Population pharmacokinetics of imatinib mesylate in patients with chronic-phase chronic myeloid leukaemia: Results of a phase III study

British Journal of Clinical Pharmacology

Volumn 60, Issue 1, 2005, Pages 35-44

  Schmidli, Heinz ^a   Peng, B ^a   Riviere, G J ^a   Capdeville, R ^a   Hensley, M ^a   Gathmann, I ^a   Bolton, A E ^a   Racine Poon, A ^a  

^a NOVARTIS PHARMA AG   (Switzerland)

Author keywords

Chronic myeloid leukaemia; Drug therapy; Imatinib mesylate; Leukaemia; Pharmacokinetics

Indexed keywords

ALPHA INTERFERON; AMFEBUTAMONE; AMITRIPTYLINE; CAPTOPRIL; CARVEDILOL; CHLORPHENIRAMINE; CINNARIZINE; CODEINE; CREATININE; CYCLOBENZAPRINE; CYTARABINE; CYTOCHROME P450 2D6; CYTOCHROME P450 3A4; CYTOCHROME P450 3A5; CYTOCHROME P450 INHIBITOR; DIPHENHYDRAMINE; DOXEPIN; ENZYME INDUCING AGENT; HEMOGLOBIN; HYDROCODONE; HYDROCORTISONE; HYDROXYAMPHETAMINE; IMATINIB; LORATADINE; METHADONE; METOCLOPRAMIDE; METOPROLOL; MIRTAZAPINE; MORPHINE; UNINDEXED DRUG;

ADULT; AGE; AGED; ARTICLE; BLOOD SAMPLING; BODY WEIGHT; CHRONIC MYELOID LEUKEMIA; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CREATININE BLOOD LEVEL; CROSSOVER PROCEDURE; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG DOSE REGIMEN; ETHNOLOGY; FEMALE; GENDER; HEMOGLOBIN DETERMINATION; HUMAN; HUMAN CELL; LEUKOCYTE COUNT; LIVER FUNCTION; MAJOR CLINICAL STUDY; MALE; MULTICENTER STUDY; NONLINEAR SYSTEM; PHASE 3 CLINICAL TRIAL; POLYPHARMACY; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL;

ADOLESCENT; ADULT; AGED; ANTINEOPLASTIC AGENTS; FEMALE; HUMANS; LEUKEMIA, MYELOID, CHRONIC-PHASE; MALE; MIDDLE AGED; PIPERAZINES; PYRIMIDINES;

EID: 21744449067     PISSN: 03065251     EISSN: None     Source Type: Journal    
DOI: 10.1111/j.1365-2125.2005.02372.x     Document Type: Article

References (18)

1. Buchdunger E, Zimmerman J, Mett H, et al. Inhibition of the Abl protein-tyrosine kinase in vitro and in vivo by a 2-phenylalaninepyrimidine derivative. Cancer Res 1996; 56: 100-4.
2. Druker BJ, Tamura S, Buchdunger E, et al. Effects of a selective inhibitor of the tyrosine kinase on the growth of Bcr-Abl positive cells. Nat Med 1996; 2: 561-6.
3. O'Brien SG, Guilhot F, Larson RA, et al. for the IRIS Investigators. Imatinib compared with interferon and low-dose cytarabine for newly diagnosed chronic-phase chronic myeloid leukemia. N Engl J Med 2003; 348: 994-1004.
4. 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: 935-42.
5. Peng B, Dutreix C, Mehring G, et al. Absolute bioavailability of imatinib (Glivec®) orally versus intravenous infusion. J Clin Pharmacol 2004; 44: 158-62.
6. Vozeh S, Steimer J-L, Rowland M, et al. The use of population pharmacokinetics in drug development. Clin Pharmacokinet 1996; 30: 81-93.
7. Cockcroft DW, Gault MH. Prediction of creatinine clearance from serum creatinine. Nephron 1976; 16: 31-41.
8. Bakhtiar R, Lohne J, Ramos L, Khemani L, Hayes M, Tse F. High-throughput quantification of the anti-leukaemia drug STI571 (Gleevec) and its main metabolite (CGP 74588) in human plasma using liquid chromatography-tandem mass spectrometry. J Chromatogr B Anal Technol Biomed Life Sci 2002; 768: 325-40.
9. Gibaldi M, Perrier D. One-Compartment Model. In Pharmacokinetics, eds. Gibaldi, M, Perrier, D. New York: Marcel Dekker, Inc. 1982; pp. 1-43.
10. Kowalski KG, Hutmacher MM. Efficient screening of covariates in population models using Wald's approximation to the likelihood ratio test. J Pharmacokinet Pharmacodyn 2001; 28: 253-75.
11. US Department of Health and Human Services, F.a. D.A. Guidance for Industry: Population Pharmacokinetics. 1999.
12. Judson I, Ma P, Peng B, et al. Imatinib pharmacokinetics in patients with gastrointestinal stromal tumour, a retrospective population pharmacokinetic study over time. EORTC Soft Tissue Bone Sarcoma Group. Cancer Chemother Pharmacol 2004; in press.
13. Kretz O, Weiss HM, Schumacher MM, Gross G. 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: 212-6.
14. Wilkinson GR. Cytochrome P4503A (CYP3A) metabolism: Prediction of in vivo activity in humans. J Pharmacokinet Biopharm 1996; 24: 475-90.
15. Bolton AE, Peng B, Hubert M, et al. Effect of rifampicin (a potent inducer of CYP450 3A4) on the pharmacokinetics of Gleevec™ (Glivec®, STI571, imatinib) (Abstract). Blood 2002; 100: 214b.
16. Dutreix C, Peng B, Mehring G, et al. Ketoconazole increases imatinib (Glivec®/STI571) exposure: Results of a drug-drug interaction study (Abstract). Blood 2002; 100: 214b.
17. 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: 1855-9.
18. Imatinib [package insert]. East Hanover, NJ. Novartis Pharmaceuticals Corporation, 2002.