Clinical pharmacokinetics and metabolism of irinotecan (CPT-11)

Clinical Cancer Research

Volumn 7, Issue 8, 2001, Pages 2182-2194

  Mathijssen, R H J ^a   Van Alphen, R J ^a   Verweij, J ^a   Loos, W J ^a   Nooter, K ^a   Stoter, G ^a   Sparreboom, A ^a  

^a ERASMUS MC CANCER INSTITUTE   (Netherlands)

Author keywords

[No Author keywords available]

Indexed keywords

7 ETHYL 10 HYDROXYCAMPTOTHECIN; BINDING PROTEIN; CARBOPLATIN; CARRIER PROTEIN; CYTOCHROME P450 3A4; ESTERASE; FLUOROURACIL; GLYCOPROTEIN P; IRINOTECAN; PACLITAXEL;

ANTINEOPLASTIC ACTIVITY; AREA UNDER THE CURVE; DRUG BLOOD LEVEL; DRUG ELIMINATION; DRUG EXCRETION; DRUG GLUCURONIDATION; DRUG METABOLISM; DRUG TRANSFORMATION; HUMAN; MOUSE; NONHUMAN; PH; PRIORITY JOURNAL; PROTEIN EXPRESSION; RAT; SHORT SURVEY;

ANTINEOPLASTIC AGENTS, PHYTOGENIC; AREA UNDER CURVE; ARYL HYDROCARBON HYDROXYLASES; CAMPTOTHECIN; CYTOCHROME P-450 CYP3A; CYTOCHROME P-450 ENZYME SYSTEM; DNA TOPOISOMERASES, TYPE I; HUMANS; OXIDOREDUCTASES, N-DEMETHYLATING; PRODRUGS;

EID: 0034892379     PISSN: 10780432     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Short Survey

References (151)

