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 microM) and low for naphthoquine (5 microM). With 20 microM naphthoquine, net efflux was blocked, suggesting saturation of the transporter. Piperaquine and dihydroartemisinin were not transported by the system.
Crowe
Andrew
A
Curtin University of Technology, School of Pharmacy, Perth, Western Australia, Australia. A.P.Crowe@curtin.edu.au
Ilett
Kenneth F
KF
Karunajeewa
Harin A
HA
Batty
Kevin T
KT
Davis
Timothy M E
TM
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000378:metabolism*; D000962:Antimalarials / Q000378:metabolism*; D001692:Biological Transport; D018938:Caco-2 Cells / Q000378:metabolism; D006801:Humans; D007408:Intestinal Absorption; D009287:Naphthyridines / Q000378:metabolism
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D000962:Antimalarials; D009287:Naphthyridines; C027871:pyronaridine