Pharmacokinetic and pharmacodynamic evaluation of the new prolonged-release leuprorelin acetate microspheres for injection compared with Enantone® in healthy Chinese male volunteers. (2nd September 2021)

• Record Type: Journal Article
• Authors: Zhou, Huan; Xie, Jing; Zhu, Xingyu; Li, Xiaoyi; Yu, Xiaohui; Zhang, Yong; Su, Yue; He, Cuixia; Zhu, Minhui; Li, Xiao li; Liu, Yuanyuan; Chen, Juan; Cheng, Dongmei; Chen, Mengmeng; Wang, Ying; Ge, Qin; Fan, Ling; Wang, Ying; Shao, ZhongHuan; Liu, Bingyan; Shan, Rongfang; Dai, Xiangrong; Wang, Hongju; Wang, Huaxue
• Is Part Of: Expert opinion on drug metabolism and toxicology. Volume 17:Number 9(2021)
• Page Start: 1149
• Page End: 1156
• Publication Date: 2021-09-02
• Subjects: New prolonged-release leuprorelin acetate microspheres for injection -- Enantone® -- PK -- testosterone -- castration -- safety; Drugs -- Toxicology -- Periodicals; Drugs -- Metabolism -- Periodicals; 615.7
• DOI: 10.1080/17425255.2021.1948534
• Languages: English
• ISSNs: 1742-5255

Abstract

ABSTRACT: Purpose: To compare the pharmacokinetics, pharmacodynamics and safety of the new prolonged-release leuprorelin acetate microspheres for injection (3.75 mg) with the reference product Enantone® (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®. Results: There were no significant differences in Cmax, AUC0-t and AUC0-48 between the test group and reference group (P > 0.05). The 90% confidence intervals of the two groups were 87.49%~112.74%, 97.15%~154.25%, and 80.85%~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.