Drug intelligence / Profile preview

piperaquine

Development stage
Phase 4
Modality
Small Molecules
Administration
Oral
01

Overview

Piperaquine is a synthetic bisquinoline antimalarial agent first synthesized in the 1960s and used extensively in China. It is primarily used as part of artemisinin-based combination therapies (ACTs), most notably with dihydroartemisinin for the treatment of uncomplicated malaria caused by *Plasmodium falciparum*. Piperaquine acts by accumulating in the parasite's digestive vacuole and interfering with heme detoxification into hemozoin—a mechanism similar to that of chloroquine—thereby exerting its antiparasitic effect. The drug has a long elimination half-life (2–3 weeks), which provides extended post-treatment prophylaxis against reinfection. Resistance to piperaquine has emerged in Southeast Asia since around 2010. Piperaquine is highly lipid-soluble and exhibits extensive tissue distribution[1][2][3][6].

Brand names
Eurartesim
Other names
Quinoline, 4,4'-(1,3-propanediyldi-4,1-piperazinediyl)bis[7-chloro-
02

Targets

CALR (Calreticulin)PfHRP2 (Plasmodium falciparum histidine-rich protein II)

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