Target intelligence / Profile preview

Piperaquine

Molecular classification
Small molecule drug, Aminoquinoline, Bisquinoline
01

Overview

Piperaquine is not a molecular therapeutic target like a receptor, enzyme, or transporter; rather, it is a small molecule drug used as an antimalarial agent, typically in combination with dihydroartemisinin[1][9][6]. Therefore, referring to "Piperaquine" as a target is incorrect. Piperaquine is a synthetic aminoquinoline antimalarial drug—specifically, an orally active bisquinoline—that was first synthesized in the 1960s and extensively used in China before resistance and alternative drugs limited its use[1][9][6]. It is commonly employed as part of artemisinin-based combination therapies (ACTs), such as dihydroartemisinin-piperaquine, for treating uncomplicated Plasmodium falciparum malaria in adults and children[4][9][6][10]. Its mechanism of action, which is not completely elucidated, is expected to resemble that of chloroquine—it is believed to inhibit the heme detoxification pathway in the malaria parasite’s food vacuole[9][6]. Piperaquine’s long-lasting activity aids post-treatment prophylaxis and prevents new infections after initial parasite clearance by fast-acting drugs like artemisinin derivatives[4][8]. In summary, Piperaquine is a small molecule antimalarial drug used as part of combination therapies to treat uncomplicated malaria, not a molecular target or receptor. Its listing as a "target" in a structural information schema is incorrect; it should be categorized as a therapeutic agent[1][9][6][4][2].

Other names
PiperaquinePiperaquinoline1,3-Bis(4-(7-chloroquinolin-4-yl)piperazin-1-yl)propaneQuinoline, 4,4'-(1,3-propanediyldi-4,1-piperazinediyl)bis[7-chloro-4085-31-8 (CAS)
02

Mechanism of action

Inhibition of heme detoxification pathway within Plasmodium food vacuole (similar to chloroquine)

03

Disease associations

Malaria
04

Safety considerations

Dose optimization in children, as standard dosing may be subtherapeutic in low-weight populations (risk of resistance development)Risk of resistance in monotherapy; usually administered in combination with artemisinin derivatives to reduce resistanceTolerability and compliance profile favorable compared to some alternativesRare cardiac safety concerns, including QT prolongation
05

Interacting drugs

Dihydroartemisinin

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