Orgovyx (relugolix)

Orgovyx may cause serious side effects, including:

• Changes in the electrical activity of your heart (QT prolongation). Your healthcare provider may check your body salts (electrolytes) and the electrical activity of your heart during treatment with Orgovyx. Tell your healthcare provider right away if you get any signs or symptoms of QT prolongation, including:
  • dizziness
  • fainting
  • feeling that your heart is pounding or racing (palpitations)
  • chest pain

The most common side effects of Orgovyx include:

• hot flashes
• increased blood sugar levels
• increased blood fat (triglyceride) levels
• muscle and joint pain
• decreased blood hemoglobin levels
• increased liver enzymes
• tiredness
• constipation
• diarrhea

Other side effects include weight gain, decreased sex drive, and erectile function problems.

Orgovyx may cause fertility problems in males, which may affect your ability to father children. Talk to your healthcare provider if this is a concern for you.

These are not all the possible side effects of Orgovyx.

Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

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. 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.
• 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.

Effect Of Other Drugs On Orgovyx

P-gp Inhibitors

• Co-administration of Orgovyx with a P-gp inhibitor increases the AUC and the maximum concentration (Cmax) of relugolix, which may increase the risk of adverse reactions associated with Orgovyx. Avoid co-administration of Orgovyx with oral P-gp inhibitors.
• If co-administration is unavoidable, take Orgovyx first, separate dosing by at least 6 hours, and monitor patients more frequently for adverse reactions.
• Treatment with Orgovyx may be interrupted for up to 2 weeks for a short course of treatment with certain P-gp inhibitors.
• If treatment with Orgovyx is interrupted for more than 7 days, resume administration of Orgovyx with a 360 mg loading dose on the first day, followed by 120 mg once daily.

Combined P-gp And Strong CYP3A Inducers

• Co-administration of Orgovyx with a combined P-gp and a strong CYP3A inducer decreases the AUC and Cmax of relugolix, which may reduce the effects of Orgovyx. Avoid co-administration of Orgovyx with combined P-gp and strong CYP3A inducers.
• If co-administration is unavoidable, increase the Orgovyx dose. After discontinuation of the combined P-gp and strong CYP3A inducer, resume the recommended dose of Orgovyx once daily.

• 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.
• There are no human data on the use of Orgovyx in pregnant females to inform the drug-associated risk.
• 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.