Relationship of imatinib-free plasma levels and target genotype with efficacy and tolerability

British Journal of Cancer

Volumn 98, Issue 10, 2008, Pages 1633-1640

  Widmer, N ^a   Decosterd, L A ^a   Leyvraz, S ^a   Duchosal, M A ^a   Rosselet, A ^a   Debiec Rychter, M ^b   Csajka, C ^a   Biollaz, J ^a   Buclin, T ^a  

^a LAUSANNE UNIVERSITY HOSPITAL   (Switzerland)

^b UNIVERSITY OF LEUVEN   (Belgium)

Author keywords

Imatinib; Leukaemia; Pharmacogenetics; Pharmacokinetics and pharmacodynamics; Sarcoma; Signal transduction inhibitors

Indexed keywords

IMATINIB; OROSOMUCOID;

ADULT; ADVERSE OUTCOME; AGED; AREA UNDER THE CURVE; ARTICLE; CHRONIC MYELOID LEUKEMIA; CONTROLLED STUDY; CORRELATION ANALYSIS; DRUG CLEARANCE; DRUG EFFICACY; DRUG EXPOSURE; DRUG TOLERABILITY; EXON; FEMALE; GASTROINTESTINAL STROMAL TUMOR; GENE MUTATION; GENETIC ASSOCIATION; GENOTYPE; HUMAN; INCIDENCE; LOGISTIC REGRESSION ANALYSIS; MAJOR CLINICAL STUDY; MALE; NONLINEAR SYSTEM; PHARMACODYNAMICS; PHARMACOGENETICS; PHARMACOLOGICAL PARAMETERS; PRIORITY JOURNAL; TREATMENT RESPONSE; UNSPECIFIED SIDE EFFECT; WILD TYPE;

ADULT; AGED; ANTINEOPLASTIC AGENTS; AREA UNDER CURVE; FEMALE; GASTROINTESTINAL STROMAL TUMORS; GENOTYPE; HUMANS; LEUKEMIA, MYELOGENOUS, CHRONIC, BCR-ABL POSITIVE; LOGISTIC MODELS; MALE; MIDDLE AGED; MULTIVARIATE ANALYSIS; ODDS RATIO; PIPERAZINES; PROTEIN KINASE INHIBITORS; PROTEIN-TYROSINE KINASES; PYRIMIDINES; TREATMENT OUTCOME;

EID: 43649107281     PISSN: 00070920     EISSN: 15321827     Source Type: Journal    
DOI: 10.1038/sj.bjc.6604355     Document Type: Article

References (54)

