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Review
. 2020 Sep;119(9):2749-2764.
doi: 10.1007/s00436-020-06786-1. Epub 2020 Jul 7.

Enhancing the antimalarial activity of artesunate

J O Adebayo  1 , H Tijjani  2 , A P Adegunloye  3 , A A Ishola  3 , E A Balogun  3 , S O Malomo  3
Affiliations
Review

Enhancing the antimalarial activity of artesunate

J O Adebayo et al. Parasitol Res. 2020 Sep.

Abstract

The global challenge to the treatment of malaria is mainly the occurrence of resistance of malaria parasites to conventionally used antimalarials. Artesunate, a semisynthetic artemisinin compound, and other artemisinin derivatives are currently used in combination with selected active antimalarial drugs in order to prevent or delay the emergence of resistance to artemisinin derivatives. Several methods, such as preparation of hybrid compounds, combination therapy, chemical modification and the use of synthetic materials to enhance solubility and delivery of artesunate, have been employed over the years to improve the antimalarial activity of artesunate. Each of these methods has advantages it bestows on the efficacy of artesunate. This review discussed the various methods employed in enhancing the antimalarial activity of artesunate and delaying the emergence of resistance of parasite to it.

Keywords: Artesunate; Combination therapy; Enhanced activity; Hybrids; Malaria.

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Conflict of interest statement

The authors declare that they have no conflicts of interest.

Figures

Fig. 1
Fig. 1
Artemisinin and its derivatives
Fig. 2
Fig. 2
Methods employed in improving the antimalarial activity of artesunate
Fig. 3
Fig. 3
Chemical structure of sodium artesunate
Fig. 4
Fig. 4
Chemical structures of some artesunate partner drugs
Fig. 5
Fig. 5
Some antibiotics co-administered as antimalarial
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Fig. 6
Artesunate hybrid compounds
Fig. 7
Fig. 7
Chemical structures of modified artesunate compounds
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