Serum testosterone suppression and potential for agonistic stimulation during chronic treatment with monthly depot formulation of domestic substitute of leuprorelin acetate microspheres for metastatic prostate cancer

• Published in: 中德临床肿瘤学杂志（英文版） no. 7; pp. 320 - 322
• Main Author: Dongliang Pan Liming Dong Lianchao Jin Bing Yang Zhe Zhou Kai Zhang Xianghua Zhang Ningchen Li
• Format: Journal Article
• Language: English
• Published: Department of Urology, Peking University Shougang Hospital Wujieping Urology Medical Center of Peking University, Beijing 100144, China%Department of Urology, Weihai Wendeng Center Hospital, Shandong 264400, China 2014
• Subjects: 前列腺癌; 微球; 慢性乙型肝炎; 替代品; 治疗; 血清睾酮; 转移性; 醋酸; leuprorelin; testosterone; prostatic neoplasms,metastatic; domestic substitute
• ISSN: 1610-1979; 1613-9089
• DOI: 10.1007/s10330-014-1326-z

Objective： We aimed to evaluate the efficiency of serum testosterone suppression as well as the potential for agonistic stimulation of serum testosterone during chronic treatment with monthly （3.75 mg） depot formulation of domestic substitute of leuprorelin acetate microspheres for patients with metastatic prostate cancer. Methods： A total of 23 patients with metastatic prostate cancer were enrolled in the prospective study and received 6 monthly intramuscular depot injections of domestic substitute of leuprorelin acetate microspheres. Their levels and patterns of serum testosterone suppression and the potential for agonistic stimulation of serum testosterone were monitored following injection monthly （3.75 rag） depot formulation of domestic substitute of leuprorelin acetate microspheres for 24 weeks. Results： Mean testosterone was 431.4 ng/dL, 119.3 ng/dL, 28.2 ng/dL by week 1, 2, 3 and decreased to less than 15.6 ng/dL by week 4 where it remained throughout the treatment period. Median time to suppression of serum testosterone was 20.7 days. No transient minor ＂escape＂ from suppression occurred in all patients which was defined as a single testosterone value greater than 50 ng/dL once suppression was achieved. Assessment of agonistic stimulation following the second depot injection revealed no pattern of stimulation. Conclusion： We concluded that monthly （3.75 mg） depot formulation of domestic substitute of leuprorelin acetate microspheres could provide persistent, stable suppression of serum testosterone throughout the dosing intervals, and that the initial depot injection of this formulation also could provide sufficient pituitary desensitization to prevent agnostic stimulation of serum testosterone during chronic treatment.