1. Antonescu CR, Besmer P, Guo T, Arkun K, Hom G, Koryotowski B, Leversha MA, Jeffrey PD, Desantis D, Singer S, Brennan MF, Maki RG, DeMatteo RP (2005) Acquired resistance to imatinib in gastrointestinal stromal tumor occurs through secondary gene mutation. Clin Cancer Res 11: 4182-4190
2. Blanke CD, Demetri GD, von Mehren M, Heinrich MC, Eisenberg B, Fletcher JA, Corless CL, Fletcher CD, Roberts PJ, Heinz D, Wehre E, Nikolova Z, Joensuu H (2008) Long-term results from a randomized phase II trial of standard-versus higher-dose imatinib mesylate for patients with unresectable or metastatic gastrointestinal stromal tumors expressing KIT. J Clin Oncol 26: 620-625
3. Blasdel C, Egorin MJ, Lagattuta TF, Druker BJ, Deininger MW (2007) Therapeutic drug monitoring in CML patients on imatinib. Blood 110: 1699-1701; author reply 1701
4. Brouard M, Saurat JH (2001) Cutaneous reactions to STI571. N Engl J Med 345: 618-619
5. Capdeville R, Buchdunger E, Zimmermann J, Matter A (2002) Glivec (STI571, imatinib), a rationally developed, targeted anticancer drug. Nat Rev Drug Discov 1: 493-502
6. Cohen MH, Johnson JR, Pazdur R (2005) US Food and Drug Administration drug approval summary: conversion of imatinib mesylate (STI571; Gleevec) tablets from accelerated approval to full approval. Clin Cancer Res 11: 12-19
7. Crossman LC, Druker BJ, Deininger MW, Pirmohamed M, Wang L, Clark RE (2005) hOCT1 and resistance to imatinib. Blood 106: 1133-1134; author reply 1134
8. Debiec-Rychter M, Dumez H, Judson I, Wasag B, Verweij J, Brown M, Dimitrijevic S, Sciot R, Stul M, Vranck H, Scurr M, Hagemeijer A, van Glabbeke M, van Oosterom AT, Eortc Soft Tissue and Bone Sarcoma Group (2004) Use of c-KIT/PDGFRA mutational analysis to predict the clinical response to imatinib in patients with advanced gastrointestinal stromal tumours entered on phase I and II studies of the EORTC Soft Tissue and Bone Sarcoma Group. Eur J Cancer 40: 689-695
9. Debiec-Rychter M, Sciot R, Le Cesne A, Schlemmer M, Hohenberger P, van Oosterom AT, Blay J-Y, Leyvraz S, Stul M, Casali PG (2006) KIT mutations and dose selection for imatinib in patients with advanced gastrointestinal stromal tumours. Eur J Cancer 42: 1093-1103
10. Delbaldo C, Chatelut E, Re M, Deroussent A, Seronie-Vivien S, Jambu A, Berthaud P, Le Cesne A, Blay JY, Vassal G (2006) Pharmacokinetic-pharmacodynamic relationships of imatinib and its main metabolite in patients with advanced gastrointestinal stromal tumors. Clin Cancer Res 12: 6073-6078
11. Demetri GD, von Mehren M, Blanke CD, Van den Abbeele AD, Eisenberg B, Roberts PJ, Heinrich MC, Tuveson DA, Singer S, Janicek M, Fletcher JA, Silverman SG, Silberman SL, Capdeville R, Kiese B, Peng B, Dimitrijevic S, Druker BJ, Corless C, Fletcher CD, Joensuu H (2002) Efficacy and safety of imatinib mesylate in advanced gastrointestinal stromal tumors. N Engl J Med 347: 472-480
12. Demetri GD, Wang Y, Wehrle E, Blanke C, Joensuu H, von Mehren M (2008) Correlation of imatinib plasma levels with clinical benefit in patients (Pts) with unresectable/metastatic gastrointestinal stromal tumors (GIST) (abstract, oral presentation). In 2008 Gastrointestinal Cancers Symposium. Orlando, January 25-27, 2008
13. Druker BJ (2003) Imatinib mesylate in the treatment of chronic myeloid leukaemia. Expert Opin Pharmacother 4: 963-971
14. Elliott MA, Mesa RA, Tefferi A (2002) Adverse events after imatinib mesylate therapy. N Engl J Med 346: 712-713
