Drug intelligence / Profile preview

artemether

Development stage
Phase 4
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral, Intramuscular
01

Overview

Artemether is a lipid-soluble methyl ether derivative of dihydroartemisinin, which is itself a derivative of artemisinin, a sesquiterpene lactone peroxide found in the plant *Artemisia annua*. It is a potent and rapidly acting antimalarial agent, particularly effective against the blood stages of *Plasmodium falciparum* and *Plasmodium vivax*. The drug's mechanism of action involves the cleavage of its internal endoperoxide bridge by intraparasitic heme iron, leading to the production of highly reactive carbon-centered free radicals. These radicals cause oxidative stress and alkylate various parasite proteins and membranes, ultimately leading to parasite death. Artemether is also thought to inhibit the parasite's calcium pump, PfATP6. It is widely used in clinical practice, often as part of artemisinin-based combination therapies (ACTs) to ensure high cure rates and prevent the emergence of resistance.

Brand names
PalutherGvither
Other names
dihydroartemisinin methyl ether(+)-artemether
02

Targets

Heme

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