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Encyclopedia of Malaria pp 1–12Cite as

Antifolate Drugs

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Synonyms

Antifols; Folate antagonists; Folate antimetabolites; Folate enzyme inhibitors; Proguanil; Pyrimethamine; Sulfa drugs; Sulfadoxine-pyrimethamine (SP)

Definition

Antifolate drugs are used as antimalarials through their inhibition of folate metabolism of the parasite, both in the synthesis and use of folate cofactors. Humans do not make any folate cofactors, relying only on exogenous supply, and are therefore mostly spared from the effects of antifolate drugs. The key enzyme targets are dihydropteroate synthase (DHPS), inhibited by sulfa drugs, and dihydrofolate reductase (DHFR), inhibited by pyrimethamine, cycloguanil, and other inhibitors. These drugs are mostly used as combinations of the two inhibitors acting against different targets, with synergistic effect. Combinations with other types of antimalarials are sometimes made in the attempt to prevent the emergence of drug resistance. Antifolate resistance occurs mainly from mutations at the genes encoding their target...

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Authors and Affiliations

  1. National Centre for Genetic Engineering and Biotechnology (BIOTEC), National Science and Technology Development Agency (NSTDA), Thailand Science Park, Phahonyothin Road, Pathum Thani, 12120, Thailand

    Yongyuth Yuthavong

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  1. Yongyuth Yuthavong
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Correspondence to Yongyuth Yuthavong .

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Editors and Affiliations

  1. Heswall, United Kingdom

    Marcel Hommel

  2. Institut für Tropenmedizin, Universität Tübingen, Tübingen, Germany

    Peter G. Kremsner

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Yuthavong, Y. (2013). Antifolate Drugs. In: Hommel, M., Kremsner, P. (eds) Encyclopedia of Malaria. Springer, New York, NY. https://doi.org/10.1007/978-1-4614-8757-9_2-1

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  • DOI: https://doi.org/10.1007/978-1-4614-8757-9_2-1

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