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Antimicrobial Agents and Chemotherapy, October 2006, p. 3504-3506, Vol. 50, No. 10
0066-4804/06/$08.00+0     doi:10.1128/AAC.00708-06
Copyright © 2006, American Society for Microbiology. All Rights Reserved.

Role of P Glycoprotein in Absorption of Novel Antimalarial Drugs{triangledown}

Andrew Crowe,1* Kenneth F. Ilett,2 Harin A. Karunajeewa,2 Kevin T. Batty,1 and Timothy M. E. Davis2

School of Pharmacy, Curtin University of Technology, Perth, Western Australia, Australia,1 School of Medicine and Pharmacology, University of Western Australia, Crawley, Western Australia, Australia2

Received 8 June 2006/ Returned for modification 17 July 2006/ Accepted 8 August 2006

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 µM) and low for naphthoquine (5 µM). With 20 µM naphthoquine, net efflux was blocked, suggesting saturation of the transporter. Piperaquine and dihydroartemisinin were not transported by the system.

* Corresponding author. Mailing address: Curtin University of Technology, School of Pharmacy, GPO Box U1987, Perth, Western Australia 6845, Australia. Phone: (618) 9266 3423. Fax: (618) 9266 2769. E-mail: A.P.Crowe{at}curtin.edu.au.

{triangledown} Published ahead of print on 17 August 2006.

Antimicrobial Agents and Chemotherapy, October 2006, p. 3504-3506, Vol. 50, No. 10
0066-4804/06/$08.00+0     doi:10.1128/AAC.00708-06
Copyright © 2006, American Society for Microbiology. All Rights Reserved.





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