Drug intelligence / Profile preview

chlorproguanil

Development stage
Phase 4
Lead developer
GSK
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Chlorproguanil is a synthetic antimalarial drug belonging to the biguanide class. It is a dichloro-derivative of chloroguanide and acts as an inhibitor of dihydrofolate reductase in malaria parasites after cytochrome P450-catalyzed cyclization. This inhibition disrupts folic acid metabolism essential for parasite DNA synthesis and replication. Chlorproguanil has been studied primarily for the treatment of malaria caused by *Plasmodium falciparum* and *Plasmodium malariae*. It was investigated both as monotherapy and in combination with dapsone or artesunate but development was discontinued due to safety concerns—specifically post-treatment hemolytic anemia in patients with glucose-6-phosphate dehydrogenase (G6PD) deficiency[1][2][3][5].

Other names
chlorproguanil1-(3,4-dichlorophenyl)-5-isopropylbiguanideclorproguanilclorpreguanilechlorproguanilumlapudrine
02

Targets

DHFR (Dihydrofolate reductase)

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