artefenomel + piperaquine

Artefenomel + piperaquine is an investigational oral fixed-dose combination of two small molecule antimalarial agents developed for the treatment of uncomplicated Plasmodium falciparum malaria. Artefenomel (also known as OZ439) is a synthetic trioxolane with a mechanism similar to artemisinin derivatives, generating reactive oxygen species that damage parasite proteins and membranes. Piperaquine is a bisquinoline antimalarial that interferes with heme detoxification in the parasite’s food vacuole. The combination was designed to provide single-dose cure potential and improve adherence compared to current multi-day regimens. Clinical development targeted both children and adults in Africa and Asia; however, phase 2b trials showed that none of the tested single-dose regimens achieved the target efficacy (>95% PCR-adjusted adequate clinical and parasitological response at day 28), with observed cure rates ranging from approximately 63%–78%. Vomiting was noted as a significant tolerability issue[1][2][4][5].

Other names

artefenomel-piperaquineOZ439-piperaquineOZ-439-piperaquineOZ 439-piperaquineartefenomel plus piperaquine phosphate