp Inhibitors
Avoid co-administration of ORGOVYX with oral P-gp inhibitors. If co-administration is unavoidable, take ORGOVYX first and separate dosing by at least 6 hours [see Drug Interactions (7.1)and Clinical Pharmacology (12.3)] . Treatment with ORGOVYX may be interrupted for up to two weeks if a short course of treatment with a P-gp inhibitor is required.
Dose Modification for Use with Combined P-gp and Strong CYP3A Inducers
Avoid co-administration of ORGOVYX with combined P-gp and strong CYP3A inducers. If co-administration is unavoidable, increase the ORGOVYX dose to 240 mg once daily. After discontinuation of the combined P-gp and strong CYP3A inducer, resume the recommended ORGOVYX dose of 120 mg once daily [see Drug Interactions (7.1)and Clinical Pharmacology (12.3)] .
Tablets: 120 mg, light red, almond-shaped, film-coated, and debossed with "R" on one side and "120" on the other side.
Pregnancy
Risk Summary
The safety and efficacy of ORGOVYX have not been established in females.
Based on findings in animals and mechanism of action, ORGOVYX can cause fetal harm and loss of pregnancy when administered to a pregnant female [see Clinical Pharmacology (12.1)] . There are no human data on the use of ORGOVYX in pregnant females to inform the drug-associated risk. In an animal reproduction study, oral administration of relugolix to pregnant rabbits during organogenesis caused embryo-fetal lethality at maternal exposures that were 0.3 times the human exposure at the recommended dose of 120 mg daily based on AUC ( see Data). Advise patients of the potential risk to the fetus.
Data
Animal Data
In an embryo-fetal development study, oral administration of relugolix to pregnant rabbits during the period of organogenesis resulted in abortion, total litter loss, or decreased number of live fetuses at a dose of 9 mg/kg/day (approximately 0.3 times the human exposure at the recommended dose of 120 mg daily based on AUC).
Lactation
Risk Summary
The safety and efficacy of ORGOVYX at the recommended dose of 120 mg daily have not been established in females. There are no data on the presence of relugolix in human milk, the effects on the breastfed child, or the effects on milk production. Relugolix and/or its metabolites were present in milk of lactating rats (see Data) .
Data
Animal Data
In lactating rats administered a single oral dose of 30 mg/kg radiolabeled relugolix on post-partum day 14, relugolix and/or its metabolites were present in milk at concentrations up to 10-fold higher than in plasma at 2 hours post-dose.
Females and Males of Reproductive Potential
Contraception
Males
Based on findings in animals and mechanism of action, advise male patients with female partners of reproductive potential to use effective contraception during treatment and for 2 weeks after the last dose of ORGOVYX [see Use in Specific Populations (8.1)].
Infertility
Males
Based on findings in animals and mechanism of action, ORGOVYX may impair fertility in males of reproductive potential [see Clinical Pharmacology (12.1)and Nonclinical Toxicology (13.1)].
Pediatric Use
The safety and efficacy of ORGOVYX in pediatric patients have not been established.
Geriatric Use
Of the 622 patients who received ORGOVYX in the HERO study, 81% were 65 years of age or older, while 35% were 75 years of age or older. No overall differences in safety or effectiveness were observed between these subjects and younger subjects. There was no clinically relevant impact of age on the pharmacokinetics of ORGOVYX or testosterone response based on population pharmacokinetic and pharmacokinetic/pharmacodynamic analyses in men 45 to 91 years of age.
ORGOVYX is contraindicated in patients with severe hypersensitivity to relugolix or to any of the product components.
QT/QTc Interval Prolongation
Androgen deprivation therapy, such as ORGOVYX may prolong the QT/QTc interval. Providers should consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients with congenital long QT syndrome, congestive heart failure, or frequent electrolyte abnormalities and in patients taking drugs known to prolong the QT interval. Electrolyte abnormalities should be corrected. Consider periodic monitoring of electrocardiograms and electrolytes [see Clinical Pharmacology (12.2)].
Hypersensitivity Reactions
ORGOVYX is contraindicated in patients with severe hypersensitivity to relugolix or any of the product components [see Contraindications (4)] . Hypersensitivity reactions, including pharyngeal edema and other serious cases of angioedema, have been reported in postmarketing in patients treated with ORGOVYX.
In the HERO study, patients treated with relugolix reported angioedema (0.2%) [see Clinical Trials Experience (6.1)] .
Advise patients who experience any symptoms of hypersensitivity to temporarily discontinue ORGOVYX and promptly seek medical care.
Discontinue ORGOVYX for severe hypersensitivity reactions and manage as clinically indicated.
Embryo-Fetal Toxicity
The safety and efficacy of ORGOVYX have not been established in females. Based on findings in animals and mechanism of action, ORGOVYX can cause fetal harm and loss of pregnancy when administered to a pregnant female. In an animal reproduction study, oral administration of relugolix to pregnant rabbits during the period of organogenesis caused embryo-fetal lethality at maternal exposures that were 0.3 times the human exposure at the recommended dose of 120 mg daily based on area under the curve (AUC). Advise males with female partners of reproductive potential to use effective contraception during treatment and for 2 weeks after the last dose of ORGOVYX [see Use in Specific Populations (8.1, 8.3)and Clinical Pharmacology (12.1)] .
Laboratory Testing
Therapy with ORGOVYX results in suppression of the pituitary gonadal system. Results of diagnostic tests of the pituitary gonadotropic and gonadal functions conducted during and after ORGOVYX may be affected. The therapeutic effect of ORGOVYX should be monitored by measuring serum concentrations of prostate specific antigen (PSA) periodically. If PSA increases, serum concentrations of testosterone should be measured.