15. Gambacorti-Passerini C, Barni R, le Coutre P, Zucchetti M, Cabrita G, Cleris L, Rossi F, Gianazza E, Brueggen J, Cozens R, Pioltelli P, Pogliani E, Corneo G, Formelli F, D'Incalci M (2000) Role of alpha1 acid glycoprotein in the in vivo resistance of human BCR-ABL(+) leukemic cells to the abl inhibitor STI571. J Natl Cancer Inst 92: 1641-1650
16. Gambacorti-Passerini C, Zucchetti M, Russo D, Frapolli R, Verga M, Bungaro S, Tornaghi L, Rossi F, Pioltelli P, Pogliani E, Alberti D, Corneo G, D'Incalci M (2003) Alpha1 acid glycoprotein binds to imatinib (STI571) and substantially alters its pharmacokinetics in chronic myeloid leukemia patients. Clin Cancer Res 9: 625-632
17. Gambillara E, Laffitte E, Widmer N, Decosterd LA, Duchosal MA, Kovacsovics T, Panizzon RG (2005) Severe pustular eruption associated with imatinib and voriconazole in a patient with chronic myeloid leukemia. Dermatology 211: 363-365
18. Gibbons J, Egorin MJ, Ramanathan RK, Fu P, Mulkerin DL, Shibata S, Takimoto CH, Mani S, LoRusso PA, Grem JL, Pavlick A, Lenz HJ, Flick SM, Reynolds S, Lagattuta TF, Parise RA, Wang Y, Murgo AJ, Ivy SP, Remick SC (2008) Phase I and pharmacokinetic study of imatinib mesylate in patients with advanced malignancies and varying degrees of renal dysfunction: a study by the National Cancer Institute Organ Dysfunction Working Group. J Clin Oncol 26: 570-576
19. Gurney H, Wong M, Balleine RL, Rivory LP, McLachlan AJ, Hoskins JM, Wilcken N, Clarke CL, Mann GJ, Collins M, Delforce SE, Lynch K, Schran H (2007) Imatinib disposition and ABCB1 (MDR1, P-glycoprotein) genotype. Clin Pharmacol Ther 82: 33-40
20. Heinrich MC, Corless CL (2006) Does tumor mutational status correlate with clinical response to imatinib? Nat Clin Pract Oncol 3: 600-601
21. Heinrich MC, Corless CL, Demetri GD, Blanke CD, von Mehren M, Joensuu H, McGreevey LS, Chen CJ, Van den Abbeele AD, Druker BJ, Kiese B, Eisenberg B, Roberts PJ, Singer S, Fletcher CD, Silberman S, Dimitrijevic S, Fletcher JA (2003) Kinase mutations and imatinib response in patients with metastatic gastrointestinal stromal tumor. J Clin Oncol 21: 4342-4349
22. Hochhaus A, La Rosee P (2004) Imatinib therapy in chronic myelogenous leukemia: strategies to avoid and overcome resistance. Leukemia 18: 1321-1331
23. Judson I, Peiming M, Peng B, Verweij J, Racine A, di Paola ED, van Glabbeke M, Dimitrijevic S, Scurr M, Dumez H, van Oosterom A (2005) Imatinib pharmacokinetics in patients with gastrointestinal stromal tumour: a retrospective population pharmacokinetic study over time. EORTC Soft Tissue and Bone Sarcoma Group. Cancer Chemother Pharmacol 55: 379-386
24. Kerkela R, Grazette L, Yacobi R, Iliescu C, Patten R, Beahm C, Walters B, Shevtsov S, Pesant S, Clubb FJ, Rosenzweig A, Salomon RN, Van Etten RA, Alroy J, Durand J-B, Force T (2006) Cardiotoxicity of the cancer therapeutic agent imatinib mesylate. Nat Med 12: 908-916
25. Larghero J, Leguay T, Mourah S, Madelaine-Chambrin I, Taksin AL, Raffoux E, Bastie JN, Degos L, Berthaud P, Marolleau JP, Calvo F, Chomienne C, Mahon FX, Rousselot P (2003) Relationship between elevated levels of the alpha 1 acid glycoprotein in chronic myelogenous leukemia in blast crisis and pharmacological resistance to imatinib (Gleevec) in vitro and in vivo. Biochem Pharmacol 66: 1907-1913
26. Larson RA, Druker BJ, Guilhot FA, O'Brien SG, Riviere GJ, Krahnke T, Gathmann I, Wang Y (2008) Imatinib pharmacokinetics and its correlation with response and safety in chronic phase chronic myeloid leukemia: a subanalysis of the IRIS study (prepublished online February 6, 2008). Blood, doi:10.1182/blood-2007-10-116475
