A single-dose, randomized, open-labeled, parallel-group study comparing the pharmacokinetics, pharmacodynamics and safety of leuprolide acetate microspheres 3.75 mg and Enantone 3.75 mg in healthy male subjects.

Leuprolide acetate microspheres developed by Shanghai Livzon Pharmaceutical Co., Ltd. (T) have been marketed in China for more than 10 years, benefiting a large number of patients, and will continue to play an important role in China. However, as a generic drug, it is unclear whether there is a difference in efficacy between T and the original product Enantone (R). This study compared the differences in efficacy and safety of two 1-month depot formulations in 48 healthy Chinese male subjects by comparing multiple pharmacokinetic (PK) and pharmacodynamic (PD) parameters. The main research indicators were the PK parameters of leuprolide (C, AUC, AUC, and AUC) and the PD parameters of testosterone (E, AUEC, AUEC, and AUEC) after 42 days of administration. The C, AUC, AUC and AUC of leuprolide were slightly higher in the T group than in the R group with 90% confidence intervals (CIs) of 94.43-118.53%, 109.13-141.88%, 109.53-139.54%, and 105.17-145.74%, respectively. No significant differences in the PD parameters (E, AUEC, AUEC, and AUEC) existed between the T and R groups, and 90% CIs were 62.80-93.57%, 88.17-110.55, 95.72%-118.50%, and 79.77-105.63, respectively. At 672 h (D28), the castration rate of T was 91.30% (21/23) and that of R was 60.87% (14/23). The PK characteristics were consistent and the inhibitory effects on testosterone levels were similar in both T and R groups; further, clinical safety was observed for both T and R formulations, suggesting that these two products can replace each other in clinical practice. http://www.chinadrugtrials.org.cn/clinicaltrials.searchlistdetail.dhtml, identifier CTR20200641.