Modulation of glucuronidation of SN-38, the active metabolite of irinotecan, by valproic acid and phenobarbital

Cancer Chemotherapy and Pharmacology

Volumn 39, Issue 5, 1997, Pages 440-444

  Gupta, Elora ^a,b   Wang, Xiaolin ^a   Ramirez, Jacqueline ^a   Ratain, Mark J ^a  

^a UNIVERSITY OF CHICAGO MEDICAL CENTER   (United States)

^b RUTGERS CANCER INSTITUTE OF NEW JERSEY   (United States)

Author keywords

Glucuronidation; Induction; Inhibition; Pharmacokinetics; SN 38

Indexed keywords

7 ETHYL 10 HYDROXYCAMPTOTHECIN; DRUG METABOLITE; IRINOTECAN; PHENOBARBITAL; VALPROIC ACID;

ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; DRUG CONJUGATION; DRUG DISPOSITION; DRUG GLUCURONIDATION; DRUG METABOLISM; FEMALE; INTRAVENOUS DRUG ADMINISTRATION; NONHUMAN; PHARMACOKINETICS; PRIORITY JOURNAL; RAT;

ANIMALS; ANTINEOPLASTIC AGENTS, PHYTOGENIC; BIOTRANSFORMATION; CAMPTOTHECIN; FEMALE; GLUCURONATES; GLUCURONOSYLTRANSFERASE; METABOLIC CLEARANCE RATE; PHENOBARBITAL; RATS; RATS, WISTAR; VALPROIC ACID;

EID: 0031055238     PISSN: 03445704     EISSN: None     Source Type: Journal    
DOI: 10.1007/s002800050595     Document Type: Article

References (25)

1. Anderson GD, Gidal BE, Kantor ED, Wilensky AJ (1994) Lorazepam-valproate interaction: studies in normal subjects and isolated perfused rat liver. Epilepsia 35:221
2. Atsumi R, Suzuki W, Hakusui H (1991) Identification of the metabolites of irinotecan, a new derivative of camptothecin, in rat bile and its biliary excretion. Xenobiotica 21:1159
3. Bock KW, Josting D, Lilienblum W, Pfeil H (1979) Purification of rat-liver microsomal UDP-glucuronosyltransferase. Separation of two enzyme forms inducible by 3-methylcholanthrene or phenobarbital. Eur J Biochem 98:19
4. Bock KW, Lilenblum W, Von Bahr C (1984) Studies of UDP-glucuronosyltransferase activities in human liver microsomes. Drug Metab Dispos 12:93
5. Forni M de, Bugat R, Chabot GG, Culine S, Extra J-M, Gouyette A, Madelaine I, Marty ME, Mathieu-Boue A (1994) Phase I and pharmacokinetic study of the camptothecin derivative irinotecan, administered on a weekly schedule in cancer patients. Cancer Res 54:4347
6. Gupta E, Lestingi TM, Mick R, Ramirez J, Vokes EE, Ratain MJ (1994) Metabolic fate of irinotecan in humans: correlation of glucuronidation with diarrhea. Cancer Res 54:3723
7. Gupta E, Mick R, Ramirez J, Wang X, Lestingi TM, Vokes EE, Ratain MJ (1997) A pharmacokinetic and pharmacodynamic evaluation of the topoisomerase inhibitor irinotecan (CPT-11) in cancer patients. J Clin Oncol (in press)
8. Haumont M, Magdalou J, Lafaurie C, Ziegler J-M, Siest J, Colin J-N (1990) Phenobarbital inducible UDP-glucuronosyltransferase is responsible for glucuronidation of 3′-azido-3′-deoxythymidine: characterization of the enzyme in human and rat liver microsomes. Arch Biochem Biophys 281:264
9. Hosokawa M, Maki T, Satoh T (1987) Multiplicity and regulation of hepatic microsomal carboxyl esterascs in rats. Pharmacology 31:579
10. Howell SR, Hazelton GA, Klaassen CD (1986) Depletion of hepatic UDP-glucuronic acid by drugs that are glucuronidated. J Pharmacol Exp Ther 236:610
11. Kaneda N, Yokokura T (1990) Nonlinear pharmacokinetics of CPT-11 in rats. Cancer Res 50:1721
12. Kawato Y, Aonuma M, Hirota Y, Kuga H, Sato K (1991) Intracellular roles of SN-38, a metabolite of the camptothecin derivative CPT-11, in the antitumor effect of CPT-11. Cancer Res 51:4187
13. Klaassen CD (1971) Studies on the increased biliary flow produced by phenobarbital in rats. J Pharmacol Exp Ther 176:743
14. Lertora JJL , Rege AB, Greenspan DL, Akula S, George WJ, Hyslop NE, Agrawal KC (1994) Pharmacokinetic interaction between zidovudine and valproic acid in patients infected with human immunodeficiency virus. Clin Pharmacol Ther 56:272
15. Lokiec F, Canal P, Gay C, Chatelut E, Armand J-P, Roche H, Bugat R, Goncalves E, Mathieu-Boue A (1995) Pharmacokinetics of irinotecan and its metabolites in human blood, bile, and urine. Cancer Chemother Pharmacol 36:79
16. McCracken NW, Blain PG, Williams FM (1993) Peripheral esterases in rat: effects of classical inducers. Chem Biol Interact 87:183
17. Pritchard M, Fournel-Gigleux S, Siest G, Mackenzie P, Magdalou J (1994) A recombinant phenobarbital-inducible rat liver UDP-glucuronosyltransferase (UDP-glucuronosyltransferase 2B1) stably expressed in V79 cells catalyzes the glucuronidation of morphine, phenols, and carboxylic acids. Mol Pharmacol 45:42
18. Rivory LP, Robert J (1995) Identification and kinetics of a β-glucuronide metabolite of SN-38 in human plasma after administration of the camptothecin derivative irinotecan. Cancer Chemother Pharmacol 36:176
19. Rothenberg ML, Kuhn JG, Burris III HA, Nelson J, Eckardt JR, Tristan-Morales M, Hilsenbeck SG, Weiss GR, Smith LS, Rodriguez GI, Rock MK, Von Hoff DD (1993) Phase I and pharmacokinetic trial of weekly CPT-11. J Clin Oncol 11:2194
20. Somani SM, Bajaj RA, Calvey TN, Norman T (1980) Effect of phenobarbitone on the elimination of neostigmine and its metabolites in bile. Biochem Pharmacol 29:2256
21. Taburet A-M, Aymard P (1983) Valproate glucuronidation by rat liver microsomes. Interaction with parahydroxyphenobarbital. Biochem Pharmacol 32:3859
22. Tsuji T, Kaneda N, Kudo K, Yokokura T, Yoshimoto T, Tsuru D (1991) CPT-11 converting enzyme from rat serum: purification and some properties. J Pharmacobio-Dyn 14:341
23. Watkins JB, Klaassen CD (1982) Effect of inducers and inhibitors of glucuronidation on the biliary excretion and choleretic action of valproic acid in the rat. J Pharmacol Exp Ther 220:305
24. Wishart GJ (1978) Demonstration of functional heterogeneity of hepatic uridine diphosphate glucuronosyltransferase activities after administration of 3-methylcholanthrene and phenobarbital in rats. Biochem J 174:671
25. Yuen AWC, Land G, Weatherley BC, Peck AW (1992) Sodium valproatc acutely inhibits lamotrigine metabolism. Br J Clin Pharmacol 33:511