The orally administered P-glycoprotein inhibitor R101933 does not alter the plasma pharmacokinetics of docetaxel

Clinical Cancer Research

Volumn 6, Issue 4, 2000, Pages 1365-1371

  Van Zuylen, Lia ^a   Sparreboom, Alex ^a   Van Der Gaast, Ate ^a   Van Der Burg, Maria E L ^a   Van Beurden, Vera ^a   Bol, Cornelis J ^b   Woestenborghs, Robert ^b   Palmer, Peter A ^b   Verweij, Jaap ^a  

^a ERASMUS MC CANCER INSTITUTE   (Netherlands)

^b JANSSEN RESEARCH FOUNDATION   (Belgium)

Author keywords

[No Author keywords available]

Indexed keywords

DOCETAXEL; GLYCOPROTEIN P; LANIQUIDAR; PROTEIN INHIBITOR; UNCLASSIFIED DRUG;

ADULT; ARTICLE; CLINICAL ARTICLE; CLINICAL TRIAL; DRUG BLOOD LEVEL; FEMALE; FEVER; HUMAN; MALE; MAXIMUM PERMISSIBLE DOSE; MUCOSA INFLAMMATION; NEUTROPENIA; PHASE 1 CLINICAL TRIAL; PLASMA CLEARANCE; PRIORITY JOURNAL; SOLID TUMOR;

ADMINISTRATION, ORAL; ADULT; AGED; ANTINEOPLASTIC AGENTS, PHYTOGENIC; AREA UNDER CURVE; BENZAZEPINES; DOSE-RESPONSE RELATIONSHIP, DRUG; FATIGUE; FEMALE; HUMANS; MALE; MIDDLE AGED; MOUTH MUCOSA; NEOPLASMS; NEUTROPENIA; P-GLYCOPROTEIN; PACLITAXEL; QUINOLINES; STOMATITIS; TAXOIDS; VOMITING;

EID: 0034006531     PISSN: 10780432     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (29)