1. Plant antitumor agents. I. The isolation and structure of camptothecine, a novel alkaloidal leukemia and tumor inhibitor from Camptotheca acuminata
2. Phase I clinical trial of weekly and daily treatment with camptothecin (NSC-100880): Correlation with preclinical studies
3. Phase II study of camptothecin (NSC-100880) in the treatment of advanced gastrointestinal cancer
4. Toxicity of camptothecin (NSC-100880)
5. Topoisomerase I inhibitors. Topotecan and irinotecan
6. A review of the pharmacology and clinical activity of new chemotherapeutic agents in lung cancer
7. Camptothecin induces protein-linked DNA breaks via mammalian DNA topoisomerase I
8. Identification of mammalian DNA topoisomerase I as an intracellular target of the anticancer drug camptothecin
9. Arrest of replication forks by drug-stabilized topoisomerase I-DNA cleavable complexes as a mechanism of cell killing by camptothecin
10. Topoisomerase I inhibitors: The relevance of prolonged exposure for clinical development
11. Camptothecins: A review of their development and schedules of administration
12. Oral topoisomerase I inhibitors in adult patients: Present and future
13. Antitumor activity of 7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxy-camptothecin, a novel water-soluble derivative of camptothecin, against murine tumors
14. Synthesis of water-soluble (aminoalkyl)camptothecin analogues: Inhibition of topoisomerase I and antitumor activity
15. The role of pH and serum albumin in the metabolic conversion of 9-nitrocamptothecin to 9-aminocamptothecin by human hematopoietic and other cells
16. Determination of the lactone and lactone plus carboxylate forms of 9-aminocamptothecin in human plasma by sensitive high-performance liquid chromatography with fluorescence detection
17. Plasma and cerebrospinal fluid pharmacokinetics of 9-aminocamptothecin (9-AC), irinotecan (CPT-11), and SN-38 in nonhuman primates
18. In vivo antitumor activity of two new seven-substituted water-soluble camptothecin analogues
19. The topoisomerase I inhibitor DX-8951f is active in a severe combined immunodeficient mouse model of human acute myelogenous leukemia
20. 14C]CPT-11 in cancer patients
21. Pharmacokinetics and pharmacodynamics of irinotecan during a phase II clinical trial in colorectal cancer
22. Phase I and pharmacologic studies of the camptothecin analog irinotecan administered every 3 weeks in cancer patients
23. Phase I and pharmacological study of the novel topoisomerase I inhibitor 7-ethyl-10-[4-(1-(piperidino)-1-piperidino] carbonyloxycamptothecin (CPT-11) administered as a ninety-minute infusion every 3 weeks
24. Phase I and pharmacokinetic trial of weekly CPT-11
25. Phase I and pharmacokinetic study of the camptothecin derivative irinotecan, administered on a weekly schedule in cancer patients
26. Phase I and pharmacokinetic study of irinotecan (CPT-11) administered daily for three consecutive days every three weeks in patients with advanced solid tumors
27. A pharmacokinetic and pharmacodynamic analysis of CPT-11 and its active metabolite SN-38
28. Phase I dose-finding and pharmacokinetic trial of irinotecan hydrochloride (CPT-11) using a once-every-throe-week dosing schedule for patients with advanced solid tumor malignancy
29. Phase I and pharmacokinetic study of irinotecan administered as a low-dose, continuous intravenous infusion over 14 days in patients with malignant solid tumors
30. Phase I and pharmacologic study of irinotecan and etoposide with recombinant human granulocyte colony-stimulating factor support for advanced lung cancer
31. Pharmacokinetic and pharmacodynamic evaluation of the topoisomerase I inhibitor irinotecan in cancer patients
32. Irinotecan (CPT-11) metabolism and disposition in cancer patients
33. Pharmacological correlation between total drug concentration and lactones of CPT-11 and SN-38 in patients treated with CPT-11
34. Kinetics of the in vivo interconversion of the carboxylate and lactone forms of irinotecan and of its metabolite SN-38 in patients
35. Population pharmacokinetics and pharmacodynamics of irinotecan (CPT-11) and active metabolite SN-38 during phase I trials
36. Pharmacokinetic interrelationships of irinotecan (CPT-11) and its three major plasma metabolites in patients enrolled in phase I/II trials
37. Role of erythrocytes and serum proteins in the kinetic profile of total 9-amino-20(S)-camptothecin in humans