27. Luo FR, Yang Z, Camuso A, Smykla R, McGlinchey K, Fager K, Flefleh C, Castaneda S, Inigo I, Kan D, Wen ML, Kramer R, Blackwood-Chirchir A, Lee FY (2006) Dasatinib (BMS-354825) pharmacokinetics and pharmacodynamic biomarkers in animal models predict optimal clinical exposure. Clin Cancer Res 12: 7180-7186
28. Mahon FX, Belloc F, Lagarde V, Chollet C, Moreau-Gaudry F, Reiffers J, Goldman JM, Melo JV (2003) MDR1 gene overexpression confers resistance to imatinib mesylate in leukemia cell line models. Blood 101: 2368-2373
29. Michor F (2007) Reply: The long-term response to imatinib treatment of CML. Br J Cancer 96: 679-680
30. Michor F, Hughes TP, Iwasa Y, Branford S, Shah NP, Sawyers CL, Nowak MA (2005) Dynamics of chronic myeloid leukaemia. Nature 435: 1267-1270
31. Peng B, Hayes M, Resta D, Racine-Poon A, Druker BJ, Talpaz M, Sawyers CL, Rosamilia M, Ford J, Lloyd P, Capdeville R (2004) Pharmacokinetics and pharmacodynamics of imatinib in a phase I trial with chronic myeloid leukemia patients. J Clin Oncol 22: 935-942
32. Picard S, Titier K, Etienne G, Teilhet E, Ducint D, Bernard MA, Lassalle R, Marit G, Reiffers J, Begaud B, Moore N, Molimard M, Mahon FX (2007) Trough imatinib plasma levels are associated with both cytogenetic and molecular responses to standard-dose imatinib in chronic myeloid leukemia. Blood 109: 3496-3499
33. Ramanathan RK, Egorin MJ, Takimoto CH, Remick SC, Doroshow JH, LoRusso PA, Mulkerin DL, Grem JL, Hamilton A, Murgo AJ, Potter DM, Belani CP, Hayes MJ, Peng B, Ivy SP (2008) Phase I and pharmacokinetic study of imatinib mesylate in patients with advanced malignancies and varying degrees of liver dysfunction: a study by the National Cancer Institute Organ Dysfunction Working Group. J Clin Oncol 26: 563-569
34. Rochat B, Fayet A, Widmer N, Lahrichi SL, Pesse B, Décosterd LA, Biollaz J (2008) Imatinib metabolite profiling in parallel to imatinib quantification in plasma of treated patients using liquid chromatography-mass spectrometry (prepublished online on February 20, 2008). J Mass Spectrom, doi:10.1002/jms.1369
35. Sawyers CL, Hochhaus A, Feldman E, Goldman JM, Miller CB, Ottmann OG, Schiffer CA, Talpaz M, Guilhot F, Deininger MW, Fischer T, O'Brien SG, Stone RM, Gambacorti-Passerini CB, Russell NH, Reiffers JJ, Shea TC, Chapuis B, Coutre S, Tura S, Morra E, Larson RA, Saven A, Peschel C, Gratwohl A, Mandelli F, Ben-Am M, Gathmann I, Capdeville R, Paquette RL, Druker BJ (2002) Imatinib induces hematologic and cytogenetic responses in patients with chronic myelogenous leukemia in myeloid blast crisis: results of a phase II study. Blood 99: 3530-3539
36. Schmidli H, Peng B, Riviere GJ, Capdeville R, Hensley M, Gathmann I, Bolton AE, Racine-Poon A (2005) Population pharmacokinetics of imatinib mesylate in patients with chronic-phase chronic myeloid leukaemia: results of a phase III study. Br J Clin Pharmacol 60: 35-44
37. Schuell B, Gruenberger T, Kornek GV, Dworan N, Depisch D, Lang F, Schneeweiss B, Scheithauer W (2005) Side effects during chemotherapy predict tumour response in advanced colorectal cancer. Br J Cancer 93: 744-748
38. Simonsson T, Sjolund K, Bumming P, Ahlman H, Nilsson B, Oden A (2007) Reducing uncertainty in health-care resource allocation. Br J Cancer 96: 1834-1838
39. Stata Corp (2003) Stata Base Reference Manual, Vol. 3, 8th edn, Stata Press: College Station, TX
40. Stebbing J, Bower M (2003) What can oncologists learn from HIV? Lancet Oncol 4: 438-445
41. Steinert DM, McAuliffe JC, Trent JC (2005) Imatinib mesylate in the treatment of gastrointestinal stromal tumour. Expert Opin Pharmacother 6: 105-113
