Comparison of Beiyi® and its reference product Enantone® as agonists of luteinizing hormone-releasing hormone against prostate cancer: a multicenter, randomized single-dose study.

BACKGROUND: Leuprolide acetate is a potent agonist of luteinizing hormone-releasing hormone that has been licensed to treat prostate cancer. The microsphere formulation of leuprolide acetate called Beiyi®, developed in China, has shown favorable pharmacokinetics, pharmacodynamics and safety similar to those of the reference drug Enantone® in healthy individuals. The present study examined whether the two formulations are bioequivalent in men with prostate cancer. METHODS: This multicenter, open-label study randomized 120 Chinese men with prostate cancer 1:1 to receive a single subcutaneous injection of Beiyi® or Enantone® (3.75 mg). The two groups were compared in terms of pharmacokinetics and safety. RESULTS: The ratio of the geometric means of the maximum serum concentration (Cmax) of Beiyi® and Enantone® was 98.34% (91.88%-105.25%); the ratio of the geometric means of the concentration-time curve from 7 to 28 days (AUC7-28) was 100.52% (88.17%-114.60%); and the ratio of the geometric means of the concentration-time curve from 0 to 28 days (AUC0-28) was 109.07% (98.54%-120.73%). The three 90% confidence intervals fell within the range of 80.00%-125.00%, indicating similar pharmacokinetics. The two drugs showed similar safety profiles, with no treatment-emergent adverse events leading to withdrawal or death. CONCLUSION: The two formulations of leuprolide acetate microspheres Beiyi® and Enantone® show similar pharmacokinetics and safety in Chinese men with prostate cancer. These results support the further clinical development of Beiyi® as a generic formulation of Enantone®. TRIAL REGISTRATION: CTR20222654 on http://www.chinadrugtrials.org.cn/index.html.