Drug intelligence / Profile preview

artesunate + sulphadoxine + pyrimethamine + chloroquine

Development stage
Unknown
Lead developer
University of Oxford
Modality
Small Molecules
Administration
Oral
01

Overview

This drug entry refers to a combination of standard-of-care antimalarial regimens used as a comparator in clinical trials conducted by the University of Oxford, specifically in the context of treating malaria in Afghanistan. The regimen consists of artesunate plus sulphadoxine-pyrimethamine (AS+SP) for the treatment of uncomplicated *Plasmodium falciparum* malaria and chloroquine for the treatment of *Plasmodium vivax* malaria. Artesunate is a rapid-acting artemisinin derivative that generates reactive oxygen species and free radicals to damage parasite proteins and membranes. Sulphadoxine and pyrimethamine are antifolate agents that synergistically inhibit dihydropteroate synthase (DHPS) and dihydrofolate reductase (DHFR), respectively, disrupting the parasite's DNA synthesis. Chloroquine acts by interfering with the parasite's ability to detoxify heme into hemozoin within its food vacuole, leading to the accumulation of toxic heme. This specific combination of regimens was evaluated in a Phase 3 trial to compare its efficacy and safety against dihydroartemisinin-piperaquine (Artekin) to support the simplification of national malaria treatment protocols.

Other names
AS+SP and CQArtesunate-Sulphadoxine/Pyrimethamine and Chloroquineartesunate + sulphadoxin + pyrimethamine + chloroquine
02

Targets

HemeDHPS (Dihydropteroate synthase)PfATP6 (Plasmodium falciparum ATP6)DHFR (Dihydrofolate reductase)

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