Drug intelligence / Profile preview

artesunate + mefloquine + piperaquine

Development stage
Phase 3
Lead developer
Drugs for Neglected Diseases initiative
Modality
Small Molecules
Administration
Oral, Parenteral, Intravenous, Intramuscular
01

Overview

This is a triple combination antimalarial therapy consisting of artesunate, mefloquine, and piperaquine. Each component is a small molecule antimalarial with distinct mechanisms of action: - **Artesunate** is an artemisinin derivative that rapidly reduces parasite biomass by generating reactive oxygen species and damaging parasite proteins. - **Mefloquine** is a quinoline methanol that interferes with the parasite's ability to detoxify heme, leading to toxic buildup within the Plasmodium cell. - **Piperaquine** is a bisquinoline compound that also inhibits heme detoxification in malaria parasites. The combination aims to enhance efficacy against multidrug-resistant *Plasmodium falciparum* by combining fast-acting (artesunate) and long-acting (mefloquine, piperaquine) agents. This approach may help delay resistance development and improve cure rates in regions where resistance to artemisinin-based therapies has emerged[6]. The safety profile reflects those of the individual components; drug-drug interactions are possible as both mefloquine and piperaquine are metabolized by CYP3A4[6].

Other names
artesunate plus mefloquine plus piperaquine
02

Targets

β-HematinPlasmodium falciparum redox network proteinsPfHRP2 (Plasmodium falciparum histidine-rich protein II)

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