Oral topotecan given once or twice daily for ten days: A Phase I pharmacology study in adult patients with solid tumors

Clinical Cancer Research

Volumn 4, Issue 5, 1998, Pages 1153-1158

  Gerrits, Cees J H ^a   Burris, Howard ^b   Schellens, Jan H M ^a   Eckardt, John R ^b   Planting, Andre S T ^a   Van Der Burg, Maria E L ^a   Rodriguez, Gayle I ^b   Loos, Walter J ^a   Van Beurden, Vera ^a   Hudson, Ian ^c   Fields, Scott ^c   Von Hoff, Dan D ^b   Verweij, Jaap ^a  

^a ERASMUS MC CANCER INSTITUTE   (Netherlands)

^b University of Texas Health Science Center at San Antonio   (United States)

^c GLAXOSMITHKLINE   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

TOPOTECAN;

ADULT; AGED; ANOREXIA; AREA UNDER THE CURVE; ARTICLE; BONE MARROW TOXICITY; CLINICAL ARTICLE; CLINICAL TRIAL; CONTROLLED STUDY; DIARRHEA; DOSE RESPONSE; DRUG BLOOD LEVEL; FATIGUE; FEMALE; HUMAN; MALE; NAUSEA; ORAL DRUG ADMINISTRATION; PHASE 1 CLINICAL TRIAL; PRIORITY JOURNAL; SOLID TUMOR; THROMBOCYTOPENIA; VOMITING;

ADMINISTRATION, ORAL; ADULT; AGED; AGED, 80 AND OVER; ANTINEOPLASTIC AGENTS; DRUG ADMINISTRATION SCHEDULE; FEMALE; HEMATOLOGIC DISEASES; HUMANS; MALE; MIDDLE AGED; NEOPLASMS; TOPOTECAN;

EID: 15444361370     PISSN: 10780432     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (43)

