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Sulfadoxine-pyrimethamine/folic acid

Centers for Disease Control and Prevention · FDA-approved active Small molecule

Sulfadoxine-pyrimethamine inhibits dihydrofolate reductase and dihydropteroate synthase in parasites, blocking folate synthesis, while folic acid supplementation protects human cells from toxicity.

Sulfadoxine-pyrimethamine inhibits dihydrofolate reductase and dihydropteroate synthase in parasites, blocking folate synthesis, while folic acid supplementation protects human cells from toxicity. Used for Malaria prophylaxis and treatment (Plasmodium falciparum), Toxoplasmosis prophylaxis and treatment in immunocompromised patients.

At a glance

Generic nameSulfadoxine-pyrimethamine/folic acid
SponsorCenters for Disease Control and Prevention
Drug classAntifolate antimalarial
TargetDihydrofolate reductase; dihydropteroate synthase
ModalitySmall molecule
Therapeutic areaInfectious Disease
PhaseFDA-approved

Mechanism of action

Sulfadoxine and pyrimethamine are antifolate agents that sequentially inhibit enzymes critical for parasitic nucleotide synthesis, preventing DNA replication in Plasmodium species and Toxoplasma gondii. Folic acid is co-formulated to mitigate bone marrow suppression and other toxicities in the host by providing an alternative folate source that bypasses the blocked enzymatic pathway in human cells.

Approved indications

Common side effects

Key clinical trials

Primary sources

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SourceUsed for
ClinicalTrials.govTrial enrolment, design, endpoints, results

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