Drug intelligence / Profile preview

dihydroartemisinin + piperaquine

Development stage
Phase 4
Lead developer
Medicines for Malaria Venture
Modality
Small Molecules
Administration
Oral
01

Overview

Dihydroartemisinin + piperaquine is an oral fixed-dose **artemisinin-based combination therapy** for uncomplicated malaria. Dihydroartemisinin is a rapidly acting artemisinin derivative that is activated in the parasite by heme-associated iron and generates reactive intermediates that damage essential parasite macromolecules. Piperaquine is a long-acting bisquinoline antimalarial that concentrates in the parasite digestive vacuole and interferes with heme detoxification through inhibition of hemozoin formation. The complementary rapid parasite clearance of dihydroartemisinin and prolonged post-treatment activity of piperaquine support both treatment and chemoprevention use. Marketed products include Eurartesim, D-Artepp, Artekin, Duo-Cotecxin, P-Alaxin, Diphos, and TimeQuin. Piperaquine exposure can prolong the QT interval, so cardiac-risk factors and concomitant QT-prolonging medicines require consideration.

Brand names
ArtekinD-ArteppD-Artepp DispersibleDiphosDuo-CotecxinDuocotexinEurartesimP-AlaxinP-Alaxin DispersibleTimeQuin
Other names
artenimol + piperaquineartenimol/piperaquineDHA-PPQDHA-PQDHAPQdihydroartemisinin + piperaquinedihydroartemisinin-piperaquinedihydroartemisinin-piperaquine phosphatedihydroartemisinin-piperaquine tetraphosphatedihydroartemisinin/piperaquinedihydroartemisinin–piperaquinepiperaquine + dihydroartemisininpiperaquine/dihydroartemisinin
02

Targets

Plasmodium falciparum mitochondrial electron transport chain (Pf mETC)Neuraminidase

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