Pharmacokinetic interrelationships of irinotecan (CPT-11) and its three major plasma metabolites in patients enrolled in phase I/II trials

Clinical Cancer Research

Volumn 3, Issue 8, 1997, Pages 1261-1266

  Rivory, Laurent P ^a   Haaz, Marie Christine ^b   Canal, Pierre ^c   Lokiec, Francois ^d   Armand, Jean Pierre ^e   Robert, Jacques ^f  

^a UNIVERSITY OF QUEENSLAND   (Australia)

^b UNIVERSITÉ DE BORDEAUX   (France)

^c INSTITUT CLAUDIUS REGAUD   (France)

^d CENTRE RENÉ HUGUENIN   (France)

^e INSTITUT GUSTAVE ROUSSY   (France)

^f INSTITUT BERGONIÉ   (France)

Author keywords

[No Author keywords available]

Indexed keywords

7 ETHYL 10 HYDROXYCAMPTOTHECIN; 7 ETHYL 10 HYDROXYCAMPTOTHECIN GLUCURONIDE; 7 ETHYL 10 [4 N (5 AMINOPENTANOIC ACID) 1 PIPERIDINO]CARBONYLOXYCAMPTOTHECIN; DRUG METABOLITE; IRINOTECAN; UNCLASSIFIED DRUG;

ADULT; AREA UNDER THE CURVE; ARTICLE; CANCER; CANCER CHEMOTHERAPY; CLINICAL ARTICLE; CLINICAL TRIAL; DRUG BLOOD LEVEL; DRUG GLUCURONIDATION; DRUG METABOLISM; DRUG TRANSFORMATION; HUMAN; PHASE 1 CLINICAL TRIAL; PHASE 2 CLINICAL TRIAL; PRIORITY JOURNAL;

EID: 0030856521     PISSN: 10780432     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (14)

1. Sawada, S., Okajima, S., Aiyama, R., Nokata, K., Furuta, T., Yokokura, T., Sugino, E., Yamaguchi, K., and Miyasaka, T. Synthesis and antitumor activity of 20(S)-camptothecin derivatives: carbamate-linked, water-soluble derivatives of 7-ethyl-10-hydroxycamptothecin. Chem. Pharm. Bull. (Tokyo), 39: 1446-1454, 1991.
2. Rougier, P., and Bugat, R. CPT-11 in the treatment of colorectal cancer: clinical efficacy and safety profile. Semin. Oncol., 23 (Suppl. 3): 34-41, 1996.
3. Rivory, L. P., and Robert, J. Molecular, cellular, and clinical aspects of the pharmacology of 20(S)-camptothecin and its derivatives. Pharmacol. & Ther., 68: 269-296, 1995.
4. Kawato, Y., Aonuma, M., Hirota, Y., Kuga, H., and Sato, K. Intracellular roles of SN-38, a metabolite of the camptothecin derivative CPT-11, in the antitumor effect of CPT-11. Cancer Res., 51: 4187-4191, 1991.
5. Rivory, L. P., and Robert, J. Identification and kinetics of a β-glucuronide of SN-38 in human plasma after administration of the camptothecin derivative irinotecan (CPT-11). Cancer Chemother. Pharmacol., 36: 176-179, 1995.
6. Lokiec, F., Canal, P., Gay, C., Chatelut, E., Armand, J-P., Roché, H., Bugat, R., Gonçalvès, E., and Mathieu-Boué, A. Pharmacokinetics of irinotecan and its metabolites in human blood, bile, and urine. Cancer Chemother. Pharmacol., 36: 79-82, 1995.
7. Gupta, E., Lestingi, T. M., Mick, R., Ramirez, J., Vokes, E. E., and Ratain, M. J. Metabolic fate of irinotecan in humans: correlation of glucuronidation with diarrhea. Cancer Res., 54: 3723-3725, 1994.
8. Rivory, L. P., Riou, J. F., Haaz, M. C., Sable, S., Vuilhorgne, M., Commerçon, A., Pond, S. M., and Robert, J. Identification and properties of a major plasma metabolite of irinotecan (CPT-11) isolated from the plasma of patients. Cancer Res., 56: 3689-3694, 1996.
9. Rivory, L. P., and Robert, J. Reversed-phase high-performance liquid chromatographic method for the simultaneous quantitation of the carboxylate and lactone forms of the camptothecin derivative irinotecan, CPT-11, and its metabolite SN-38 in plasma. J. Chromatogr., 661: 133-141, 1994.
10. Rivory, L. P., Chatelut, E., Canal, P., Mathieu-Boué, A., and Robert, J. Kinetics of the in vivo interconversion of the carboxylate and lactone forms of irinotecan (CPT-11) and of its metabolite SN-38 in patients. Cancer Res., 54: 6330-6333, 1994.
11. Abigerges, D., Chabot, G. G., Armand, J-P., Herait, P., Gouyette, A., and Gandia, D. Phase I and pharmacologic studies of the camptothecin analog irinotecan administered every 3 weeks in cancer patients. J. Clin. Oncol., 13: 210-221, 1995.
12. Negoro, S., Fukuoka, M., Masuda, N., Takada, M., Kusunoki, Y., Matsui, K., Takifuji, N., Kudoh, S., Niitani, H., and Taguchi, T. Phase I study of weekly intravenous infusions of CPT-11, a new derivative of camptothecin, in the treatment of advanced non-small cell lung cancer. J. Natl. Cancer Inst., 83: 1164-1168, 1991.
13. Rivory, L. P., Bowles, M. R., Robert, J., and Pond, S. M. The conversion of irinotecan (CPT-11) to its active metabolite, 7-ethyl-10-hydroxycamptothecin (SN-38), by human liver carboxylesterase. Biochem. Pharmacol., 52: 1103-1111, 1996.
14. Houghton, P. J., Cheshire, P. J., Hallman, J. D., Lutz, L., Friedman, H. S., Danks, M., and Houghton, J. A. Efficacy of topoisomerase I inhibitors, 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.