Relugolix (Orgovyx) is a next-generation gonadotropin-releasing hormone receptor antagonist that provides an important treatment option for patients with advanced prostate cancer. As an orally administered endocrine therapy, special attention to precautions and standardized monitoring during medication is required to ensure therapeutic efficacy and minimize the risk of adverse reactions.

What are the Precautions for Using Relugolix (Orgovyx)?

Confirmation of Contraindications

Before initiating relugolix treatment, it is essential to confirm whether the patient has any contraindications.

This drug is strictly contraindicated in patients with a severe hypersensitivity reaction to relugolix or any product components.

Hypersensitivity reactions may present as severe symptoms such as angioedema; patients with a prior history of such hypersensitivity should not use the drug.

Cardiovascular Risk Assessment

Relugolix is an androgen deprivation therapy (ADT) that may cause QT/QTc interval prolongation.

For patients with congenital long QT syndrome, congestive heart failure, recurrent electrolyte abnormalities, or those taking medications known to prolong the QT interval, physicians should carefully assess whether the benefits of ADT outweigh the potential risks.

Correct electrolyte abnormalities before treatment, and consider regular monitoring of electrocardiograms (ECGs) and electrolyte levels.

Fertility and Embryo Toxicity Warnings

This drug has embryo-fetal toxicity and may cause fetal harm and pregnancy loss.

Male patients with female partners of childbearing potential should use effective contraceptive measures during treatment and for 2 weeks after the last dose.

Based on animal study results and its mechanism of action, relugolix may impair fertility in male patients of reproductive potential.

Medication Timing Management

If a patient misses a dose, take the missed dose immediately upon remembering.

If more than 12 hours have passed since the missed dose, do not take the missed dose and instead take 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 continuation of the maintenance dose of 120 mg daily.

Concomitant Use with P-gp Inhibitors

Concomitant use of relugolix with oral P-gp inhibitors should be avoided.

If unavoidable, administer relugolix first, followed by the P-gp inhibitor with an interval of at least 6 hours, and enhance monitoring of the patient for adverse reactions.

For short-term use of P-gp inhibitors, relugolix treatment may be interrupted for up to 2 weeks, and resumed after discontinuing the P-gp inhibitor.

Concomitant Use with P-gp and Strong CYP3A Inducers

Concomitant use of relugolix with combined P-gp and strong CYP3A inducers should be avoided.

If concurrent use is necessary, increase the relugolix dose to 240 mg once daily.

After discontinuing the inducer, resume the recommended dose of 120 mg once daily.

Medication Monitoring for Relugolix (Orgovyx)

Regular Monitoring of Laboratory Indicators

During treatment, regularly monitor serum prostate-specific antigen (PSA) levels to assess therapeutic efficacy.

If PSA increases, measure serum testosterone concentrations.

Periodically monitor liver function indicators (including ALT and AST), as well as blood glucose, triglyceride, and hemoglobin levels.

Special Monitoring for Adverse Reactions

Closely monitor for the occurrence of hot flashes, the most common adverse reaction with an incidence rate of up to 54%.

Monitor changes in blood glucose and lipid levels, and observe for symptoms such as musculoskeletal pain, fatigue, constipation, and diarrhea.

Cardiovascular System Monitoring

Regularly perform ECG monitoring, with special attention to changes in the QT interval.

Observe for early signs of serious adverse events such as myocardial infarction, acute kidney injury, and arrhythmias.

Hypersensitivity Reaction Monitoring

Be vigilant for hypersensitivity reactions, including symptoms such as angioedema.

If relevant symptoms occur, temporarily discontinue relugolix immediately and seek medical attention promptly.