proguanil

Proguanil is a synthetic antimalarial drug used for the prevention and treatment of malaria, particularly infections caused by Plasmodium falciparum and Plasmodium vivax. It is often administered in combination with other antimalarials such as atovaquone or chloroquine to enhance efficacy, especially in regions with drug-resistant malaria. As a prodrug, proguanil is metabolized in the liver to its active form, cycloguanil. Cycloguanil acts as a selective inhibitor of plasmodial dihydrofolate reductase (DHFR), an enzyme essential for folic acid synthesis and DNA replication in the parasite. This inhibition disrupts nucleic acid synthesis and cell division within the parasite, leading to its death[1][5]. When combined with atovaquone, proguanil also enhances mitochondrial membrane collapse in parasites through mechanisms independent of DHFR inhibition[5]. Developed originally by ICI (now part of AstraZeneca), it has been widely used since its approval.

Brand names

PaludrineProguanilum

Other names

1-(p-Chlorophenyl)-5-isopropylbiguanideChlorguanideChloroguanideProguanileProguanilo