38. Sparse-data set analysis for irinotecan and SN-38 pharmacokinetics in cancer patients co-treated with cisplatin
39. Phase I study and pharmacokinetics of CPT-11 with 5-day continuous infusion
40. Phase II trial of irinotecan in patients with progressive or rapidly recurrent colorectal cancer
41. Limited-sampling models for irinotecan pharmacokinetics-pharmacodynamics: Prediction of biliary index and intestinal toxicity
42. Phase I and pharmacokinetic study of intravenous irinotecan (CPT-11) administered once every 2 weeks +/- G-CSF
43. Factors involved in prolongation of the terminal disposition phase of SN-38: Clinical and experimental studies
44. In vitro binding and partitioning of irinotecan (CPT-11) and its metabolite, SN-38, in human blood
45. Pharmacokinetics of irinotecan and its metabolites SN-38 and APC in children with recurrent solid tumors after protracted low-dose irinotecan
46. The structural basis of camptothecin interactions with human serum albumin: Impact on drug stability
47. The important role of albumin in determining the relative human blood stabilities of the camptothecin anticancer drugs
48. Bioactivation of the anticancer agent CPT-11 to SN-38 by human hepatic microsomal carboxylesterases and the in vitro assessment of potential drug interactions
49. Characterization of CPT-11 hydrolysis by human liver carboxylesterase isoforms hCE-1 and hCE-2
50. Isolation and characterization of a cDNA encoding a horse liver butyrylcholinesterase: Evidence for CPT-11 drug activation
51. The anticancer prodrug CPT-11 is a potent inhibitor of acetylcholinesterase but is rapidly catalyzed to SN-38 by butyrylcholinesterase
52. The transformation of irinotecan (CPT-11) to its active metabolite SN-38 by human liver microsomes
53. Antitumor activity of a camptothecin derivative, CPT-11, against human tumor xenografts in nude mice
54. Conversion of CPT-11 to its active form SN-38, by carboxylesterase of non-small cell lung cancer
55. Determinants of CPT-11 and SN-38 activities in human lung cancer cells
56. CPT-11 converting carboxylesterase and topoisomerase I activities in tumour and normal colon and liver tissues
57. In vivo human carboxylesterase cDNA gene transfer to activate the prodrug CPT-11 for local treatment of solid tumors
58. Reversal of CPT-11 resistance of lung cancer cells by adenovirus-mediated gene transfer of the human carboxylesterase cDNA
59. Comparison of activation of CPT-11 by rabbit and human carboxylesterases for use in enzyme/prodrug therapy
60. Metabolic activation of CPT-11, 7-ethyl-10-[4-(1-piperidino)1-piperidino]carbonyloxycamptothecin, a novel antitumor agent, by carboxylesterase
61. Pharmacokinetics of CPT-11 in rhesus monkeys
62. Overexpression of a rabbit liver carboxylesterase sensitizes human tumor cells to CPT-11
63. Genetic predisposition to the metabolism of irinotecan (CPT-11)
64. Identification and kinetics of a β-glucuronide metabolite of SN-38 in human plasma after administration of the camptothecin derivative irinotecan
65. Identification of the metabolites of irinotecan, a new derivative of camptothecin, in rat bile and its biliary excretion
66. Metabolic fate of irinotecan in humans: Correlation of glucuronidation with diarrhea
67. Glucuronidation of 7-ethyl-10-hydroxycamptothecin (SN-38) by the human UDP-glucuronosyltransferases encoded at the UGT1 locus
68. UGT1A1 genotypes and glucuronidation of SN-38, the active metabolite of irinotecan
69. Phenotype-genotype correlation of in vitro SN-38 (active metabolite of irinotecan) and bilirubin glucuronidation in human liver tissue with UGT1A1 promoter polymorphism
70. Genetic variation in bilirubin UDP-glucuronosyltransferase gene promoter and Gilbert's syndrome
71. Severe CPT-11 toxicity in patients with Gilbert's syndrome: Two case reports
72. Bilirubin (BIL) and SN-38: Pharmacokinetic/pharmacodynamics correlation
73. Polymorphisms of UDP-glucuronosyltransferase gene and irinotecan toxicity: A pharmacogenetic analysis
74. Modulation of glucuronidation of SN-38, the active metabolite of irinotecan, by valproic acid and phenobarbital
75. The role of glucuronidation in 7-ethyl-10-hydroxycamptothecin resistance in vitro
76. Camptothecin resistance: Role of the ATP-binding cassette (ABC), mitoxantrone-resistance half-transporter (MXR), and potential for glucuronidation in MXR-expressing cells
77. Irinotecan (CPT-11) metabolites in human bile and urine
78. Metabolism of irinotecan (CPT-11) by hepatic microsomes: Participation of cytochrome P-450 3A and drug interactions
