Target intelligence / Profile preview

Dihydroartemisinin (DHA)

Target
DHA
Molecular classification
Other (Small molecule drug, artemisinin derivative, sesquiterpene lactone)
01

Overview

Dihydroartemisinin is a semi-synthetic derivative and active metabolite of artemisinin, a sesquiterpene lactone isolated from *Artemisia annua*. It is the most potent antimalarial metabolite of the artemisinin derivatives, and it acts rapidly against the erythrocytic stage of *Plasmodium* parasites. Its mechanism of action involves generation of free radicals upon cleavage of its endoperoxide bridge by intra-parasitic iron, leading to multiple damaging reactions within the parasite. Dihydroartemisinin also exhibits potential anti-inflammatory and investigational anti-cancer effects. It is poorly water soluble and mostly used in combination therapies for malaria due to rapid clearance and risk of resistance when used alone.

Other names
ArtenimolDHADihydroqinghaosuCotexinAlaxinalpha-Dihydroartemisinin
02

Mechanism of action

Dihydroartemisinin and artemisinin derivatives undergo activation by iron (heme), generating reactive radicals that cause oxidative stress and damage vital parasite macromolecules, leading to death of malaria parasites.

03

Biological functions

Antimalarial activity (active against erythrocytic stages of *Plasmodium* species)Some anti-inflammatory and potential anti-tumor effects
04

Disease associations

Infection (malaria)Other (investigational for cancer and inflammatory diseases)
05

Safety considerations

Generally well-tolerated, but risks may include neurotoxicity, hemolysis (particularly in G6PD-deficient patients), rare allergic reactions, and potential excipient (e.g., Cremophor EL) toxicity due to poor aqueous solubility.
06

Interacting drugs

Artemether (parent compound, metabolized to DHA)

2 more in the full profile.

07

Biomarkers

None specifically known for Dihydroartemisinin patient selection; efficacy is determined by clinical response and parasite clearance in malaria.

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