Role of P glycoprotein in absorption of novel antimalarial drugs

Bidirectional transport of four novel antimalarial compounds was determined using Caco-2 cell monolayers. P glycoprotein-mediated efflux was greatest for pyronaridine (5 to 20 mu M) and low for naphthoquine (5 mu M). With 20 mu M naphthoquine, net efflux was blocked, suggesting saturation of the transporter. Piperaquine and dihydroartemisinin were not transported by the system.