Artemisinin

Artemisinin is a natural product, a sesquiterpene lactone with a distinctive peroxide bridge, derived from the plant Artemisia annua, commonly known as sweet wormwood. It is the core component of artemisinin-based combination therapies (ACTs), which pair an artemisinin derivative with a longer-acting partner drug to treat malaria and reduce the risk of resistance. Common derivatives used clinically include artesunate, artemether, and dihydroartemisinin.

Discovery and legacy: Artemisinin was isolated in the early 1970s by You you Tu and colleagues as part of China’s traditional-medicine research program. The discovery drew on ancient texts and modern pharmacology, leading to a highly effective treatment for Plasmodium falciparum malaria. Tu Youyou received the Nobel Prize in Physiology or Medicine in 2015 for discoveries concerning artemisinin.

Mechanism of action and use: The endoperoxide moiety in artemisinin is activated by iron within the parasite, generating reactive radicals that damage multiple parasite proteins and membranes, rapidly reducing parasite biomass. ACTs cure most uncomplicated infections and reduce mortality when used promptly. For severe malaria, intravenous artesunate is preferred over quinine where available.

Resistance and safety: Widespread monotherapy has contributed to reduced efficacy; resistance signals have emerged in some regions, often linked to delayed parasite clearance associated with K13-propeller gene mutations. When used in ACTs, artemisinin derivatives are generally well tolerated, with occasional gastrointestinal or dizziness-related side effects.

Production and supply: Artemisinin is extracted from A. annua, but semi-synthetic production via engineered microorganisms has increased supply stability. Industrial-scale production began in the 2010s, helping meet global demand for malaria treatment.