General Information

Orgovyx (relugolix) is a gonadotropin-releasing hormone (GnRH) receptor antagonist. It blocks the GnRH receptor and reduces production of testicular testosterone, a hormone known to stimulate the growth of prostate cancer.

Orgovyx is specifically indicated for the treatment of adult patients with advanced prostate cancer.

Orgovyx is supplied as a tablet for oral administration. 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. Tablets should be swallowed whole and not crushed or chewed.

A missed dose of Orgovyx should be taken as soon as it is remembered. 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.

Side Effects

Adverse effects associated with the use of Orgovyx may include, but are not limited to, the following:

hot flush

glucose increased

triglycerides increased

musculoskeletal pain

hemoglobin decreased

alanine aminotransferase (ALT) increased

fatigue,

aspartate aminotransferase (AST) increased

constipation

diarrhea

Clinical Trial Results

The FDA approval of Orgovyx was based on the Phase 3 HERO study, a randomized, open label study in men with advanced prostate cancer requiring at least 1 year of androgen deprivation therapy and defined as biochemical (PSA) or clinical relapse following local primary intervention, newly diagnosed castration-sensitive metastatic disease, or advanced localized disease. A total of 934 patients were randomized to receive Orgovyx or leuprolide in a 2:1 ratio for 48 weeks: a) Orgovyx at a loading dose of 360 mg on the first day followed by daily doses of 120 mg orally b) Leuprolide acetate 22.5 mg injection (or 11.25 mg in Japan and Taiwan) subcutaneously every 3 months. Leuprolide acetate 11.25 mg is a dosage regimen that is not recommended for this indication in the US. Orgovyx met the primary endpoint and achieved sustained testosterone suppression to castrate levels (< 50 ng/dL) through 48 weeks in 96.7% of men, compared with 88.8% of men receiving leuprolide acetate injections. Orgovyx also achieved several key secondary endpoints compared to leuprolide acetate, including suppression of testosterone to castrate levels at Day 4 and Day 15 (56% versus 0% and 99% versus 12%, respectively) and profound suppression of testosterone (< 20 ng/dL) at Day 15 (78% versus 1%). Orgovyx lowered prostate-specific antigen (PSA), on average, by 65% at Day 15 and by 83% at Day 29. In a substudy, 55% of men treated with Orgovyx achieved normal testosterone levels (> 280 ng/dL) or returned to baseline within 90 days of treatment discontinuation.