Drug intelligence / Profile preview

sulfalene + pyrimethamine + amodiaquine

Development stage
Unknown
Lead developer
The London School of Hygiene & Tropical Medicine
Modality
Small Molecules
Administration
Oral
01

Overview

Sulfalene-pyrimethamine + amodiaquine is a combination antimalarial regimen primarily utilized for seasonal intermittent preventive treatment (IPTc) or seasonal malaria chemoprevention (SMC) in children. The regimen consists of three active small molecule components: sulfalene (a long-acting sulfonamide), pyrimethamine (a dihydrofolate reductase inhibitor), and amodiaquine (a 4-aminoquinoline). Sulfalene and pyrimethamine act synergistically as antifolate agents; sulfalene inhibits dihydropteroate synthase (DHPS) and pyrimethamine inhibits dihydrofolate reductase (DHFR), effectively blocking the parasite's folate synthesis pathway. Amodiaquine interferes with the parasite's ability to detoxify heme, a toxic byproduct of hemoglobin digestion. This triple combination provides a multi-targeted approach to prevent *Plasmodium falciparum* infection in areas with highly seasonal malaria transmission, such as sub-Saharan Africa.

Other names
sulfamethoxypyrazine-pyrimethamine + amodiaquinesulfalene-pyrimethamine + amodiaquine
02

Targets

DHPS (Dihydropteroate synthase)β-HematinDHFR (Dihydrofolate reductase)CYP2C8 (Cytochrome P450 2C8)DHFR-TS (Bifunctional dihydrofolate reductase-thymidylate synthase)

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