Relugolix (Orgovyx) is an oral gonadotropin-releasing hormone (GnRH) receptor antagonist indicated for the treatment of adult patients with advanced prostate cancer. As a novel endocrine therapy, its unique pharmacological mechanism and administration regimen provide additional options for clinical treatment.

Dosage and Administration, Recommended Dosage of Relugolix (Orgovyx)

Standard Dosage Regimen

A loading dose of 360 mg is required on the first day of treatment, followed by a daily oral dose of 120 mg. It is recommended to take the medication at a fixed time each day to maintain stable blood concentrations.

Tablets should be swallowed whole; do not chew or crush.

If a patient misses a dose by less than 12 hours, take the missed dose immediately.

If more than 12 hours have passed since the missed dose, skip the missed dose and continue with the next scheduled dose as planned.

If treatment is interrupted for more than 7 days, restart with a loading dose of 360 mg, followed by the resumption of the maintenance dose of 120 mg daily.

Administration Precautions

Studies have shown that relugolix absorption is not affected by food, so it can be taken with meals or on an empty stomach.

This is particularly convenient for elderly patients requiring long-term medication, improving treatment adherence.

Dosage Adjustments for Relugolix (Orgovyx)

Interaction with P-gp Inhibitors

Relugolix is a P-gp substrate. Concomitant use of oral P-gp inhibitors (e.g., certain antiarrhythmic drugs) may increase its blood concentration, thereby raising the risk of adverse reactions.

If concurrent use is unavoidable:

Administer relugolix first, followed by the P-gp inhibitor with an interval of at least 6 hours.

Enhance monitoring for adverse reactions.

For short-term use of P-gp inhibitors (≤2 weeks), relugolix may be temporarily discontinued. Resume relugolix after the inhibitor is stopped (a loading dose of 360 mg is required again if the interruption exceeds 7 days).

Concomitant Use with P-gp and Strong CYP3A Inducers

Concurrent use of strong P-gp and CYP3A inducers such as rifampicin reduces relugolix exposure, which may impair efficacy.

If concurrent use cannot be avoided, increase the relugolix dose to 240 mg daily. Resume the daily dose of 120 mg after discontinuing the inducer.

Use in Special Populations for Relugolix (Orgovyx)

Patients with Hepatic or Renal Impairment

No dosage adjustment is required for patients with mild to moderate renal impairment (creatinine clearance 15-89 mL/min) or mild to moderate hepatic impairment (Child-Pugh Class A/B).

However, there are currently no data on the use of relugolix in patients with end-stage renal disease (with or without dialysis) or severe hepatic impairment (Child-Pugh Class C), so cautious assessment is necessary.

Elderly Patients

Clinical studies showed that 81% of treated patients were ≥65 years old, and 35% were ≥75 years old.

Age did not significantly affect pharmacokinetics or testosterone suppression efficacy, so elderly patients may receive the standard dose.

Men of Reproductive Age

Animal studies indicate that relugolix may cause embryo toxicity. It is recommended that male patients advise their female partners of childbearing potential to use effective contraceptive measures during treatment and for 2 weeks after the last dose.

The drug may have a reversible impact on male fertility, which should be communicated to patients in advance.