Ozonide Antimalarial Activity in the Context of Artemisinin-Resistant Malaria

被引:41
作者
Giannangelo, Carlo [1 ]
Fowkes, Freya J. I. [2 ,3 ,4 ]
Simpson, Julie A. [3 ]
Charman, Susan A. [5 ]
Creek, Darren J. [1 ]
机构
[1] Monash Univ, Monash Inst Pharmaceut Sci, Drug Delivery Disposit & Dynam, Clayton, Vic, Australia
[2] Burnet Inst, Melbourne, Vic, Australia
[3] Univ Melbourne, Melbourne Sch Populat & Global Hlth, Ctr Epidemiol & Biostat, Melbourne, Vic, Australia
[4] Monash Univ, Dept Epidemiol & Prevent Med, Clayton, Vic, Australia
[5] Monash Univ, Monash Inst Pharmaceut Sci, Ctr Drug Candidate Optimisat, Clayton, Vic, Australia
基金
澳大利亚国家健康与医学研究理事会; 英国医学研究理事会;
关键词
PLASMODIUM-FALCIPARUM MALARIA; IN-VITRO ASSESSMENT; DELAYED-CLEARANCE; PHARMACODYNAMIC PROPERTIES; SYNTHETIC TRIOXOLANE; HEME ALKYLATION; RING STAGES; DIHYDROARTEMISININ; ARTESUNATE; ARTEROLANE;
D O I
10.1016/j.pt.2019.05.002
中图分类号
R38 [医学寄生虫学]; Q [生物科学];
学科分类号
07 ; 0710 ; 09 ; 100103 ;
摘要
The ozonides are one of the most advanced drug classes in the antimalarial development pipeline and were designed to improve on limitations associated with current front-line artemisinin-based therapies. Like the artemisinins, the pharmacophoric peroxide bond of ozonides is essential for activity, and it appears that these antimalarials share a similar mode of action, raising the possibility of cross-resistance. Resistance to artemisinins is associated with Plasmodium falciparum mutations that allow resistant parasites to escape short-term artemisinin-mediated damage (elimination half-life similar to 1 h). Importantly, some ozonides (e.g., OZ439) have a sustained in vivo drug exposure profile, providing a major pharmacokinetic advantage over the artemisinin derivatives. Here, we describe recent progress made towards understanding ozonide antimalarial activity and discuss ozonide utility within the context of artemisinin resistance.
引用
收藏
页码:529 / 543
页数:15
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