Pharmacokinetic And Pharmacodynamic Evaluation Of The New Prolonged-Release Leuprorelin Acetate Microspheres For Injection Compared With Enantone (R) In Healthy Chinese Male Volunteers

Purpose: To compare the pharmacokinetics, pharmacodynamics and safety of the new prolongedrelease leuprorelin acetate microspheres for injection (3.75 mg) with the reference product Enantone (R) (3.75 mg).Method: 48 healthy male volunteers were enrolled and randomly received a single 3.75 mg dose of the test drug or Enantone (R).Results: There were no significant differences in C-max, AUC(0-t) and AUC(0-48) between the test group and reference group (P > 0.05). The 90% confidence intervals of the two groups were 87.49%similar to 112.74%, 97.15%similar to 154.25%, and 80.85%similar to 109.01%, respectively. Twenty-eight days after administration, both groups reached 100.0% castration level; there was no difference in the time from administration to reaching castration level between the two groups (P > 0.05); However, the difference between the two groups in the duration of castration level was statistically significant (P < 0.05). There were no major or serious adverse events, and the severity was mild to moderate.Conclusion: The pharmacokinetic characteristics of leuprorelin in two groups were consistent. The two groups exhibited similar inhibitory effects on testosterone and more subjects in the test group maintained a longer castration time than those in the reference group.