Environmental and Genetic Factors Affecting Transport of Imatinib by OATP1A2

被引：44

作者：

Eechoute, K. ^{[1
]}

Franke, R. M. ^{[2
]}

Loos, W. J. ^{[1
]}

Scherkenbach, L. A. ^{[2
]}

Boere, I. ^{[1
]}

Verweij, J. ^{[1
]}

Gurney, H. ^{[3
]}

Kim, R. B. ^{[4
]}

Tirona, R. G. ^{[4
]}

Mathijssen, R. H. J. ^{[1
]}

Sparreboom, A. ^{[2
]}

机构：

[1] Erasmus MC, Daniel den Hoed Canc Ctr, Dept Med Oncol, Rotterdam, Netherlands

[2] St Jude Childrens Hosp, Dept Pharmaceut Sci, Memphis, TN 38105 USA

[3] Westmead Hosp, Dept Med Oncol, Sydney, NSW, Australia

[4] Univ Western Ontario, Dept Med, London, ON, Canada

来源：

CLINICAL PHARMACOLOGY & THERAPEUTICS | 2011年 / 89卷 / 06期

关键词：

CANCER RESISTANCE PROTEIN; CHRONIC MYELOID-LEUKEMIA; POLYPEPTIDE; 1A2; BREAST-CANCER; PLASMA-LEVELS; CLINICAL BENEFIT; ROSUVASTATIN; DRUG; PHARMACOKINETICS; PHARMACOGENETICS;

D O I：

10.1038/clpt.2011.42

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The bioavailability of orally administered imatinib is >90%, although the drug is monocationic under the acidic conditions in the duodenum. In vitro, we found that imatinib is transported by the intestinal uptake carrier organic anion transporting polypeptide (OATP1A2) and that this process is sensitive to pH, rosuvastatin, and genetic variants. However, in a study in patients with cancer, imatinib absorption was not associated with OATP1A2 variants and was unaffected by rosuvastatin. These findings highlight the importance of verifying in a clinical setting the drug-transporter interactions observed in in vitro tests.

引用

页码：816 / 820

页数：5

共 25 条

[1] Interaction of methotrexate with organic-anion transporting polypeptide 1A2 and its genetic variants [J].

Badagnani, Ilaria ;

Castro, Richard A. ;

Taylor, Travis R. ;

Brett, Claire M. ;

Huang, Conrad C. ;

Stryke, Douglas ;

Kawamoto, Michiko ;

Johns, Susan J. ;

Ferrin, Thomas E. ;

Carlson, Elaine J. ;

Burchard, Esteban G. ;

Giacomini, Kathleen M. .

JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, 2006, 318 (02) :521-529

[2] Imatinib mesylate (STI571) is a substrate for the breast cancer resistance protein (BCRP)/ABCG2 drug pump [J].

Burger, H ;

van Tol, H ;

Boersma, AWM ;

Brok, M ;

Wiemer, EAC ;

Stoler, G ;

Nooter, K .

BLOOD, 2004, 104 (09) :2940-2942

[3] Imatinib Plasma Levels Are Correlated With Clinical Benefit in Patients With Unresectable/Metastatic Gastrointestinal Stromal Tumors [J].

Demetri, George D. ;

Wang, Yanfeng ;

Wehrle, Elisabeth ;

Racine, Amy ;

Nikolova, Zariana ;

Blanke, Charles D. ;

Joensuu, Heikki ;

von Mehren, Margaret .

JOURNAL OF CLINICAL ONCOLOGY, 2009, 27 (19) :3141-3147

[4] Drug Transporters and Imatinib Treatment: Implications for Clinical Practice [J].

Eechoute, Karel ;

Sparreboom, Alex ;

Burger, Herman ;

Franke, Ryan M. ;

Schiavon, Gaia ;

Verweij, Jaap ;

Loos, Walter J. ;

Wiemer, Erik A. C. ;

Mathijssen, Ron H. J. .

CLINICAL CANCER RESEARCH, 2011, 17 (03) :406-415

[5] Pharmacogenetics of the organic anion transporting polypeptide 1A2 [J].

Franke, Ryan M. ;

Scherkenbach, Lisa A. ;

Sparreboom, Alex .

PHARMACOGENOMICS, 2009, 10 (03) :339-344

[6] Association of enzyme and transporter genotypes with the pharmacokinetics of imatinib [J].

Gardner, Erin R. ;

Burger, Herman ;

van Schaik, Ron H. ;

van Oosterom, Allan T. ;

de Bruijn, Ernst A. ;

Guetens, Gunther ;

Prenen, Hans ;

de Jong, Floris A. ;

Baker, Sharyn D. ;

Bates, Susan E. ;

Figg, William D. ;

Verweij, Jaap ;

Sparreboom, Alex ;

Nooter, Kees .

CLINICAL PHARMACOLOGY & THERAPEUTICS, 2006, 80 (02) :192-201

[7] Membrane transporters in drug development [J].

Giacomini, Kathleen M. ;

Huang, Shiew-Mei ;

Tweedie, Donald J. ;

Benet, Leslie Z. ;

Brouwer, Kim L. R. ;

Chu, Xiaoyan ;

Dahlin, Amber ;

Evers, Raymond ;

Fischer, Volker ;

Hillgren, Kathleen M. ;

Hoffmaster, Keith A. ;

Ishikawa, Toshihisa ;

Keppler, Dietrich ;

Kim, Richard B. ;

Lee, Caroline A. ;

Niemi, Mikko ;

Polli, Joseph W. ;

Sugiyama, Yuicchi ;

Swaan, Peter W. ;

Ware, Joseph A. ;

Wright, Stephen H. ;

Yee, Sook Wah ;

Zamek-Gliszczynski, Maciej J. ;

Zhang, Lei .

NATURE REVIEWS DRUG DISCOVERY, 2010, 9 (03) :215-236

[8] Intestinal drug transporter expression and the impact of grapefruit juice in humans [J].

Glaeser, H. ;

Bailey, D. G. ;

Dresser, G. K. ;

Gregor, J. C. ;

Schwarz, U. I. ;

McGrath, J. S. ;

Jolicoeur, E. ;

Lee, W. ;

Leake, B. F. ;

Tirona, R. G. ;

Kim, R. B. .

CLINICAL PHARMACOLOGY & THERAPEUTICS, 2007, 81 (03) :362-370

[9] Interaction of imatinib mesilate with human P-glycoprotein [J].

Hamada, A ;

Miyano, H ;

Watanabe, H ;

Saito, H .

JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, 2003, 307 (02) :824-828

[10] Drug and bile acid transporters in rosuvastatin hepatic uptake: Function, expression, and pharmacogenetics [J].

Ho, Richard H. ;

Tirona, Rommel G. ;

Leake, Brenda F. ;

Glaeser, Hartmut ;

Lee, Wooin ;

Lemke, Christopher J. ;

Wang, Yi ;

Kim, Richard B. .

GASTROENTEROLOGY, 2006, 130 (06) :1793-1806

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