79. Metabolism of irinotecan (CPT-11) by CYP3A4 and CYP3A5 in humans
80. Identification of a new metabolite of CPT-11 (irinotecan): Pharmacological properties and activation to SN-38
81. Biosynthesis of an aminopiperidino metabolite of irinotecan [7-ethyl-10-[4-(1-piperidino] carbonyloxycamptothecine] by human hepatic microsomes
82. Further elucidation of the pathways involved in the catabolism of the camptothecin analogue irinotecan
83. Identification and properties of a major plasma metabolite of irinotecan (CPT-11) isolated from the plasma of patients
84. Identification of a new metabolite of CPT-11 (irinotecan): Pharmacological properties and activation to SN-38
85. Comparison of mouse and human colon tumors with regard to phase I and phase II drug-metabolizing enzyme systems
86. Conversion of irinotecan (CPT-11) to its active metabolite, 7-ethyl-10-hydroxycamptothecin (SN-38), by human liver carboxylesterase
87. Pharmacokinetic-pharmacodynamic consequences and clinical relevance of cytochrome P450 3A4 inhibition
88. β-glucuronidase activity related to bacterial growth in common bile duct bile in gallstone patients
89. Inhibition of UDP-glucuronosyltransferase by aglycons of natural glucuronides in kampo medicines using SN-38 as a substrate
90. The role of β-glucuronidase in drug disposition and drug targeting in humans
91. Involvement of β-glucuronidase in intestinal microflora in the intestinal toxicity of the antitumor camptothecin derivative irinotecan hydrochloride (CPT-11) in rats
92. Relevance of irinotecan hydrochloride-induced diarrhea to the level of prostaglandin E2 and water absorption of large intestine in rats
93. Relationship between development of diarrhea and the concentration of SN-38, an active metabolite of CPT-11, in the intestine and the blood plasma of athymic mice following intraperitoneal administration of CPT-11
94. Inhibition of intestinal microflora β-glucuronidase modifies the distribution of the active metabolite of the antitumor agent irinotecan hydrochloride (CPT-11) in rats
95. Influence of various bile salts on β-glucuronide activity of intestinal bacteria
96. The influence of the host on expression of intestinal microbial enzyme activities involved in metabolism of foreign compounds
97. Diffuse mucosal damage in the large intestine associated with irinotecan (CPT-11)
98. The influence of incubation pH on the activity of rat and human gut flora enzymes
99. Modulation of irinotecan pharmacokinetics/pharmacodynamics by combined treatment with neomycin
100. Pharmacokinetics of irinotecan and its metabolites in human blood, bile and urine
101. Multispecific organic anion transporter is responsible for the biliary excretion of the camptothecin derivative irinotecan and its metabolites in rats
102. Multiplicity of biliary excretion mechanisms for irinotecan, CPT-11, and its metabolites in rats
103. Biliary excretion mechanism of CPT-11 and its metabolites in humans: Involvement of primary active transporters
104. Pharmacokinetic modulation of irinotecan and metabolites by cyclosporin A
105. Multiplicity of biliary excretion mechanisms for the camptothecin derivative irinotecan (CPT-11), its metabolite SN-38, and its glucuronide: Role of canalicular multispecific organic anion transporter and P-glycoprotein
106. Possible involvement of P-glycoprotein in biliary excretion of CPT-11 in rats
107. A mutation in the human canalicular multispecific organic anion transporter gene causes the Dubin-Johnson syndrome
108. Efficacy of topoisomerase I inhibitors, topotecan and irinotecan, administered at low dose levels in protracted schedules to mice bearing xenografts of human tumors
109. Efficacy of systemic administration of irinotecan against neuroblastoma xenografts
110. Phase I and pharmacologic study of irinotecan administered as a 96-hour infusion weekly to adult cancer patients
111. Direct translation of a protracted irinotecan schedule from a xenograft model to a phase I trial in children
112. In vitro activation of irinotecan to SN-38 by human liver and intestine
113. Phase I and pharmacokinetic trial of oral irinotecan administered daily for 5 days every 3 weeks in patients with solid tumors
114. Altered irinotecan and SN-38 disposition after intravenous and oral administration of irinotecan in mice bearing human neuroblastoma xenografts
115. Disposition of irinotecan and SN-38 following oral and intravenous irinotecan dosing in mice
