Clinical pharmacokinetics of imatinib

Clinical Pharmacokinetics

Volumn 44, Issue 9, 2005, Pages 879-894

  Peng, Bin ^a   Lloyd, Peter ^b   Schran, Horst ^a  

^a NOVARTIS PHARMA AG   (Switzerland)

^b NOVARTIS HORSHAM RESEARCH CENTRE   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

CYCLOSPORIN A; HYPERICUM PERFORATUM EXTRACT; IMATINIB; KETOCONAZOLE; RIFAMPICIN; SIMVASTATIN; WARFARIN;

AGE DISTRIBUTION; ANALYTIC METHOD; BODY WEIGHT; CHRONIC MYELOID LEUKEMIA; CLINICAL TRIAL; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CAPSULE; DRUG DISTRIBUTION; DRUG DOSE REGIMEN; DRUG ELIMINATION; DRUG FECES LEVEL; DRUG FORMULATION; DRUG HALF LIFE; DRUG INFORMATION; DRUG METABOLISM; DRUG PROTEIN BINDING; DRUG URINE LEVEL; FOOD DRUG INTERACTION; GASTROINTESTINAL STROMAL TUMOR; HEMATOLOGICAL PARAMETERS; HUMAN; LIVER METASTASIS; LIVER TOXICITY; NEPHROTOXICITY; PHYSICAL CHEMISTRY; PRIORITY JOURNAL; RACE DIFFERENCE; REVIEW; SEX DIFFERENCE; STEADY STATE; TABLET;

ABSORPTION; ANIMALS; DRUG INTERACTIONS; HUMANS; METABOLIC CLEARANCE RATE; MICRODIALYSIS; PIPERAZINES; PYRIMIDINES; TISSUE DISTRIBUTION;

EID: 24344482346     PISSN: 03125963     EISSN: 03125963     Source Type: Journal    
DOI: 10.2165/00003088-200544090-00001     Document Type: Review

References (78)