1. Leighton, J. C., and Goldstein, L. J. P-glycoprotein in adult solid tumors. Expression and prognostic significance. Hematol. Oncol. Clin. N. Am., 9: 251-271, 1995.
2. Bradshaw, D. M., and Arceci, R. J. Clinical relevance of transmembrane drug efflux as a mechanism of multidrug resistance. J. Clin. Oncol., 16: 3674-3690, 1998.
3. Ford, J. M., and Hait, W. N. Pharmacology of drugs that alter multidrug resistance in cancer. Pharm. Rev., 42: 155-199, 1990.
4. Kaye, S. B. Reversal of multidrug resistance. Cancer Treat. Rev., 17 (Suppl. A): 37-43, 1990.
5. Raderer, M., and Scheithauer, W. Clinical trials of agents that reverse multidrug resistance. Cancer (Phila.), 73: 3553-3563, 1993.
6. Relling, M. V. Are the major effects of P-glycoprotein modulators due to altered pharmacokinetics of anticancer drugs? Ther. Drug Monit., 18: 350-356, 1996.
7. Pastan, I., and Gottesman, M. M. Multidrug resistance. Annu. Rev. Med., 42: 277-286, 1991.
8. Twentyman, P. R. MDR1 (P-glycoprotein) gene expression - implications for resistance modifier trials. J. Natl. Cancer Inst., 84: 1458-1460, 1992.
9. Van Zuylen, L., Nooter, K., Sparreboom, A., and Verweij, J. Development of multidrug-resistance converters: sense or nonsense? Invest. New Drugs, in press, 1999.
10. Wouters, W., Janssens F., van Dun, J., Krekels, M., and Smets, G. R101933 is an antagonist of Pgp and modulates resistance to different chemotherapy agents. Proc. Am. Assoc. Cancer Res., 40: 4374, 1999.
11. Van Ginckel, R., Floren, W., Moelans, P., Janssens, B., Moelenberghs, K., and Wouters, W. Oral treatment with R101933 restores the sensitivity towards paclitaxel and Adriamycin in resistant human tumors xenografted in athymic mice. Proc. Am. Assoc. Cancer Res., 40: 4375, 1999.
12. Fulton, B., and Spencer, C. M. Docetaxel: a review of its pharmacodynamic and pharmacokinetic properties and therapeutic efficacy in the management of metastatic breast cancer. Drugs, 5: 1075-1092, 1996.
13. Ringel, I., and Horwitz, S. B. Studies with RP 56976 (Taxotere): a semisynthetic analogue of Taxol. J. Natl. Cancer Inst., 83: 288-291, 1991.
14. Sparreboom, A., Van Zuylen, C., Brouwer, E., Loos, W. J., De Bruijn, P., Gelderblom, A. J., Pillay, M., Nooter, K., Stoter, G., and Verweij, J. Cremophor EL-mediated alteration of paclitaxel distribution in human blood: clinical pharmacokinetic implications. Cancer Res., 59: 1454-1457,1999.
15. Van Asperen, J., Sparreboom, A., Van Tellingen, O., and Beijnen, J. H. Cremophor EL masks the effect of mdr1a P-glycoprotein on the plasma pharmacokinetics of paclitaxel in mice. In: J. van Asperen (ed.). The Pharmacological Role of Drug-transporting P-glycoproteins in Mice (Thesis), Chap. 3.2, pp. 109-124. Utrecht, the Netherlands: Utrecht University, 1998.
16. Willey, T. A., Bekos, E. J., Gaver, R. C., Duncan, G. F., Tay, L. K., Beijnen, J. H., and Farmen, R. H. High-performance liquid chromatographic procedure for the quantitative determination of paclitaxel (Taxol) in human plasma. J. Chromatogr., 621: 231-238, 1993.
17. Gibaldi, M., and Perier, D. Pharmacokinetics, 2nd ed. New York: Marcel Dekker, Inc., 1982.
18. Clarke, S. J., and Rivory, L. P. Clinical pharmacokinetics of docetaxel. Clin. Pharmacokinet., 36: 99-114, 1999.
19. Altman, D. G. Practical Statistics for Medical Research, pp. 440-476. London: Chapman & Hall, 1994.
20. Van Zuylen, L., Verweij, J., Nooter, K., Brouwer, E., Stoter, G., and Sparreboom, A. Role of intestinal MDR1 P-glycoprotein in the plasma disposition and fecal elimination pathways of docetaxel in humans. Clin. Cancer Res., 5 (Suppl.): 3834, 1999.
21. Berg, S. L., Tolcher, A., O'Shaughnessy, J. A., Denicoff, A. M., Noone, M., Ognibene, F. P., Cowan, K. H., and Balis, F. M. Effect of r-verapamil on the pharmacokinetics of paclitaxel in women with breast cancer. J. Clin. Oncol., 13: 2039-2042, 1995.
22. Sarris, A. H., Younes, A., McLaughlin, P., Moore, D., Hagemeister, F., Swan, F., Rodriguez, M. A., Romaguera, J., North, L., Mansfield, P., Callendar, D., Mesina, O., and Cabanillas, F. Cyclosporin A does not reverse clinical resistance to paclitaxel in patients with relapsed non-Hodgkin's lymphoma. J. Clin. Oncol., 14: 233-239, 1996.
23. Fields, A., Hochster, H., Runowicz, C., Speyer, J., Goldberg, G., Cohen, C., Dottino, P., Wadler, S., Berk, G., Gretz, H., Mandeli, J., Holland, J., and Letvak, L. PSC833: initial clinical results in refractoty ovarian cancer patients. Curr. Opin. Oncol., 10 (Suppl. 1): S21, 1998.
24. Rowinsky, E. K., Smith, L., Wang, Y-M., Chaturvedi, P., Villalona, M., Campbell, E., Aylesworth, C., Eckhardt, S. G., Hammond, L., Kraynak, M., Drgengler, R., Stephenson, J., Harding, M. W., and Von Hoff, D. D. Phase I and pharmacokinetic study of paclitaxel in combination with biricodar, a novel agent that reverses multidrug resistance conferred by overexpression of both MDR1 and MRP. J. Clin. Oncol., 16: 2964-2976, 1998.
25. Royer, L, Monsarrat, B., Sonnier, M., Wright, M., and Cresteil, T. Metabolism of docetaxel by human cytochromes P450: interactions with paclitaxel and other antineoplastic drugs. Cancer Res., 56: 58-65, 1996.
26. Marre, F., Sanderink, G. J., De Souza, G., Martinet, M., and Rahmanui, R. Hepatic biotransformation of docetaxel (Taxotere) in vitro: involvement of the CYP3A subfamily in humans. Cancer Res., 56: 1296-1302, 1996.
27. Sparreboom, A., Van Tellingen, O., Scherenburg, E. J., Boesen, J. J. B., Huizing, M. T., Nooijen, W. J., Versluis, C., and Beijnen, J. H. Isolation, purification and biological activity of major docetaxel metabolites from human feces. Drug Metab. Dispos., 24: 655-661, 1996.
28. Commerçon, A., Bourzat, J. D., Bézard, D., and Vuilhorgne, M. Partial synthesis of major metabolites of docetaxel. Tetrahedron, 50: 10289-10298, 1994.
29. Trudeau, M. E. Docetaxel (Taxotere). An overview of first line monotherapy. Semin. Oncol., 22 (Suppl. 13): 17-21, 1995.