Therapeutic drug monitoring of targeted anticancer therapy. Tyrosine kinase inhibitors and selective estrogen receptor modulators: A clinical pharmacology laboratory perspective

LC-MS in Drug Bioanalysis

Volumn 9781461438281, Issue , 2012, Pages 197-250

  Decosterd, Laurent ^a   Dahmane, Elyes ^b   Neeman, Marine ^b   Buclin, Thierry ^b   Csajka, Chantal ^b   Haouala, Amina ^b   Widmer, Nicolas ^b  

^a LAUSANNE UNIVERSITY HOSPITAL   (Switzerland)

^b UNIVERSITY OF LAUSANNE   (Switzerland)

Author keywords

[No Author keywords available]

Indexed keywords

AMINO ACIDS; CHEMOTHERAPY; DIAGNOSIS; DISEASES; DRUG DOSAGE; ENZYME INHIBITION; MASS SPECTROMETRY; METABOLITES; PATIENT MONITORING;

ANTI-CANCER THERAPIES; ANTICANCER TREATMENT; CANCER THERAPY; CLINICAL PHARMACOLOGY; CYTOTOXIC; DIAGNOSTIC TESTS; MOLECULAR THERAPY; SELECTIVE ESTROGEN RECEPTOR MODULATORS; THERAPEUTIC DRUG MONITORING; TYROSINE KINASE INHIBITOR;

PHARMACOKINETICS;

EID: 84949176834     PISSN: None     EISSN: None     Source Type: Book    
DOI: 10.1007/978-1-4614-3828-1_9     Document Type: Chapter

References (269)