1. Robinson DR, Wu YM, Lin SF. The protein tyrosine kinase family of the human genome. Oncogene 2000; 19 (49): 5548-57
2. Savage DG, Antman KH. Imatinib mesylate: a new oral targeted therapy. N Engl J Med 2002; 346 (9): 683-93
3. Levitzki A. Tyrphostins: potential antiproliferative agents and novel molecular tools. Biochem Pharmacol 1990; 40 (5): 913-8
4. O'Dwyer M. Multifaceted approach to the treatment of Bcr-Abl-positive leukemias. Oncologist 2002; 7 Suppl. 1: 30-8
5. Verfaillie CM, Hurley R, Zhao RC, et al. Pathophysiology of CML: do defects in integrin function contribute to the premature circulation and massive expansion of the BCR/ABL positive clone? J Lab Clin Med 1997; 129 (6): 584-91
6. Tsai M, Takeishi T, Thompson H, et al. Induction of mast cell proliferation, maturation, and heparin synthesis by the rat c-kit ligand, stem cell factor. Proc Natl Acad Sci U S A 1991; 88 (14): 6382-6
7. Huizinga JD, Thuneberg L, Kluppel M, et al. W/kit gene required for interstitial cells of Cajal and for intestinal pacemaker activity. Nature 1995; 373 (6512): 347-9
8. Ward SM, Burns AJ, Torihashi S, et al. Impaired development of interstitial cells and intestinal electrical rhythmicity in steel mutants. Am J Physiol 1995; 269 (6 Pt 1): C1577-85
9. Heinrich MC, Griffith DJ, Druker BJ, et al. Inhibition of c-kit receptor tyrosine kinase activity by STI 571, a selective tyrosine kinase inhibitor. Blood 2000; 96 (3): 925-32
10. Hirota S, Isozaki K, Nishida T, et al. Effects of loss-of-function and gain-of-function mutations of c-kit on the gastrointestinal tract. J Gastroenterol 2000; 35 Suppl. 12: 75-9
11. Lux ML, Rubin BP, Biase TL, et al. KIT extracellular and kinase domain mutations in gastrointestinal stromal tumors. Am J Pathol 2000; 156 (3): 791-5
12. Rubin BP, Singer S, Tsao C, et al. KIT activation is a ubiquitous feature of gastrointestinal stromal tumors. Cancer Res 2001; 61 (22): 8118-21
13. Demetri GD, von Mehren M, Blanke CD, et al. Efficacy and safety of imatinib mesylate in advanced gastrointestinal stromal tumors. N Engl J Med 2002; 347 (7): 472-80
14. Heinrich MC, Corless C, Blanke CD, et al. KIT mutational status predicts clinical response to STI571 in patients with metastatic gastrointestinal stromal tumors (GISTs). Proc Am Soc Clin Oncol 2002; 21: 2A
15. Singer S, Rubin BP, Lux ML, et al. Prognostic value of KIT mutation type, mitotic activity, and histologic subtype in gastrointestinal stromal tumors. J Clin Oncol 2002; 20 (18): 3898-905
16. Croom KF, Perry CM. Imatinib mesylate: in the treatment of gastrointestinal stromal tumours. Drugs 2003; 63 (5): 513-22
17. Heinrich MC, Corless CL, Duensing A, et al. PDGFRA activating mutations in gastrointestinal stromal tumors. Science 2003; 299 (5607): 708-10
18. Cools J, DeAngelo DJ, Gotlib J, et al. A tyrosine kinase created by fusion of the PDGFRA and FIP1L1 genes as a therapeutic target of imatinib in idiopathic hypereosinophilic syndrome. N Engl J Med 2003; 348: 1201-14
19. Sjöblom T, Shimizu A, O'Brien KP, et al. Growth inhibition of dermatofibrosarcoma protuberans tumors by the platelet-derived growth factor receptor antagonist STI571 through induction of apoptosis. Cancer Res 2001; 61: 5778-83
20. Druker BJ, Lydon NB. Lessons learned from the development of an abl tyrosine kinase inhibitor for chronic myelogenous leukemia. J Clin Invest 2000; 105 (1): 3-7
21. Buchdunger E, Zimmermann J, Mett H, et al. Inhibition of the Abl protein-tyrosine kinase in vitro and in vivo by a 2-phenylaminopyrimidine derivative. Cancer Res 1996; 56 (1): 100-4
22. Druker BJ, Tamura S, Buchdunger E, et al. Effects of a selective inhibitor of the Abl tyrosine kinase on the growth of Bcr-Abl positive cells. Nat Med 1996; 2 (5): 561-6
