Hormone-sensitive prostate cancer

Active Ingredient: Relugolix

Indication for Relugolix

Population group: only adults (18 years old or older)
Therapeutic intent: Curative procedure

Relugolix is indicated for the treatment of adult patients with advanced hormone-sensitive prostate cancer.

For this indication, competent medicine agencies globally authorize below treatments:

360 mg on the first day and 120 mg once daily thereafter

For:

Dosage regimens

Oral, 360 milligrams relugolix, once daily, over the duration of 1 day. Afterwards, oral, 120 milligrams relugolix, once daily.

Detailed description

Treatment with relugolix should be initiated with a loading dose of 360 mg (three tablets) on the first day, followed by a 120 mg (one tablet) dose taken once daily at approximately the same time each day.

Because relugolix does not induce an increase in testosterone concentrations, it is not necessary to add an anti-androgen as surge protection at initiation of therapy.

Dose modification for use with P-gp inhibitors

Co-administration of relugolix with oral P-glycoprotein (P-gp) inhibitors must be avoided. If co-administration is unavoidable, relugolix should be taken first and dosing should be separated by at least 6 hours. Treatment with relugolix may be interrupted for up to 2 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

Co-administration of relugolix with combined P-gp and strong cytochrome P450 (CYP) 3A inducers must be avoided. If co-administration is unavoidable, the dose of relugolix must be increased to 240 mg once daily. After discontinuation of the combined P-gp and strong CYP3A inducer, the recommended 120 mg dose of relugolix once daily must be resumed.

Missed doses

If a dose is missed, relugolix must be taken as soon as the patient remembers. If the dose was missed by more than 12 hours, the missed dose must not be taken and regular dosing schedule should be resumed the following day.

If treatment with relugolix is interrupted for greater than 7 days, relugolix must be restarted with a loading dose of 360 mg on the first day, followed with a dose of 120 mg once daily.

Dosage considerations

Relugolix can be taken with or without food. Relugolix tablets should be taken with some liquid as needed and should be swallowed whole.

Active ingredient

Relugolix

Relugolix is a nonpeptide GnRH receptor antagonist that competitively binds to GnRH receptors in the anterior pituitary gland preventing native GnRH from binding and signalling the secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). Consequently, the production of testosterone from the testes is reduced.

Read more about Relugolix

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