Artefenomel + d-alpha-tocopheryl polyethylene glycol 1000 succinate

Artefenomel (OZ439) is a synthetic trioxolane peroxide antimalarial drug candidate designed for single-dose oral cure of malaria. It acts rapidly against all asexual erythrocytic stages of *Plasmodium falciparum* and demonstrates efficacy comparable to artemisinin derivatives. Artefenomel has improved pharmacokinetic properties over earlier peroxides due to stabilization of its peroxide bond, resulting in prolonged blood concentrations and increased half-life. It is being developed primarily for the treatment of malaria in combination with other agents such as piperaquine. TPGS (d-alpha-tocopheryl polyethylene glycol 1000 succinate) is a water-soluble derivative of vitamin E used as a pharmaceutical excipient. It functions as an absorption enhancer and solubilizer for poorly soluble drugs by forming micelles and inhibiting P-glycoprotein-mediated drug efflux, thereby increasing bioavailability and overcoming multidrug resistance. The combination "OZ439 + TPGS" refers to the use of artefenomel formulated with TPGS to improve oral bioavailability in granule or suspension form for easier administration—especially relevant for pediatric populations unable to swallow tablets[1][2][3][4][5][6].

Other names

trioxolane (for OZ439)vitamin E TPGS (for TPGS)