23. Deininger MW, Druker BJ. Specific targeted therapy of chronic myelogenous leukemia with imatinib. Pharmacol Rev 2003; 55 (3): 401-23
24. van Oosterom AT, Judson IR, Verweij J, et al. Update of phase I study of imatinib (STI571) in advanced soft tissue sarcomas and gastrointestinal stromal tumors: a report of the EORTC Soft Tissue and Bone Sarcoma Group. Eur J Cancer 2002; 38 Suppl. 5: S83-7
25. Druker BJ, Talpaz M, Resta DJ, et al. Efficacy and safety of a specific inhibitor of the BCR-ABL tyrosine kinase in chronic myeloid leukemia. N Engl J Med 2001; 344 (14): 1031-7
26. Deininger MW, Goldman JM, Lydon N, et al. The tyrosine kinase inhibitor CGP57148B selectively inhibits the growth of BCR-ABL-positive cells. Blood 1997; 90 (9): 3691-8
27. Gambacorti-Passerini C, le Coutre P, Mologni L, et al. Inhibition of the ABL kinase activity blocks the proliferation of BCR/ABL+ leukemic cells and induces apoptosis. Blood Cells Mol Dis 1997; 23 (3): 380-94
28. Heinrich MC, Corless CL, Demetri GD, et al. Kinase mutations and imatinib response in patients with metastatic gastrointestinal stromal tumor. J Clin Oncol 2003; 21 (23): 4342-9
29. Novartis Pharma Stein AG. Gleevec® (imatinib mesylate): prescribing information [online]. Available from URL: http://www.gleevec.com/info/page/ prescribing_info [Accessed 2005 Jun 16]
30. Ottmann OG, Druker BJ, Sawyers CL, et al. A phase 2 study of imatinib in patients with relapsed or refractory Philadelphia chromosome-positive acute lymphoid leukemias. Blood 2002; 100: 1965-71
31. Gschwind H, Pfaar U, Waldmeier F, et al. Metabolism and disposition of gleevec™ (STI571) in healthy volunteers [abstract]. Drug Metab Rev 2001; 33 (1): 217
32. Peng B, Dutreix C, Mehring G, et al. Absolute bioavailability of imatinib (Glivec) orally versus intravenous infusion. J Clin Pharmacol 2004; 44 (2): 158-62
33. Peng B, Hayes M, Resta D, et al. Pharmacokinetics and pharmacodynamics of imatinib in a phase I trial with chronic myeloid leukemia patients. J Clin Oncol 2004; 22 (5): 935-42
34. Judson I, Donato di Paola E, Verweij J, et al. Population pharmacokinetic (PK) analysis and PK-pharmacodynamic (PD) correlations in phase I/II trial of imatinib in gastrointestinal stromal tumors (GIST) conducted by the European Organisation for Research and Treatment of Cancer Soft Tissue and Bone Sarcoma Group. Proc Am Soc Clin Oncol 2003; 22: 818A
35. Peng B, Schmidli H, Riviere GJ, et al. Population pharmacokinetics of imatinib in patients with newly diagnosed Philadelphia chromosome positive (Ph+) chronic myekogenous leukemia in chronic phase. Blood 2002; 100 (11): 784A
36. Bakhtiar R, Lohne J, Ramos L, et al. High-throughput quantification of the anti-leukemia drug STI571 (Gleevec) and its main metabolite (CGP 74588) in human plasma using liquid chromatography-tandem mass spectrometry. J Chromatogr B 2002; 768 (2): 325-40
37. Guetens G, De Boeck G, Highley M, et al. Quantification of the anticancer agent STI-571 in erythrocytes and plasma by measurement of sediment technology and liquid chromatography-tandem mass spectrometry. J Chromatogr A 2003; 1020 (1): 27-34
38. Dagher R, Cohen M, Williams G, et al. Approval summary: imatinib mesylate in the treatment of metastatic and/or unresectable malignant gastrointestinal stromal tumors. Clin Cancer Res 2002; 8 (10): 3034-8
39. Druker BJ, Sawyers CL, Kantarjian H, et al. Activity of a specific inhibitor of the BCR-ABL tyrosine kinase in the blast crisis of chronic myeloid leukemia and acute lymphoblastic leukemia with the Philadelphia chromosome. N Engl J Med 2001; 344 (14): 1038-42
