Pharmacokinetics and Therapeutic Applications of Artemisinin

Artemisinin is a sesquiterpene lactone derived from Artemisia annua renowned for its rapid antimalarial action and broad therapeutic potential. Its pharmacokinetic profile is characterised by rapid absorption, extensive first-pass metabolism by cytochrome P450 enzymes and a short terminal elimination half-life, which collectively drive the need for combination regimens and formulation innovations. Variability in oral bioavailability has prompted exploration of plant-based delivery, metabolic inhibitors and micronised preparations to enhance systemic exposure. Auto-induction of metabolic pathways can lead to increasing clearance during multi-day dosing, influencing dosing schedules and drug–drug interaction risk. Beyond malaria, artemisinin and its derivatives exhibit anti-inflammatory, anti-fibrotic and antiproliferative activities, modulating cytokine release, fibroblast function and extracellular matrix remodelling. Such pleiotropic effects suggest applications in conditions ranging from fibrotic skin disorders to certain cancers, though clinical translation requires careful dose optimisation and safety evaluation. Ongoing research seeks to integrate pharmacokinetic insights with novel delivery systems and adjunctive agents to maximise therapeutic index and global impact.

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Pharmacokinetics and Therapeutic Applications of Artemisinin publication trend

The graph below shows the total number of articles in pharmacokinetics and therapeutic applications of artemisinin across all publications each year (not limited to Nature Index journals).

Technical terms

Bioavailability: The fraction of an orally administered dose that reaches systemic circulation in an active form.

Clearance: The volume of plasma from which a drug is completely removed per unit time, reflecting elimination efficiency.

Terminal elimination half-life: The time required for the plasma concentration of a drug to decrease by half during the terminal phase.

Cytochrome P450: A superfamily of liver enzymes responsible for the oxidative metabolism of many xenobiotics, including artemisinin.

Pharmacokinetics: The study of drug movement through absorption, distribution, metabolism and excretion processes.

Fibroblast: A connective-tissue cell that synthesises extracellular matrix components and plays a central role in wound healing and fibrosis.

Matrix metalloproteinase (MMP): A group of zinc-dependent enzymes that degrade extracellular matrix proteins, involved in tissue remodelling and fibrosis.

References

1. Differential Anti-Fibrotic and Remodeling Responses of Human Dermal Fibroblasts to Artemisia sp., Artemisinin, and Its Derivatives. Molecules (2024).
2. Dried Leaf Artemisia Annua Improves Bioavailability of Artemisinin via Cytochrome P450 Inhibition and Enhances Artemisinin Efficacy Downstream. Biomolecules (2020).
3. Auto-induction of phase I and phase II metabolism of artemisinin in healthy Chinese subjects after oral administration of a new artemisinin-piperaquine fixed combination. Malaria Journal (2014).
4. Population pharmacokinetic properties of artemisinin in healthy male Vietnamese volunteers. Malaria Journal (2016).