116. Phase I and pharmacokinetic study of oral irinotecan in pediatric patients with solid tumors
117. pH-dependent uptake of irinotecan and its active metabolite, SN-38, by intestinal cells
118. Comparison of the pharmacokinetics and efficacy of irinotecan after administration by the intravenous versus intraperitoneal route in mice
119. Phase I study of 3-week schedule of irinotecan combined with cisplatin in patients with advanced solid tumors
120. Pharmacokinetic, metabolic, and pharmacodynamic profiles in a dose-escalating study of irinotecan and cisplatin
121. Phase I clinical trial of irinotecan (CPT-11), 7-ethyl-10[4-(1-piperidino)-1-piperidino]carbonyloxy-camptothecin, and cisplatin in combination with fixed dose of vindesine in advanced non-small cell lung cancer
122. Combination effects of cisplatin, vinorelbine and irinotecan in non-small-cell lung cancer cell lines in vitro
123. Phase I/II study of cisplatin, ifosfamide and irinotecan with rhG-CSF support in patients with stage IIIB and IV non-small-cell lung cancer
124. Phase II study of irinotecan plus cisplatin in patients with advanced non-small-cell lung cancer
125. Relationship between the pharmacokinetics of irinotecan and diarrhea during combination chemotherapy with cisplatin
126. Drug-administration sequence does not change pharmacodynamics and kinetics of irinotecan and cisplatin
127. A Phase I clinical and pharmacologic study of a carboplatin and irinotecan regimen combined with recombinant human granulocyte-colony stimulating factor in the treatment of patients with advanced non-small cell lung carcinoma
128. Phase I study of irinotecan combined with carboplatin in previously untreated solid cancers
129. Platinum anticancer drugs modulate P-450 mRNA levels and differentially alter hepatic drug and steroid hormone metabolism in male and female rats
130. Simultaneous administration of CPT-11 and fluorouracil: Alteration of the pharmacokinetics of CPT-11 and SN-38 in patients with advanced colorectal cancer
131. Phase I clinical and pharmacokinetic study of irinotecan, fluorouracil, and leucovorin in patients with advanced solid tumors
132. Phase I study of a weekly schedule of irinotecan, high-dose leucovorin, and infusional fluorouracil as a first-line chemotherapy in patients with advanced colorectal cancer
133. A phase I and pharmacokinetic study of CPT-11 and 5-FU (F) combination
134. CPT-11 (irinotecan) 5-fluorouracil: A promising combination for therapy of colorectal cancer
135. Phase I and pharmacokinetic study of irinotecan and docetaxel in patients with advanced solid tumors: Preliminary evidence of clinical activity
136. Paclitaxel (Taxol) affects pharmacokinetics of irinotecan and its metabolites
137. Pharmacokinetic interaction of the combination of paclitaxel and irinotecan in vivo and clinical study
138. Role of formulation vehicles in taxane pharmacology
139. Dose escalation and pharmacokinetic study of irinotecan in combination with paclitaxel in patients with advanced cancer
140. Irinotecan therapy in adults with recurrent or progressive malignant glioma
141. Pharmacokinetics of irinotecan (IRN) and metabolites in pediatric high-grade glioma patients with and without co-administration of enzyme-inducing anticonvulsants
142. Increased 9-amino-camptothecin dose requirements in patients on anticonvulsants
143. Modulation of irinotecan-induced diarrhea by cotreatment with neomycin in cancer patients
144. Limited sampling models for simultaneous estimation of the pharmacokinetics of irinotecan and its active metabolite SN-38
145. A limited sampling model for estimating pharmacokinetics of CPT-11 and its metabolite SN-38
146. Efficient sampling strategies for forecasting pharmacokinetic parameters of irinotecan (CPT-11): Implication for area under the concentration-time curve monitoring
147. CPT-11: Population pharmacokinetic model and estimation of pharmacokinetics using the bayesian method in patients with lung cancer
148. Combination of oxaliplatin plus irinotecan in patients with gastrointestinal tumors: Results of two independent phase I studies with pharmacokinetics
149. Phase I and pharmacokinetic study of docetaxel and irinotecan in patients with advanced solid tumors
150. Phase I and pharmacologic study of docetaxel and irinotecan in advanced non-small-cell lung cancer
151. Phase I study of irinotecan and raltitrexed in patients with advanced gastrointestinal tract adenocarcinoma