1. Kingsburry, W. D., Boehm, J. C., Jakas, D. R., Holden, K. G., Hecht, S. M., Gallagher, G., Caranfa, M. J., McCabe, F. L., and Johnson, R. K. Synthesis of water soluble (aminoalkyl) camptothecin analogues: inhibition of topoisomerase I and antitumor activity. J. Med. Chem., 34: 98-107, 1991.
2. Champoux, J. Evidence from an intermediate with a single strand break in the reaction catalyzed by the DNA untwisting enzyme. Proc. Natl. Acad. Sci. USA, 73: 3488-3491, 1976.
3. Camilloni, G., Di Martino, E., Caserta, M., and Di Mauro, E. Eukaryotic DNA topoisomerase I is topology dependent. Nucleic Acids Res., 16: 7071-7085, 1988.
4. Camilloni, G., Di Martino, E., Di Mauro, E., and Caserta, M. Regulation of the function of eukaryotic DNA topoisomerase I: topological conditions for inactivity. Proc. Natl. Acad. Sci. USA, 86: 3080-3084, 1989.
5. Muller, M. Quantitation of eukaryotic topoisomerase I reactivity with DNA: preferential cleavage of supercoiled DNA. Biochim. Biophys. Acta, 824: 263-267, 1985.
6. Muller, M., Pfund, W., Metha, V., and Trask, D. Eukaryotic type I isomerase is enriched in the nucleolus and catalytically active on ribosomal DNA. EMBO J., 4: 1237-1243, 1985.
7. Hsiang, Y. H., Hertzberg, R., Hecht, S., and Liu, L. Camptothecin induces protein-linked DNA breaks via mammalian DNA topoisomerase I. J. Biol. Chem., 260: 14873-14878, 1985.
8. Hsiang, Y. H., and Liu, L. F. Identification of mammalian DNA topoisomerase I as an intracellular target of the anticancer drug camptothecin. Cancer Res., 48: 1722-1726, 1988.
9. Rowinsky, E. K., Grochow, L. B., Hendricks, C. B., Ettinger, D. S., Forastiere, A. A., Hurowitz, L. A., McGuire, W. P., Sartorius, S. E., Lubejko, B. G., Kaufmann, S. H., and Donehower, R. C. Phase I and pharmacologic study of topotecan: a novel topoisomerase I inhibitor. J. Clin. Oncol., 10: 647-656, 1992.
10. Van Warmerdam, L. J. C., Verweij, J., Schellens, J. H. M., Rosing, H., Davies, B. E., de Boer-Dennert, M., Macs, R. A. A., and Beijnen, J. H. Pharmacokinetics and pharmacodynamics of topotecan administered in a daily times five regimen every three weeks. Cancer Chemother. Pharmacol., 35: 237-245, 1995.
11. Verweij, J., Lund, B., Beijnen, J. H., Planting, A. S. T., De Boer-Dennert, M., Koier, I., Rosing, H., and Hansen, H. Phase I and pharmacokinetic study of topotecan, a new topoisomerase I inhibitor. Ann. Oncol., 4: 673-678, 1993.
12. Saltz, L., Sirott, M., Young, C., Tong, W., Niedzwiecki, D., Tzy-Jyun, Y., Tao, Y., Trochowski, B., Wright, P., Barbosa, K., Toomasi, F., and Kelsen, D. Phase I clinical and pharmacology study of topotecan given daily for 5 consecutive days to patients with advanced solid tumors, with attempt at dose intensification using recombinant granulocyte colony-stimulating factor. J. Natl. Cancer Inst. (Bethesda), 85: 1499-1507, 1993.
13. Creemers, G. J., Bolis, G., Gore, M., Scarfone, G., Lacave, A. J., Guastall, J. P., Despax, R., Favalli, G., Kleinberg, R., Van Belle, S., Hudson, I., Verweij, J., and Ten Bokkel Huinink, W. W. Topotecan, an active drug in the second-line treatment of epithelial ovarian cancer: results of a large European Phase II study. J. Clin. Oncol., 14: 3056-3061, 1996.
14. Malmstrom, H., Sorbe, B., and Simonsen, E. The effect of topotecan in platinum refractory ovarian cancer. Proc. Am. Soc. Clin. Oncol. Annu. Meet., 15: 299, 1996.
15. Wanders, J., Ardizanni, A., Hansen, H. H., Dombernowsky, P., Postmus, P. E., Buitenhuis, M., McDonald, M., Giaccone, G., and Verweij, J. Phase II study of topotecan in refractory and sensitive small cell lung cancer (SCLC). Proc. Am. Assoc. Cancer Res., 36: 237, 1995.
