Drug intelligence / Profile preview

amodiaquine + sulphadoxine-pyrimethamine + artesunate + sulphadoxine-pyrimethamine

Development stage
Unknown
Lead developer
Sanofi
Modality
Small Molecules
Administration
Oral
01

Overview

Amodiaquine + sulphadoxine-pyrimethamine + artesunate + sulphadoxine-pyrimethamine is a multi-drug combination regimen for malaria, consisting of four well-established antimalarial agents: **amodiaquine**, **sulphadoxine**, **pyrimethamine**, and **artesunate**. Each drug targets *Plasmodium* species via different mechanisms, making the combination particularly potent for both treatment and preventive strategies, especially where resistance or high transmission is a concern. - **Amodiaquine** is a 4-aminoquinoline antimalarial that inhibits heme polymerase, interfering with the parasite's ability to detoxify heme[5]. - **Sulphadoxine** and **pyrimethamine** act synergistically as a fixed-dose combination: sulphadoxine inhibits dihydropteroate synthase, and pyrimethamine inhibits dihydrofolate reductase, both disrupting folate synthesis in the parasite[5]. - **Artesunate** is an artemisinin derivative, rapidly reducing parasite biomass by producing free radicals after activation by heme within the parasite, leading to parasite death[7]. This combination is used for both curative and intermittent preventive treatment of uncomplicated *Plasmodium falciparum* malaria and is a mainstay in regions with high transmission and seasonal malaria chemoprevention programs, particularly in Africa[1][2][5]. The drugs have complementary pharmacokinetics and are generally well tolerated when used as recommended. Used together, these agents offer broad coverage and reduce the risk of resistance emergence. This specific four-drug regimen is not a fixed-dose tablet but rather a regimen where the drugs may be administered together as co-packaged or separately dosed treatments.

02

Targets

β-HematinHemeDHFR (Dihydrofolate reductase)DHPS (Dihydropteroate synthase)

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