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sulfadoxine + pyrimethamine + chloroquine
- Development stage
- Unknown
- Lead developer
- Roche
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
This drug is a fixed-dose combination of three antimalarial agents—sulfadoxine, pyrimethamine, and chloroquine—used for the treatment of uncomplicated malaria. Sulfadoxine is a long-acting sulfonamide antibiotic that inhibits dihydropteroate synthase, blocking folate synthesis in the parasite. Pyrimethamine is an antiprotozoal agent that selectively inhibits protozoal dihydrofolate reductase, further preventing tetrahydrofolate formation. Chloroquine acts by interfering with heme detoxification in Plasmodium species, leading to toxic buildup within the parasite. The combination was developed to improve efficacy and reduce resistance compared to monotherapy; however, widespread resistance has limited its use in many regions[1][2][6][8]. It has been used as first-line therapy for uncomplicated falciparum malaria in several countries where artemisinin-based therapies are unavailable or not licensed[1].
- Brand names
- Fansidar (for sulfadoxine-pyrimethamine)
- Other names
- pyrimethamine and sulfadoxine + chloroquine
02
Targets
DHFR-TS (Bifunctional dihydrofolate reductase-thymidylate synthase)DHFR (Dihydrofolate reductase)DHPS (Dihydropteroate synthase)β-Hematin
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