Bioequivalence and safety study of letrozole tablet in healthy Chinese postmenopausal women volunteers

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	Bioequivalence and safety study of letrozole tablet in healthy Chinese postmenopausal women volunteers
	Liu Y(刘一); Zhang YF(张逸凡); Wang Q(王茜); Yang W(杨巍); Chen XY(陈笑艳); Jing S(荆珊); Zhao LB(赵立波); Zhang CY(张春燕); Wei LH(魏丽恵); Li XP(李小平)
刊名	Journal of Chinese Pharmaceutical Sciences
	2013
卷号	22 期号:2 页码:190-196
关键词	Letrozole Bioequivalence Safety LC-MS/MS Chinese postmenopausal women LC-MS/MS
ISSN号	1003-1057
其他题名	来曲唑片在中国健康绝经期女性志愿者人体生物等效性及安全性研究
文献子类	Article
英文摘要	Letrozole is an orally active aromatase inhibitor for the treatment of postmenopausal women with breast cancer. A single-dose, randomized, open-label, two-way crossover study was designed to compare the bioequivalence and safety of two formulations of letrozole (2.5 mg/tablet), including a newly developed generic formulation (test) and a branded formulation (reference) in a group of healthy Chinese postmenopausal women volunteers under fasting conditions. Blood samples were obtained before study drug administration and at 0.25, 0.50, 0.75, 1.00,1.25, 1.50,2.00, 2.50,3.00, 3.50,4.00,6.00 8.00, 12.00, 24.00, 48.00, 72.00, 96.00,144.00, 192.00 and 240.00 h after drug administration. Letrozole levels in plasma were analyzed using a liquid chromatography-tandem mass spectrometry (LC-MS/MS) method. The safety profile was evaluated by adverse events (AEs) record, and assessed by physical examination, vital signs, spontaneous reporting, and clinical laboratory results. A total of 30 healthy Chinese postmenopausal women were enrolled in this study; however, only 29 subjects were included in bioequivalence assessments due to serious adverse events (SAEs) in 1 subject. The 90% CIs for the ln-transformed ratios of C_(max), AUC_(0-t), and AUC_(0-) were 99.55%-115.17%, 97.35%-103.50%, and 97.29%-103.96%, respectively. All values met the predetermined criteria for assuming bioequivalence. One subject (3.3%) experienced SAE who received the reference formulation and 10 subjects (33.3%) reported a total of 13 mild AEs (4 reported from 4 subjects who received the test formulation, and 9 reported from 6 subjects who received the reference formulation). In this single-dose (2.5 mg) study, we found that the test and reference formulations of letrozole tablet met the regulatory definition for assuming bioequivalence in healthy Chinese postmenopausal women. Both formulations were generally well tolerated in the population studied. Chinese Clinical Trials registration number: ChiCTR-TRC-11001457.
资助项目	supported by Fresenius Kabi Oncology Ltd[00000000]
WOS研究方向	Pharmacology & Pharmacy (provided by Clarivate Analytics)
语种	英语
CSCD记录号	CSCD:4905294
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/267765]
专题	上海药物代谢研究中心
通讯作者	Zhong DF(钟大放)
作者单位	1.Department of Pharmacy, Peking University Peoples Hospital, Beijing 100044, China.; 2.Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.; 3.Department of Gynecology and Obstetrics, Peking University Peoples Hospital, Beijing 100044, China.
推荐引用方式 GB/T 7714	Liu Y,Zhang YF,Wang Q,et al. Bioequivalence and safety study of letrozole tablet in healthy Chinese postmenopausal women volunteers[J]. Journal of Chinese Pharmaceutical Sciences,2013,22(2):190-196.
APA	刘一.,张逸凡.,王茜.,杨巍.,陈笑艳.,...&方翼.(2013).Bioequivalence and safety study of letrozole tablet in healthy Chinese postmenopausal women volunteers.Journal of Chinese Pharmaceutical Sciences,22(2),190-196.
MLA	刘一,et al."Bioequivalence and safety study of letrozole tablet in healthy Chinese postmenopausal women volunteers".Journal of Chinese Pharmaceutical Sciences 22.2(2013):190-196.