16. Schiller, J. H., Kim, K., and Johnson, D. Phase II study of topotecan in extensive stage small cell lung cancer. Proc. Am. Soc. Clin. Oncol. Annu. Meet., 13: 330, 1994.
17. Kudelka, A., Edwards, C., Freedman, R., Wallin, B., Hord, M., Howell, E., Harper, K., Raber, M., and Kavanagh, J. An open Phase II study to evaluate the efficacy and toxicity of topotecan administered intravenously as 5 daily infusions every 21 days to women with advanced epithelial ovarian carcinoma. Proc. Am. Soc. Clin. Oncol. Annu. Meet., 12: 259, 1993.
18. Armstrong, D., Rowinsky, E., Donehower, R., Rosenshein, N., Walczak, J., and McGuire, W. A Phase II trial of topotecan as salvage therapy in epithelial ovarian cancer. Proc. Am. Soc. Clin. Oncol. Annu. Meet., 14: 275, 1995.
19. Carmichael, J., Gordon, A., Malfetano, J., Gore, M., Spaczynski, M., Davidson, N., Savage, J., Clarke Pearson, D., Hudson, I., Broom, C., and Ten Bokkel Huinink, W. Toptecan, a new active drug vs paclitaxel in advanced epithelial ovarian carcinoma: international topotecan study group trial. Proc. Am. Soc. Clin. Oncol. Annu. Meet., 15: 283, 1996.
20. Phillips, P. C., Janss, A., Kaufmann, S. H., Levow, C., Yao, Y., and Calvin, O. M. Topoisomerase I inhibitor schedule dependent activity and determinants of cytotoxicity in human brain tumor cell lines. Proc. Am. Assoc. Cancer Res., 35: 363, 1994.
21. Pantazis, P., Kozielski, A. J., Vardeman, D. M., Petry, E. R., and Giovanella, B. C. Efficacy of camptothecin cogeners in the treatment of human breast carcinoma xenografts. Oncol. Res., 5: 273-281, 1993.
22. Giovanella, B. C., Stehlin, J. S., Hinz, H. R., Vardeman, D., Mendoza, J. T., and Potmesil, M. Studies of time/dose intensity in treatment of human cancer xenografts with camptothecin analogues. Proc. Am. Assoc. Cancer Res., 35: 455, 1994.
23. Burris, H. A., Hanauske, A. R., Johnson, R. K., Mashall, M. H., Kuhn, J. G., Hilsenbeck, S. G., and Von Hoff, D. D. Activity of topotecan a new topoisomerase I inhibitor against human tumor colony forming units in vitro. J. Natl. Cancer Inst. (Bethesda), 23: 1816-1820, 1992.
24. Houghton, P. J., Chesine, P. J., Myer, L., Stewart, C. F., Synold, T. W., and Houghton, J. A. Evaluation of 9-dimethylaminomethyl-10-hydroxy-camptothecin (topotecan) against xenografts derived from adult and childhood tumors. Cancer Chemother. Pharmacol., 31: 229-239, 1991.
25. Houghton, P. J., Chesire, P. J., Hallman, J. D., Lutz, L., Friedman, H. S., Danks, M. K., and Houghton, J. A. Efficacy of topoisomerase I inhibitor topotecan and irinotecan administered at low dose levels in protracted schedules to mice bearing xenografts of human tumors. Cancer Chemother. Pharmacol., 36: 393-403, 1995.
26. Hochster, H., Liebes, L., Speyer, J., Sorich, J., Taubes, B., Oratz, R., Wernz, J., Chachoua, A., Raphael, B., Vinci, R. Z., and Blum, R. H. Phase I trial of low-dose continuous topotecan infusion in patients with cancer: an active and well-tolerated regimen. J. Clin. Oncol., 12: 553-559, 1994.
27. Kuhn, J., Rizzo, J., Eckardt, J., Fields, S., Cobb, P., Rodriguez, G., Rinaldi, D., Drengler, R., Smith, L., Peacock, N., Thurman, A., Dela-Cruz, P., Hodges, S., Von Hoff, D., and Burris, H. Phase I bioavailability study of oral topotecan. Proc. Am. Soc. Clin. Oncol. Annu. Meet., 14: 474, 1995.
28. Schellens, J. H. M., Creemers, G. J., Beynen, J. H., Rosing, H., de Boer-Dennert, M., McDonald, M., Davies. B., and Verweij, J. Bioavailability and pharmacokinetics of oral topotecan: a new topoisomerase I inhibitor. Br. J. Cancer, 73: 1268-1271, 1996.
