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Investigational hypoxia-activated prodrugs: Making sense of future development
Su,Min Xia1; Zhang,Le Le1; Huang,Zhang Jian2; Shi,Jia Jie1; Lu,Jin Jian1
Source PublicationCurrent Drug Targets

Hypoxia, which occurs in most cancer cases, disrupts the efficacy of anticarcinogens. Fortunately, hypoxia itself is a potential target for cancer treatment. Hypoxia-activated prodrugs (HAPs) can be selectively activated by reductase under hypoxia. Some promising HAPs have been already achieved, and many clinical trials of HAPs in different types of cancer are ongoing. However, none of them has been approved in clinic to date. From the studies on HAPs began, some achievements are obtained but more challenges are put forward. In this paper, we reviewed the research progress of HAPs to discuss the strategies for HAPs development. According to the research status and results of these studies, administration pattern, reductase activity, and patient selection need to be taken into consideration to further improve the efficacy of existing HAPs. As the requirement of new drug research and development, design of optimal preclinical models and clinical trials are quite important in HAPs development, while different drug delivery systems and anticancer drugs with different mechanisms can be sources of novel HAPs.

KeywordDna Alkylating Agents Hypoxia-activated Prodrug Patient Selection Reductase Activity Targeted Drugs Topoisomerase Ii Inhibitors
URLView the original
Indexed BySCIE
WOS Research AreaPharmacology & Pharmacy
WOS SubjectPharmacology & Pharmacy
WOS IDWOS:000462720500004
Scopus ID2-s2.0-85064558937
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Cited Times [WOS]:2   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionInstitute of Chinese Medical Sciences
Affiliation1.State Key Laboratory of Quality Research in Chinese Medicine,Institute of Chinese Medical Sciences,University of Macau,Macao
2.State Key Laboratory of Natural Medicines,Department of Pharmaceutics,China Pharmaceutical University,Nanjing,China
First Author AffilicationInstitute of Chinese Medical Sciences
Recommended Citation
GB/T 7714
Su,Min Xia,Zhang,Le Le,Huang,Zhang Jian,et al. Investigational hypoxia-activated prodrugs: Making sense of future development[J]. Current Drug Targets,2019,20(6):668-678.
APA Su,Min Xia,Zhang,Le Le,Huang,Zhang Jian,Shi,Jia Jie,&Lu,Jin Jian.(2019).Investigational hypoxia-activated prodrugs: Making sense of future development.Current Drug Targets,20(6),668-678.
MLA Su,Min Xia,et al."Investigational hypoxia-activated prodrugs: Making sense of future development".Current Drug Targets 20.6(2019):668-678.
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