IR@PKUHSC  > 北京大学临床肿瘤学院
学科主题临床医学
Prodrug AST-003 Improves the Therapeutic Index of the Multi-Targeted Tyrosine Kinase Inhibitor Sunitinib
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
2015-10-29
DOI10.1371/journal.pone.0141395
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
WOS记录号WOS:000363920300035
项目编号2011Y038
资助机构Introduced Innovative R&amp ; D Team Leadership of Guangdong Province (P.R. China)
引用统计
被引频次:2[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/62163
专题北京大学临床肿瘤学院
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
推荐引用方式
GB/T 7714
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).
APA Huang, Qiang.,Zhou, Changhua.,Chen, Xiao.,Dong, Bing.,Chen, Siqi.,...&Wang, Zhong.(2015).Prodrug AST-003 Improves the Therapeutic Index of the Multi-Targeted Tyrosine Kinase Inhibitor Sunitinib.PLOS ONE,10(10).
MLA Huang, Qiang,et al."Prodrug AST-003 Improves the Therapeutic Index of the Multi-Targeted Tyrosine Kinase Inhibitor Sunitinib".PLOS ONE 10.10(2015).
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