Oseltamivir (Tamiflu) efflux transport at the blood-brain barrier via P-glycoprotein

Drug Metabolism and Disposition

Volumn 36, Issue 1, 2008, Pages 6-9

  Morimoto, Kaori ^a   Nakakariya, Masanori ^b   Shirasaka, Yoshiyuki ^b   Kakinuma, Chihaya ^a   Fujita, Takuya ^c   Tamai, Ikumi ^b   Ogihara, Takuo ^a,b  

^a TAKASAKI UNIVERSITY OF HEALTH AND WELFARE   (Japan)

^b TOKYO UNIVERSITY OF SCIENCE   (Japan)

^c RITSUMEIKAN UNIVERSITY   (Japan)

Author keywords

[No Author keywords available]

Indexed keywords

4 ACETAMIDO 5 AMINO 3 (1 ETHYLPROPOXY) 1 CYCLOHEXENE 1 CARBOXYLIC ACID; CYCLOSPORIN A; GLYCOPROTEIN P; OSELTAMIVIR;

ANIMAL EXPERIMENT; APICAL MEMBRANE; ARTICLE; BLOOD BRAIN BARRIER; CONTROLLED STUDY; DRUG ACCUMULATION; DRUG DISTRIBUTION; DRUG PENETRATION; DRUG PROTEIN BINDING; DRUG TRANSPORT; HUMAN; HUMAN CELL; KNOCKOUT MOUSE; MOUSE; NONHUMAN; PRIORITY JOURNAL; SINGLE DRUG DOSE; WILD TYPE;

ANIMALS; ANTIVIRAL AGENTS; ATP-BINDING CASSETTE TRANSPORTERS; BLOOD-BRAIN BARRIER; CELL LINE; CELL MEMBRANE PERMEABILITY; CLONING, MOLECULAR; HUMANS; MALE; MICE; MICE, KNOCKOUT; OSELTAMIVIR; P-GLYCOPROTEINS; TISSUE DISTRIBUTION;

MUS; RATTUS;

EID: 37549037089     PISSN: 00909556     EISSN: 1521009X     Source Type: Journal    
DOI: 10.1124/dmd.107.017699     Document Type: Article

References (15)

1. Demeule M, Régina A, Jodoin J, Laplante A, Dagenais C, Berthelet F, Moghrabi A, and Béliveau R (2002) Drug transport to the brain: key roles for the efflux pump P-glycoprotein in the blood-brain barrier. Vascul Pharmacol 38:339-348.
2. Ebinger M and Uhr M (2006) ABC drug transporter at the blood-brain barrier: effects on drug metabolism and drug response. Eur Arch Psychiatry Clin Neurosci 256:294-298.
3. Hill G, Cihlar T, Oo C, Ho ES, Prior K, Wiltshire H, Barrett J, Liu B, and Ward P (2002) The anti-influenza drug oseltamivir exhibits low potential to induce pharmacokinetic drug interactions via renal secretion-correlation of in vivo and in vitro studies. Drug Metab Dispos 30:13-19.
4. Ishiguro N, Nozawa T, Tsujihata A, Saito A, Kishimoto W, Yokoyama K, Yotsumoto T, Sakai K, Igarashi T, and Tamai I (2004) Influx and efflux transport of H1-antagonist epinastine across the blood-brain barrier. Drug Metab Dispos 32:519-524.
5. Johanson CE (1980) Permeability and vascularity of the developing brain: cerebellum vs cerebral cortex. Brain Res 190:3-16.
6. Li C, Yu Q, Ye Z, Sun Y, He Q, Li Z, Zhang W, Luo J, Gu X, Zheng X, et al. (2007) A nonsynonymous SNP in human cytosolic sialidase in a small Asian population results in reduced enzyme activity: potential link with severe adverse reactions to oseltamivir. Cell Res 17:357-362.
7. Li W, Escarpe PA, Eisenberg EJ, Cundy KC, Sweet C, Jakeman KJ, Merson J, Lew W, Williams M, Zhang L, et al. (1998) Identification of GS 4104 as an orally bioavailable prodrug of the influenza virus neuraminidase inhibitor GS 4071 Antimicrob Agents Chemother 42:647-653.
8. Ogihara T, Kamiya M, Ozaawa M, Fujita T, Yamamoto A, Yamashita S, Ohnishi S, and Isomura Y (2006) What kinds of substrates show P-glycoprotein-dependent intestinal absorption? Comparison of verapamil with vinblastine. Drug Metab Pharmacokinet 21:238-244.
9. Shi D, Yang J, Yang D, LeCluyse EL, LeCluyse CB, Black C, You L, Akhlaghi F, and Yan B (2006) Anti-influenza prodrug oseltamivir is activated by carboxyesterase human 1, and the activation is inhibited by antiplatelet agent clopidgrel. J Pharmacol Exp Ther 319:1477-1484.
10. Shirasaka Y, Sakane T, and Yamashita S (2007) Effect of P-glycoprotein expression levels on the concentration-dependent permeability of drugs to the cell membrane. J Pharm Sci, in press.
11. Tanigawara Y, Okamura N, Hirai M, Yasuhara M, Ueda K, Kioka N, Komano T, and Hori R (1992) Transport of digoxin by human P-glycoprotein expressed in a porcine kidney epithelial cell line (LLC-PK1). J Pharmacol Exp Ther 263:840-845.
12. Tsuji A (1998) P-glycoprotein-mediated efflux transport of anticancer drugs at the blood-brain barrier. Ther Drug Monit 20:588-590.
13. Ueda K, Okamura N, Hirai M, Tanigawara Y, Saeki T, Kioka N, Komano T, and Hori R (1992) Human P-glycoprotein transporters cortisol, aldosterone, and dexamethasone, but not progesterone. J Biol Chem 267:24248-24252.
14. Wiltshire H, Wiltshire B, Citron A, Clarke T, Serpe C, Gray D, and Herron W (2000) Development of a high-performance liquid chromatographic-mass spectrometric assay for the specific and sensitive quantification of Ro 64-0802, an anti-influenza drug, and its pro-drug, oseltamivir, in human and animal plasma and urine. J Chromatogr B Biomed Sci Appl 745:373-388.
15. Yamaoka K, Tanigawara Y, Nakagawa T, and Uno T (1981) A pharmacokinetic analysis program (multi) for microcomputer. J Pharmacobiodyn 4:879-885.