40. Reckmann AH, Fischer T, Peng B, et al. Effect of food on STI571 Glivec pharmacokinetics and bioavailability. Proc Am Assoc Clin Oncol 2001; 20: 307A
41. Novartis Oncology, The Glivec International Site. About Glivec: [European] summary of product characteristics [online]. Available from URL: http://www.glivec.com/spc [Accessed 2005 Jun 16]
42. Kretz O, Weiss HM, Schumacher MM, et al. In vitro blood distribution and plasma protein binding of the tyrosine kinase inhibitor imatinib and its active metabolite, CGP74588, in rat, mouse, dog, monkey, healthy humans and patients with acute lymphatic leukaemia. Br J Clin Pharmacol 2004; 58 (2): 212-6
43. Lyseng-Williamson K, Jarvis B. Imatinib. Drugs 2001; 61 (12): 1765-74
44. Gambacorti-Passerini C, Barni R, le Coutre P, et al. Role of α1 acid glycoprotein in the in vivo resistance of human BCR-ABL(+) leukemic cells to the ABL inhibitor STI571. J Natl Cancer Inst 2000; 92 (20): 1641-50
45. Gambacorti-Passerini C, Zucchetti M, Russo D, et al. α1 Acid glycoprotein binds to imatinib (STI571) and substantially alters its pharmacokinetics in chronic myeloid leukemia patients. Clin Cancer Res 2003; 9 (2): 625-32
46. Jorgensen HG, Elliott MA, Allan EK, et al. α1-acid glycoprotein expressed in the plasma of chronic myeloid leukemia patients does not mediate significant in vitro resistance to STI571. Blood 2002; 99 (2): 713-5
47. le Coutre P, Kreuzer KA, Na IK, et al. Determination of α-1 acid glycoprotein in patients with Ph+ chronic myeloid leukemia during the first 13 weeks of therapy with STI571. Blood Cells Mol Dis 2002; 28 (1): 75-85
48. Larghero J, Leguay T, Mourah S, et al. Relationship between elevated levels of the α1 acid glycoprotein in chronic myelogenous leukemia in blast crisis and pharmacological resistance to imatinib (Gleevec) in vitro and in vivo. Biochem Pharmacol 2003; 66 (10): 1907-13
49. Tanaka C, Kawai R, Tse FLS. Physiologically-based pharmacokinetic modeling of a protein-tyrosine kinase inhibitor, STI571. AAPS PharmSci 1999; 1 (4): Epub
50. Petzer AL, Gunsilius E, Hayes M, et al. Low concentrations of STI571 in the cerebrospinal fluid: a case report. Br J Haematol 2002; 117 (3): 623-5
51. Takayama N, Sato N, O'Brien SG, et al. Imatinib mesylate has limited activity against the central nervous system involvement of Philadelphia chromosome-positive acute lymphoblastic leukaemia due to poor penetration into cerebrospinal fluid. Br J Haematol 2002; 119 (1): 106-8
52. Pfeifer H, Wassmann B, Hofmann WK, et al. Risk and prognosis of central nervous system leukemia in patients with Philadelphia chromosome-positive acute leukemias treated with imatinib mesylate. Clin Cancer Res 2003; 9 (13): 4674-81
53. le Coutre P, Kreuzer KA, Pursche S, et al. Pharmacokinetics and cellular uptake of imatinib and its main metabolite CGP74588. Cancer Chemother Pharmacol 2004 Apr; 53 (4): 313-23
54. Kilic T, Alberta JA, Zdunek PR, et al. Intracranial inhibition of platelet-derived growth factor-mediated glioblastoma cell growth by an orally active kinase inhibitor of the 2-phenylaminopyrimidine class. Cancer Res 2000; 60 (18): 5143-50
55. Cohen MH, Williams G, Johnson JR, et al. Approval summary for imatinib mesylate capsules in the treatment of chronic myelogenous leukemia. Clin Cancer Res 2002; 8 (5): 935-42
56. Baker DE. Imatinib mesylate. Rev Gastroenterol Disord 2002; 2 (2): 75-86
57. Nikolova Z, Peng B, Hubert M, et al. Bioequivalence, safety, and tolerability of imatinib tablets compared with capsules. Cancer Chemother Pharmacol 2004; 53: 433-8
58. Mahon FX, Belloc F, Lagarde V, et al. MDR1 gene overexpression confers resistance to imatinib mesylate in leukemia cell line models. Blood 2003; 101 (6): 2368-73
