Drug intelligence / Profile preview

mefloquine + dihydroartemisinin + piperaquine

Development stage
Unknown
Lead developer
Mahidol Oxford Tropical Medicine Research Unit
Modality
Small Molecules
Administration
Oral
01

Overview

Mefloquine + dihydroartemisinin + piperaquine is an investigational triple artemisinin-based combination therapy (triple ACT) developed by the University of Oxford for the treatment of multidrug-resistant *Plasmodium falciparum* malaria. This combination therapy integrates three small-molecule antimalarial agents with distinct mechanisms: dihydroartemisinin (an artemisinin derivative), piperaquine (a bisquinoline), and mefloquine (a quinoline methanol). Artemisinins act rapidly by generating free radicals and alkylating heme, while piperaquine and mefloquine are long-acting blood schizonticides that interfere with heme detoxification within the parasite's food vacuole. The triple combination is specifically designed to overcome resistance to standard artemisinin-based combination therapies (ACTs) in regions like Southeast Asia. Clinical evaluation has focused on pharmacokinetic interactions and safety, demonstrating that the addition of mefloquine is generally well-tolerated without significantly increasing cardiotoxicity compared to dihydroartemisinin-piperaquine alone.

Other names
triple artemisinin-based combination therapytriple ACTdihydroartemisinin-piperaquine + mefloquine
02

Targets

β-HematinKCNH2 (Voltage-gated potassium channel subfamily H member 2)Heme

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