August 2021: The first oral gonadotropin-releasing hormone (GnRH) receptor antagonist, relugolix (ORGOVYX, Myovant Sciences, Inc.), was approved by the Food and Drug Administration on December 18, 2020, for adult patients with metastatic prostate cancer.
HERO (NCT03085095), a randomised, open label trial in males requiring at least one year of androgen deprivation therapy for prostate cancer recurrence after radiotherapy or surgery or newly diagnosed castration-sensitive advanced prostate cancer, was used to assess efficacy. Relugolix 360 mg oral loading dosage on the first day, followed by daily oral doses of 120 mg, or leuprolide acetate 22.5 mg injection subcutaneously every 3 months for 48 weeks were given to patients (N=934).
The key efficacy end measure was medical castration rate, which was defined as achieving and maintaining serum testosterone suppression to castrate levels (50 ng/dL) by day 29 of treatment and maintaining it for the next 48 weeks. In the relugolix arm, the medical castration rate was 96.7 percent (95 percent CI: 94.9 percent, 97.9 percent).
Hot flush, musculoskeletal pain, weariness, diarrhoea, and constipation were the most common side effects (ten percent) in patients taking relugolix in HERO. Increased glucose, triglycerides, alanine aminotransferase, and aspartate aminotransferase were the most prevalent laboratory abnormalities (15%). Hemoglobin levels were also found to be lower.
A loading dose of 360 mg on the first day is indicated, followed by a daily oral dose of 120 mg at about the same time each day, with or without meals.
Reference : https://www.fda.gov/
Check details here.
