Drug intelligence / Profile preview

sulfadoxine + pyrimethamine + chlorproguanil + dapsone

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

Overview

This is a combination drug consisting of four antimalarial agents: sulfadoxine, pyrimethamine, chlorproguanil, and dapsone. Each component targets the folate synthesis pathway in Plasmodium species but at different enzymatic steps. Sulfadoxine is a sulfonamide that inhibits dihydropteroate synthase; pyrimethamine and chlorproguanil are both inhibitors of dihydrofolate reductase (DHFR), though they have different binding affinities and resistance profiles; dapsone is a sulfone that also inhibits dihydropteroate synthase. The rationale for combining these drugs would be to provide broad inhibition of folate metabolism in malaria parasites, potentially overcoming resistance seen with dual or triple combinations. However, there is no evidence from the provided sources or current literature that this specific four-drug combination has been developed as a marketed product or tested in clinical trials as a single formulation. Instead, dual combinations such as sulfadoxine-pyrimethamine (Fansidar) and chlorproguanil-dapsone (Lapdap) have been studied extensively for malaria treatment[1][2][3][5][7][9].

02

Targets

DHPS (Dihydropteroate synthase)DHFR (Dihydrofolate reductase)

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