29. Creemers, G. J., Gerrits, C. J. H., Eckardt, J. R., Schellens, J. H. M., Burris, H. A., Planting, A. S. T., Rodriguez, G. I., Loos, W. J., Hudson, I., Broom, C., Verweij, J., and Von Hoff, D. D. Phase I and pharmacologic study of oral topotecan administered twice daily for 21-days to adult patients with solid tumors. J. Clin. Oncol., 15: 1071-1079, 1997.
30. Hochster, H., Liebes, L., Zleniuch-Jacquotte, A., Speyer, J., Oratz, R., Wernz, J., Sorich, J., Taubes, B., Vinci, R. Z., Kim, A., Fry, D., Blum, R., and Potmesil, M. Progressive cleavable complex formation with 21-day topotecan infusion: a Phase I/Pharmacodynamic study. Proc. Am. Soc. Clin. Oncol. Annu. Meet., 14: 463, 1995.
31. National Cancer Institute, Division of Cancer Treatment. Guidelines for Reporting of Adverse Drug Reactions. Bethesda, Maryland: National Cancer Institute, 1988.
32. WHO. WHO handbook for reporting results of cancer treatment. WHO Offset Publ. No. 40. Geneva: WHO, 1979.
33. Loos, W. J., Stoter, G., Verweij, J., and Schellens, J. H. M. Sensitive high-performance liquid chromatographic fluorescence assay for the quantitation of topotecan (SKF 104864-A) and the lactone ring-opened product (hydroxy-acid) in human plasma and urine. J. Chromatogr. B Biomed. Appl., 678: 309-315, 1996.
34. Holford, N. H., and Scheiner, L. B. Understanding the dose-effect relationship: clinical application of pharmacokinetic-pharmacodynamic models. Clin. Pharmacokinet., 6: 242-247, 1981.
35. Dancey, J., and Eisenhauer, E. A. Current perspectives on camptothecins in cancer treatment. Br. J. Cancer., 74: 327-338, 1996.
36. Creemers, G. J., Lund, B., and Verweij, J. J. Topoisomerase I inhibitors: topotecan and irinotecan. Cancer Treat. Rev., 20: 73-96, 1994.
37. Creemers, G. J., Gerrits, C. J. H., Schellens, J. H. M., Planting, A. S. T., van der Burg, M. E. L., van Beurden, V. M., de Boer-Dennert, M., Harteveld, M., Loos, W., Hudson, I., Stoter, G., and Verweij, J. Phase II and pharmacologic study of topotecan administered as a 21-day continuous infusion to patients with colorectal cancer. J. Clin. Oncol., 14: 2540-2545, 1996.
38. Hochster, H., Speyer, J., Wadler, S., Runowiez, C., Wallach, R., Oratz, R., Chachoua, A., Sorich, J., Taubes, B., Ludwig, E., Broom, C., and Blum, R. Phase II study of topotecan 21 day infusion in platinum treated ovarian cancer: a highly active regimen. Proc. Am. Soc. Clin. Oncol. Annu. Meet., 15: 285, 1996.
39. Rougier, R., and Bugat, R. CPT-11 in the treatment of colorectal cancer: clinical efficacy and safety profile. Semin. Oncol., 23 (Suppl. 3): 34-41, 1996.
40. Stehlin, J. S., Natelson, E. A., Hinz, H. R., Biovanella, B. C., Ipolyi, P. D., Fehin, K. M., Trezona, T. P., Vardeman, D. M., Harris, N. J., Marcee, J. K., Kozielski, A. J., and Ruiz-Razura, A. Phase I clinical trial and pharmacokinetic results with oral administration of 20-S-camptothecin. In: M. Potmesil and H. Pinedo (eds.), Camptothecins: New Anticancer Agents, pp. 59-65. Boca Raton, FL: CRC Press, 1995.
41. Verschraegen, C. F., Natelson, E., Giovanella, B., Kavanagh, J. J., Freedman, R. S., Kudelka, A. P., Edwards, C. L., Ende, K., and Stehlin, J. Phase I study of oral 9-nitrocamptothecin (9NC). Proc. Am. Soc. Clin. Oncol. Annu. Meet., 15: 482, 1996.
42. Ikuno, N., Soda, H., Watanabe, M., and Oka, M. Irinotecan (CPT-11) and characteristic mucosal changes in the mouse ileum and cecum. J. Natl. Cancer Inst. (Bethesda), 87: 1876-1883, 1995.
43. Mick. R., Gupta, E., Vokes, E. E., and Ratain, M. J. Limited sampling model for irinotecan (CPT-11) pharmacokinetics-pharmacodynamics (PK-PD): prediction of biliary index (BI) and its resulting intestinal toxicity. Proc. Am. Soc. Clin. Oncol. Annu. Meet., 15: 472, 1996.