Drug intelligence / Profile preview

dihydroartesunate

Development stage
Unknown
Modality
Small Molecules
Administration
Oral, Intravenous, Intramuscular
01

Overview

Dihydroartesunate is an **active metabolite of artesunate and other artemisinin derivatives**, commonly referred to as DHA. It is a **semisynthetic derivative of artemisinin** and serves as the principal antimalarial agent responsible for the activity of artesunate, artemether, and other related drugs. Dihydroartesunate acts rapidly against all erythrocytic stages of Plasmodium species and is widely used, either directly or via its parent prodrugs, as a frontline treatment for *severe malaria*. Its mechanism of action involves generating reactive oxygen species via the cleavage of its endoperoxide bridge upon interaction with heme or ferrous iron in malaria parasites, which disrupts multiple essential parasite proteins and biomolecules, inhibiting protein and nucleic acid synthesis, and alkylating parasitic enzymes such as calcium ATPases and glutathione S-transferases. DHA is considered central to the efficacy and pharmacology of artemisinin-based therapies. It is also under investigation for other therapeutic indications including cancer, antiviral activity, and immunomodulation[1][3][4].

Other names
DHA
02

Targets

PfATP6 (Plasmodium falciparum ATP6)26S proteasome

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