59. Hegedus T, Orfi L, Seprodi A, et al. Interaction of tyrosine kinase inhibitors with the human multidrug transporter proteins, MDR1 and MRP1. Biochim Biophys Acta 2002; 1587 (2-3): 318-25
60. Dai H, Marbach P, Lemaire M, et al. Distribution of STI-571 to the brain is limited by P-glycoprotein-mediated efflux. J Pharmacol Exp Ther 2003; 304 (3): 1085-92
61. Illmer T, Schaich M, Platzbecker U, et al. P-glycoprotein-mediated drug efflux is a resistance mechanism of chronic myelogenous leukemia cells to treatment with imatinib mesylate. Leukemia 2004 Mar; 18 (3): 401-8
62. Thomas H, Coley HM. Overcoming multidrug resistance in cancer: an update on the clinical strategy of inhibiting p-glycoprotein. Cancer Control 2003; 10 (2): 159-65
63. Ozvegy-Laczka C, Hegedus T, Varady G, et al. High-affinity interaction of tyrosine kinase inhibitors with the ABCG2 multidrug transporter. Mol Pharmacol 2004; 65: 1485-95
64. Gurney H, Wong M, Rivory L, et al. Imatinib disposition: characterisation by genotype and phenotype measurement. Br J Clin Pharmacol. In Press
65. Sandoval C, Giamelli J, Jayabose S. Imatinib mesylate noncompliance simulating chronic myeloid leukemia resistance. J Pediatr Hematol Oncol 2003; 25 (6): 507-8
66. Champagne MA, Capdeville R, Krailo M, et al. Imatinib mesylate (STI571) for treatment of children with Philadelphia chromosome-positive leukemia: results from a Children's Oncology Group phase I study. Blood 2004 Nov 1; 104 (9): 2655-60
67. Pindolia VK, Zarowitz BJ. Imatinib mesylate, the first molecularly targeted gene suppressor. Pharmacotherapy 2002; 22 (10): 1249-65
68. Peng B, Knight H, Riviere G, et al. Pharmacokinetic interaction between Gleevec™ (imatinib) and cyclosporin. Blood 2002; 101 (1b): 433-34B
69. Ramanathan RK, Remick SC, Mulkerin D, et al. A phase I pharmacokinetic (PK) study of STI571 in patients (pts) with advanced malignancies and varying degrees of liver dysfunction (LD) [abstract]. Proc Am Assoc Clin Oncol 2003; 22: 126
70. Bauer S, Hagen V, Pielken HJ, et al. Imatinib mesylate therapy in patients with gastrointestinal stromal tumors and impaired liver function. Anticancer Drugs 2002; 13 (8): 847-9
71. Remick SC, Ramanathan RK, Mulkerin D, et al. A phase I pharmacokinetic study of STI-571 in patients (pts) with advanced malignancies and varying degrees of renal dysfunction [abstract]. Proc Am Assoc Clin Oncol 2003; 22: 126
72. Druker BJ, Sawyers CL, Capdeville R, et al. Chronic myelogenous leukemia. Hematology (Am Soc Hematol Educ Program) 2001; 200 (1): 87-112
73. Deininger MW, O'Brien SG, Ford JM, et al. Practical management of patients with chronic myeloid leukemia receiving imatinib. J Clin Oncol 2003; 21 (8): 1637-47
74. McFarland H. Identification and management of drug interactions [online]. Available from URL: http://www.medscape.com/viewarticle/418376 [Accessed 2003 Sep 17]
75. Bolton AE, Peng B, Hubert M, et al. Effect of rifampicin on the pharmacokinetics of imatinib mesylate (Gleevec, STI571) in healthy subjects. Cancer Chemother Pharmacol 2004; 53 (2): 102-6
76. Frye RF, Fitzgerald SM, Lagattuta BS, et al. Effect of St John's Wort on imatinib mesylate pharmacokinetics. Clin Pharmacol Ther 2004; 76 (4): 323-9
77. Dutreix C, Peng B, Mehring G, et al. Ketoconazole increases imatinib (Glivec®/STI571) exposure: results of a drug-drug interaction study [abstract no. 4365]. Blood 2002; 100 (11): 214B
78. O'Brien SG, Meinhardt P, Bond E, et al. Effects of imatinib mesylate (STI571, Glivec) on the pharmacokinetics of simvastatin, a cytochrome P450 3A4 substrate, in patients with chronic myeloid leukaemia. Br J Cancer 2003; 89 (10): 1855-9