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学科主题: 临床医学
题名:
Prodrug AST-003 Improves the Therapeutic Index of the Multi-Targeted Tyrosine Kinase Inhibitor Sunitinib
作者: Huang, Qiang1,2; Zhou, Changhua1,2; Chen, Xiao1; Dong, Bing1,2; Chen, Siqi1,2; Zhang, Ning3; Liu, Yawei4; Li, Anrong5; Yao, Meicun1; Miao, Ji1; Li, Qing1,2; Wang, Zhong1,2
刊名: PLOS ONE
发表日期: 2015-10-29
DOI: 10.1371/journal.pone.0141395
卷: 10, 期:10
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Multidisciplinary Sciences
研究领域[WOS]: Science & Technology - Other Topics
关键词[WOS]: SIGNALING PATHWAYS ; IN-VIVO ; ANGIOGENESIS ; CARCINOMA ; APOPTOSIS ; DESIGN ; CANCER
英文摘要:

Patients have responded well to the multi-targeted tyrosine kinase inhibitor (TKI) Sunitinib in the clinic. But the severe toxic side effects associated with Sunitinib limit its therapeutic index. To improve the therapeutic index of Sunitinib, a prodrug strategy was employed to modify Sunitinib. The inactive prodrug AST-003 can be converted to Sunitinib in vitro and in vivo. Compared with Sunitinib, AST-003 has unique biochemical, cellular and pharmacokinetic properties with improved tolerability in mice and yield higher efficacy in tumor xenograft models. This prodrug strategy may constitute a novel paradigm to improve the therapeutic index of Sunitinib and other TKI or anti-angiogenesis drugs in general.

语种: 英语
所属项目编号: 2011Y038
项目资助者: Introduced Innovative R&amp ; D Team Leadership of Guangdong Province (P.R. China)
WOS记录号: WOS:000363920300035
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/62163
Appears in Collections:北京大学临床肿瘤学院_期刊论文

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作者单位: 1.Sun Yat Sen Univ, Sch Pharmaceut Sci, Guangzhou 510275, Guangdong, Peoples R China
2.Sun Yat Sen Univ, Ctr Cellular & Struct Biol, Guangzhou 510275, Guangdong, Peoples R China
3.Peking Univ, Canc Hosp, Beijing Inst Canc Res, Beijing 100871, Peoples R China
4.Gen Staff Dept PLA, Hlth Div, Guard Bur, Beijing, Peoples R China
5.Ascenta Pharmaceut, Guangzhou, Guangdong, Peoples R China

Recommended Citation:
Huang, Qiang,Zhou, Changhua,Chen, Xiao,et al. Prodrug AST-003 Improves the Therapeutic Index of the Multi-Targeted Tyrosine Kinase Inhibitor Sunitinib[J]. PLOS ONE,2015,10(10).
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