Abstract
The emergence of multi-drug resistant strains of Plasmodium falciparum has rendered many affordable antimalarials, such as chloroquine, much less effective in addressing the severe health issues in sub-Saharan Africa, Southeast Asia and the Amazon region. In order to overcome the neurotoxicity of an initial series of artemisinin-derived drugs and their relatively high production costs, an intensive and all-inclusive research programme to develop new derivatives has been undertaken. Two efficient antimalarial drug candidates of different chemotype have been devised, the artemisinin derivative artemisone and 1,2,4-troxolane OZ277. Both are nontoxic, more potent than artemisinin and should be affordable to people of endemic regions. The same may hold for the backup candidates artemiside and OZ439.
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Notes
- 1.
However, dihydroartemisinin was detected in plasma during assessment of the safety of artemisone [27]. The concentrations were low, with geometric mean C max values of 10 ng/ml after an 80 mg dose.
- 2.
The annual demand for artemisinin as a starting material for transformation into semi-synthetic products amounts to ca. 114 tonnes for Coartem® production only. Since synthesis of artemisinin is uneconomical currently, Novartis initiated an increase of the agricultural cultivation of Artemisia annua in Kenya, Tanzania and Uganda and extraction of artemisinin therefrom, in addition to Chinese supplies of artemisinin.
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Opsenica, D.M., Šolaja, B.A. (2011). Second-Generation Peroxides: The OZs and Artemisone. In: Staines, H., Krishna, S. (eds) Treatment and Prevention of Malaria. Milestones in Drug Therapy. Springer, Basel. https://doi.org/10.1007/978-3-0346-0480-2_10
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