Small molecule
PubChem CID 6917864
Artesunate
Artesunate for Injection
- Mechanism of action
- Endoperoxide-mediated oxidative damage (antimalarial)
- In plain language
- Breaks apart inside malaria parasites when it contacts the iron they release from digesting blood, creating destructive molecules that kill the parasite from within.
- How it works
- Artesunate is a semisynthetic derivative of artemisinin, the sesquiterpene lactone first isolated from Artemisia annua. Following intravenous administration, artesunate is rapidly hydrolyzed by blood esterases to its active metabolite, dihydroartemisinin (DHA). Both artesunate and DHA retain the parent compound's endoperoxide bridge — an unusual oxygen-oxygen bond rarely found in bioactive natural products. Inside the malaria parasite, this bridge is cleaved by heme iron released as the parasite digests host hemoglobin, generating reactive carbon-centered free radicals that alkylate parasite proteins and other biomolecules, producing oxidative stress, inhibition of protein and nucleic acid synthesis, and ultrastructural damage that halts parasite growth.
- Therapeutic applications
- Per FDA-approved labeling, Artesunate for Injection is indicated for the initial treatment of severe malaria in adult and pediatric patients, and must always be followed by a complete course of an appropriate oral antimalarial regimen. It does not treat the hypnozoite liver-stage forms of Plasmodium and therefore does not prevent relapse due to P. vivax or P. ovale; concomitant therapy with an 8-aminoquinoline agent is required for those species.
- Class
- Small molecule
- Therapeutic area
- Antimalarial
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