Journal of Clinical Oncology, Vol 20, Issue 13
(July), 2002: 2943-2950
© 2002 American Society for Clinical Oncology
Increased Oral Bioavailability of Topotecan in Combination With the Breast Cancer Resistance Protein and P-Glycoprotein Inhibitor GF120918
By C. M.F. Kruijtzer,
J. H. Beijnen,
H. Rosing,
W. W. ten Bokkel Huinink,
M. Schot,
R. C. Jewell,
E. M. Paul,
J. H.M. Schellens
From the Department of Medical Oncology, the Netherlands Cancer Institute/Antoni van Leeuwenhoek Hospital; Department of Pharmacy and Pharmacology, the Netherlands Cancer Institute/Slotervaart Hospital, Amsterdam; Division of Drug Toxicology, Faculty of Pharmacy, Utrecht University, Utrecht, the Netherlands; and GlaxoSmithKline, Research Triangle Park, NC.
Address reprint requests to J.H.M. Schellens, MD, PhD, Department of Medical Oncology, the Netherlands Cancer Institute, Plesmanlaan 121, 1066 CX, Amsterdam, the Netherlands; email: jhm{at}nki.nl
PURPOSE: We discovered that breast cancer resistance protein (BCRP), a recently identified adenosine triphosphate–binding cassette drug transporter, substantially limits the oral bioavailability of topotecan in mdr1a/1b(-/-) P-glycoprotein (P-gp) knockout and wild-type mice. GF120918 is a potent inhibitor of BCRP and P-gp. The aim was to increase the bioavailability of topotecan by GF120918.
PATIENTS AND METHODS: In cohort A, eight patients received 1.0 mg/m2 oral topotecan with or without coadministration of one single oral dose of 1,000 mg GF120918 (day 1 or day 8). In cohort B, eight other patients received 1.0 mg/m2 intravenous topotecan with or without 1,000 mg oral GF120918 to study the effect of GF120918 on the systemic clearance of topotecan.
RESULTS: After oral topotecan, the mean area under the plasma concentration-time curve (AUC) of total topotecan increased significantly from 32.4 ± 9.6 µg·h/L without GF120918 to 78.7 ± 20.6 µg·h/L when GF120918 was coadministered (P = .008). The mean maximum plasma concentration of total topotecan increased from 4.1 ± 1.5 µg/L without GF120918 to 11.5 ± 2.4 µg/L with GF120918 (P = .008). The apparent bioavailability in this cohort increased significantly from 40.0% (range, 32% to 47%) to 97.1% (range, 91% to 120%) (P = .008). Interpatient variability of the apparent bioavailability was 17% without and 11% with GF120918. After intravenous administration of topotecan, coadministration of oral GF120918 had a small but statistically significant effect on the AUC and systemic clearance of total topotecan but no statistically significant effect on maximum plasma concentration and terminal half-life of total topotecan.
CONCLUSION: Coadministration of the BCRP and P-gp inhibitor GF120918 resulted in a significant increase of the systemic exposure of oral topotecan. The apparent oral bioavailability increased from 40.0% without to 97.1% with GF120918.
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R. W. Robey, K. Steadman, O. Polgar, K. Morisaki, M. Blayney, P. Mistry, and S. E. Bates
Pheophorbide a Is a Specific Probe for ABCG2 Function and Inhibition
Cancer Res.,
February 15, 2004;
64(4):
1242 - 1246.
[Abstract]
[Full Text]
[PDF]
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A. E. van Herwaarden, J. W. Jonker, E. Wagenaar, R. F. Brinkhuis, J. H. M. Schellens, J. H. Beijnen, and A. H. Schinkel
The Breast Cancer Resistance Protein (Bcrp1/Abcg2) Restricts Exposure to the Dietary Carcinogen 2-Amino-1-methyl-6-phenylimidazo[4,5-b]pyridine
Cancer Res.,
October 1, 2003;
63(19):
6447 - 6452.
[Abstract]
[Full Text]
[PDF]
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G. D. Leonard, T. Fojo, and S. E. Bates
The Role of ABC Transporters in Clinical Practice
Oncologist,
October 1, 2003;
8(5):
411 - 424.
[Abstract]
[Full Text]
[PDF]
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Z.-S. Chen, R. W. Robey, M. G. Belinsky, I. Shchaveleva, X.-Q. Ren, Y. Sugimoto, D. D. Ross, S. E. Bates, and G. D. Kruh
Transport of Methotrexate, Methotrexate Polyglutamates, and 17{beta}-Estradiol 17-({beta}-D-glucuronide) by ABCG2: Effects of Acquired Mutations at R482 on Methotrexate Transport
Cancer Res.,
July 15, 2003;
63(14):
4048 - 4054.
[Abstract]
[Full Text]
[PDF]
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F. Van Bambeke, J.-M. Michot, and P. M. Tulkens
Antibiotic efflux pumps in eukaryotic cells: occurrence and impact on antibiotic cellular pharmacokinetics, pharmacodynamics and toxicodynamics
J. Antimicrob. Chemother.,
May 1, 2003;
51(5):
1067 - 1077.
[Full Text]
[PDF]
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J. D. Allen, S. C. van Dort, M. Buitelaar, O. van Tellingen, and A. H. Schinkel
Mouse Breast Cancer Resistance Protein (Bcrp1/Abcg2) Mediates Etoposide Resistance and Transport, but Etoposide Oral Availability Is Limited Primarily by P-glycoprotein
Cancer Res.,
March 15, 2003;
63(6):
1339 - 1344.
[Abstract]
[Full Text]
[PDF]
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Y. Sugimoto, S. Tsukahara, Y. Imai, Y. Sugimoto, K. Ueda, and T. Tsuruo
Reversal of Breast Cancer Resistance Protein-mediated Drug Resistance by Estrogen Antagonists and Agonists
Mol. Cancer Ther.,
January 1, 2003;
2(1):
105 - 112.
[Abstract]
[Full Text]
[PDF]
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C.M.F. Kruijtzer, J.H. Beijnen, and J.H.M. Schellens
Improvement of Oral Drug Treatment by Temporary Inhibition of Drug Transporters and/or Cytochrome P450 in the Gastrointestinal Tract and Liver: An Overview
Oncologist,
December 1, 2002;
7(6):
516 - 530.
[Abstract]
[Full Text]
[PDF]
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J. W. Jonker, M. Buitelaar, E. Wagenaar, M. A. van der Valk, G. L. Scheffer, R. J. Scheper, T. Plosch, F. Kuipers, R. P. J. O. Elferink, H. Rosing, et al.
The breast cancer resistance protein protects against a major chlorophyll-derived dietary phototoxin and protoporphyria
PNAS,
November 26, 2002;
99(24):
15649 - 15654.
[Abstract]
[Full Text]
[PDF]
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G. Hudes
Boosting Bioavailability of Topotecan: What Do We Gain?
J. Clin. Oncol.,
July 1, 2002;
20(13):
2918 - 2919.
[Full Text]
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