Advances in the research on the targets of anti-malaria actions of artemisinin

Pharmacol Ther. 2020 Dec;216:107697. doi: 10.1016/j.pharmthera.2020.107697. Epub 2020 Oct 6.


Malaria has been a global epidemic health threat since ancient times. It still claims roughly half a million lives every year in this century. Artemisinin and its derivatives, are frontline antimalarial drugs known for their efficacy and low toxicity. After decades of wide use, artemisinins remain our bulwark against malaria. Here, we review decades of efforts that aim to understand the mechanism of action (MOA) of artemisinins, which help explain the specificity and potency of this anti-malarial drug. We summarize the methods and approaches employed to unravel the MOA of artemisinin over the last three decades, showing how the development of advanced techniques can help provide mechanistic insights and resolve some long-standing questions in the field of artemisinin research. We also provide examples to illustrate how to better repurpose artemisinins for anti-cancer therapies by leveraging on MOA. These examples point out a practical direction to engineer artemisinin for broader applications beyond malaria.

Keywords: Anti-malaria; Artemisinin; Mechanism of action; Repurpose of artemisinin.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Antimalarials / adverse effects
  • Antimalarials / therapeutic use*
  • Antineoplastic Agents / adverse effects
  • Antineoplastic Agents / therapeutic use*
  • Artemisinins / adverse effects
  • Artemisinins / therapeutic use*
  • Drug Repositioning*
  • Host-Parasite Interactions
  • Humans
  • Malaria / drug therapy*
  • Malaria / metabolism
  • Malaria / parasitology
  • Neoplasms / drug therapy*
  • Neoplasms / metabolism
  • Neoplasms / pathology
  • Plasmodium / drug effects*
  • Plasmodium / pathogenicity


  • Antimalarials
  • Antineoplastic Agents
  • Artemisinins
  • artemisinin