42. Talpaz M, Silver RT, Druker BJ, Goldman JM, Gambacorti-Passerini C, Guilhot F, Schiffer CA, Fischer T, Deininger MW, Lennard AL, Hochhaus A, Ottmann OG, Gratwohl A, Baccarani M, Stone R, Tura S, Mahon FX, Fernandes-Reese S, Gathmann I, Capdeville R, Kantarjian HM, Sawyers CL (2002) Imatinib induces durable hematologic and cytogenetic responses in patients with accelerated phase chronic myeloid leukemia: results of a phase 2 study. Blood 99: 1928-1937
43. Therasse P, Arbuck SG, Eisenhauer EA, Wanders J, Kaplan RS, Rubinstein L, Verweij J, Van Glabbeke M, van Oosterom AT, Christian MC, Gwyther SG (2000) New guidelines to evaluate the response to treatment in solid tumors. European Organization for Research and Treatment of Cancer, National Cancer Institute of the United States, National Cancer Institute of Canada. J Natl Cancer Inst 92: 205-216
44. Thomas J, Wang L, Clark RE, Pirmohamed M (2004) Active transport of imatinib into and out of cells: implications for drug resistance. Blood 104: 3739-3745
45. Tothova E, Kafkova A, Fricova M, Benova B, Kirschnerova G, Tothova A (2005) Imatinib mesylate in Philadelphia chromosome-positive, chronicphase myeloid leukemia after failure of interferon alpha. Neoplasma 52: 63-67
46. Tsang J, Rudychev I, Pescatore SL (2006) Prescription compliance and persistency in chronic myelogenous leukemia (CML) and gastrointestinal stromal tumor (GIST) patients (pts) on imatinib (IM). J Clin Oncol ASCO Annual Meeting Proceedings Part I. 24: 6119
47. Tuma RS (2007) With targeted drugs, chronic myelogenous leukemia therapy may follow HIV's model. J Natl Cancer Inst 99: 192-194
48. Verweij J, Casali PG, Zalcberg J, LeCesne A, Reichardt P, Blay JY, Issels R, van Oosterom A, Hogendoorn PC, Van Glabbeke M, Bertulli R, Judson I (2004) Progression-free survival in gastrointestinal stromal tumours with high-dose imatinib: randomised trial. Lancet 364: 1127-1134
49. Wang L, Giannoudis A, Lane S, Williamson P, Pirmohamed M, Clark RE (2008) Expression of the uptake drug transporter hOCT1 is an important clinical determinant of the response to imatinib in chronic myeloid leukemia. Clin Pharmacol Ther 83: 258-264
50. Weisberg E, Griffin JD (2003) Resistance to imatinib (Glivec): update on clinical mechanisms. Drug Resist Updat 6: 231-238
51. Widmer N, Béguin A, Rochat B, Buclin T, Kovacsovics T, Duchosal MA, Leyvraz S, Rosselet A, Biollaz J, Decosterd LA (2004) Determination of imatinib (Gleevec) in human plasma by solid-phase extraction-liquid chromatography-ultraviolet absorbance detection. J Chromatogr B Analyt Technol Biomed Life Sci 803: 285-292
52. Widmer N, Decosterd LA, Csajka C, Leyvraz S, Duchosal MA, Rosselet A, Rochat B, Eap CB, Henry H, Biollaz J, Buclin T (2006) Population pharmacokinetics of imatinib and role of alpha-1-acid glycoprotein. Br J Clin Pharmacol 62: 97-112
53. Widmer N, Rumpold H, Untergasser G, Fayet A, Buclin T, Decosterd LA (2007) Resistance reversal by RNAi silencing of MDR1 in CML cells associated with increase in imatinib intracellular levels. Leukemia 21: 1561-1562; author reply 1562-1564
54. Zalcberg JR, Verweij J, Casali PG, Le Cesne A, Reichardt P, Blay JY, Schlemmer M, Van Glabbeke M, Brown M, Judson IR, EORTC Soft Tissue and Bone Sarcoma Group-the Italian Sarcoma Group; Australasian Gastrointestinal Trials Group (2005) Outcome of patients with advanced gastro-intestinal stromal tumours crossing over to a daily imatinib dose of 800mg after progression on 400 mg. Eur J Cancer 41: 1751-1757