A randomized, open-label, multi-center, active-controlled phase II study comparing abiraterone acetate tablets (II), an improved formulation, versus originator abiraterone acetate in patients with metastatic castration-resistant prostate cancer

作者：Xiaolin Lü, Tao Dai, Xue Chen, Bin Wu, H. Chen, Jitao Wu, Dexin Yu, Huixin Ge, Jian Li, Houbao Huang, Tiwu Fan, Linzhong Cheng, Xiaoping Zhang, Xuepei Zhang, Xin Yao, Junli Wei, Zhenqiang Xu, Wenzeng Yang, Chaohong He, Jiexin Luo, Ling Guan, Bin Fu, Qilin Wang, Xiaofeng Chen, Yongdong Zhang, Benkang Shi, Bin Zheng, Yong Wang, Hong Luo, G. Chen, Huan Wang, Quanren Wang, Dingwei Ye · 发表于：BMC Medicine · 年份：2025 · DOI：10.1186/s12916-025-04053-7 · 被引用次数：1 · 研究领域：Prostate Cancer Treatment and Research、Prostate Cancer Diagnosis and Treatment、Radiopharmaceutical Chemistry and Applications

BACKGROUND: Abiraterone is a 17α-hydroxylase/C17-20 lyase inhibitor used for the treatment of metastatic castration-resistant prostate cancer (CRPC). This multi-center, randomized, open-label, active-controlled phase II study compared the pharmacodynamics (PD), pharmacokinetics (PK), and safety of abiraterone acetate tablets (II) (AAT[II]), a new formulation of abiraterone acetate, and ZYTIGA®, the originator abiraterone acetate (OAA), in patients with metastatic CRPC. METHODS: Patients were randomized 1:1 to receive 300 mg AAT(II) daily plus 5 mg prednisone twice daily or 1000 mg OAA daily plus 5 mg prednisone twice daily for 84 days. The primary endpoint was the serum testosterone level (rounded-up) on Day 9 and/or Day 10. Absolute testosterone concentration, prostate-specific antigen (PSA) concentration, steady-state PK of abiraterone, and safety were also evaluated. RESULTS: Sixty-nine patients were enrolled in the study, with 35 assigned to AAT(II) and 34 to OAA. The least squares (LS) mean (standard error) of serum testosterone concentration (rounded-up) on Day 9 and/or Day 10 were 1.075 (0.034) and 1.000 (0.034) in the AAT(II) and OAA groups, respectively. The geometric mean ratio (AAT[II] vs. OAA) was 1.053 (90% confidence interval [CI], 0.998 to 1.110) and the LS mean difference was 0.075 (95% CI, -0.021 to 0.171). The 90% CI fell within the 80.0% to 125.0% equivalence limits, suggesting equivalent PD effect of the two formulations. AAT(II) also exhibited high testos...