1. Jemal A et al (2010) Cancer statistics, 2010. CA Cancer J Clin 60:277-300
2. Chabner BA et al (2005) Timeline: chemotherapy and the war on cancer. Nat Rev Cancer 5:65-72
3. Giamas G et al (2010) Kinases as targets in the treatment of solid tumors. Cell Signal 22:984-1002
4. Hughes TP, et al. Monitoring disease response to tyrosine kinase inhibitor therapy in CML. Hematology Am Soc Hematol Educ Program. 2009:477-87
5. Table of pharmacogenomic biomarkers in drug labels. Last accessed 5 Jan 2012
6. Schilsky RL (2010) Personalized medicine in oncology: the future is now. Nat Rev Drug Discov 9:363-366
7. McDermott U et al (2009) Personalized cancer therapy with selective kinase inhibitors: an emerging paradigm in medical oncology. J Clin Oncol 27:5650-5659
8. Cortes JE et al (2009) Pharmacokinetic/pharmacodynamic correlation and blood-level testing in imatinib therapy for chronic myeloid leukemia. Leukemia 23:1537-1544
9. Von Mehren M et al (2011) Correlations between imatinib pharmacokinetics, pharmacodynamics, adherence, and clinical response in advanced metastatic gastrointestinal stromal tumor (GIST): an emerging role for drug blood level testing? Cancer Treat Rev 37:291-299
10. Stearns V et al (2003) Active tamoxifen metabolite plasma concentrations after coadministration of tamoxifen and the selective serotonin reuptake inhibitor paroxetine. J Natl Cancer Inst 95:1758-1764
11. Borges S et al (2006) Quantitative effect of CYP2D6 genotype and inhibitors on tamoxifen metabolism: implication for optimization of breast cancer treatment. Clin Pharmacol Ther 80:61-74
12. Widmer N et al (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
13. Krause DS et al (2005) Tyrosine kinases as targets for cancer therapy. N Engl J Med 353:172-187
14. Oliff A et al (1996) New molecular targets for cancer therapy. Sci Am 275:144-149
15. Larson RA et al (2008) Imatinib pharmacokinetics and its correlation with response and safety in chronic-phase chronic myeloid leukemia: a subanalysis of the IRIS study. Blood 111:4022-4028
16. Picard S et al (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
17. Demetri GD et al (2009) Imatinib plasma levels are correlated with clinical bene fit in patients with unresectable/metastatic gastrointestinal stromal tumors. J Clin Oncol 27(19):3141-3147
18. Peng B et al (2005) Clinical pharmacokinetics of imatinib. Clin Pharmacokinet 44:879-894
19. Widmer N et al (2008) Relationship of imatinib-free plasma levels and target genotype with efficacy and tolerability. Br J Cancer 98:1633-1640
20. Widmer N et al (2010) Imatinib plasma levels: correlation with clinical bene fit in GIST patients. Br J Cancer 102:1198-1199
21. Badalamenti G et al (2007) Gastrointestinal stromal tumors (GISTs): focus on histopathological diagnosis and biomolecular features. Ann Oncol 18(Suppl 6): vi136-vi140
22. Geyer CE et al (2006) Lapatinib plus capecitabine for HER2-positive advanced breast cancer. N Engl J Med 355:2733-2743
23. Le TC et al (2008) New developments in multitargeted therapy for patients with solid tumours. Cancer Treat Rev 34:37-48
24. Mitsudomi T et al (2005) Mutations of the epidermal growth factor receptor gene predict prolonged survival after ge fitinib treatment in patients with non-small-cell lung cancer with postoperative recurrence. J Clin Oncol 23:2513-2520
25. Cadranel J et al (2011) Genetic pro filing and epidermal growth factor receptor-directed therapy in nonsmall cell lung cancer. Eur Respir J 37:183-193
26. Commander H et al (2011) Vandetanib: first global approval. Drugs 71:1355-1365
27. Flaherty KT et al (2010) Inhibition of mutated, activated BRAF in metastatic melanoma. N Engl J Med 363:809-819
28. Sasaki T et al (2011) New strategies for treatment of ALK-rearranged non-small cell lung cancers. Clin Cancer Res 17:7213-7218
29. Widmer N et al (2008) Principles of therapeutic drug monitoring. Rev Med Suisse 4:1644-1648
30. Widmer N et al (2008) Therapeutic drug monitoring: the clinical practice. Rev Med Suisse 4:1649-1660
31. Decosterd LA et al (2010) Multiplex ultra-performance liquid chromatography-tandem mass spectrometry method for simultaneous quanti fication in human plasma of fluconazole, itraconazole, hydroxyitraconazole, posaconazole, voriconazole, voriconazole-N-oxide, anidulafungin, and caspofungin. Antimicrob Agents Chemother 54:5303-5315
32. Fayet A et al (2009) A LC-tandem MS assay for the simultaneous measurement of new antiretroviral agents: raltegravir, maraviroc, darunavir, and etravirine. J Chromatogr B Analyt Technol Biomed Life Sci 877:1057-1069
33. Fayet Mello A et al (2011) Successful efavirenz dose reduction guided by therapeutic drug monitoring. Antivir Ther 16:189-197
34. Gotta V et al (2010) Suivi thérapeutique de l'imatinib. Forum Med Suisse 10:403-406
35. Gervasini G et al (2010) Pharmacogenetic testing and therapeutic drug monitoring are complementary tools for optimal individualization of drug therapy. Eur J Clin Pharmacol 66:755-774
36. McMahon G et al (2009) Therapeutic drug monitoring in oncology: does it have a future? Bioanalysis 1:507-511
37. Lennard L (2001) Therapeutic drug monitoring of cytotoxic drugs. Br J Clin Pharmacol 52(Suppl 1):75S-87S
38. Kamath AV et al (2008) Preclinical pharmacokinetics and in vitro metabolism of dasatinib (BMS-354825): a potent oral multi-targeted kinase inhibitor against SRC and BCR-ABL. Cancer Chemother Pharmacol 61:365-376
39. Lathia C et al (2006) Lack of effect of ketoconazole-mediated CYP3A inhibition on sorafenib clinical pharmacokinetics. Cancer Chemother Pharmacol 57:685-692
40. O'Brien SG et al (2003) 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 89:1855-1859
41. White DL et al (2006) OCT-1-mediated in flux is a key determinant of the intracellular uptake of imatinib but not nilotinib (AMN107): reduced OCT-1 activity is the cause of low in vitro sensitivity to imatinib. Blood 108:697-704
42. Widmer N et al (2006) Population pharmacokinetics of imatinib and the role of alpha-acid glycoprotein. Br J Clin Pharmacol 62:97-112
43. Haouala A et al. (2011) Prediction of free imatinib concentrations based on total plasma levels in GIST patients. Br J Clin Pharmacol, in press
44. Hazarika M et al (2008) Tasigna for chronic and accelerated phase Philadelphia chromosome-positive chronic myelogenous leukemia resistant to or intolerant of imatinib. Clin Cancer Res 14:5325-5331
45. Koch KM et al (2009) Effects of food on the relative bioavailability of lapatinib in cancer patients. J Clin Oncol 27:1191-1196
46. Dai G et al (2008) Importance of characterizing determinants of variability in exposure: application to dasatinib in subjects with chronic myeloid leukemia. J Clin Pharmacol 48(11):1254-1269
47. Houk BE et al (2010) Relationship between exposure to sunitinib and efficacy and tolerability endpoints in patients with cancer: results of a pharmacokinetic/pharmacodynamic meta-analysis. Cancer Chemother Pharmacol 66:357-371
48. Klumpen HJ et al (2011) Moving towards dose individualization of tyrosine kinase inhibitors. Cancer Treat Rev 37(4):251-260
49. Moore M et al (2005) Phase I study to determine the safety and pharmacokinetics of the novel Raf kinase and VEGFR inhibitor BAY 43-9006, administered for 28 days on/7 days off in patients with advanced, refractory solid tumors. Ann Oncol 16:1688-1694
50. Peng B et al (2004) Pharmacokinetics and pharmacodynamics of imatinib in a phase I trial with chronic myeloid leukemia patients. J Clin Oncol 22:935-942
51. Strumberg D et al (2005) Phase I clinical and pharmacokinetic study of the novel Raf kinase and vascular endothelial growth factor receptor inhibitor BAY 43-9006 in patients with advanced refractory solid tumors. J Clin Oncol 23:965-972
52. Tan AR et al (2004) Evaluation of biologic end points and pharmacokinetics in patients with metastatic breast cancer after treatment with erlotinib, an epidermal growth factor receptor tyrosine kinase inhibitor. J Clin Oncol 22:3080-3090
53. Burris HA III et al (2005) Phase I safety, pharmacokinetics, and clinical activity study of lapatinib (GW572016), a reversible dual inhibitor of epidermal growth factor receptor tyrosine kinases, in heavily pretreated patients with metastatic carcinomas. J Clin Oncol 23:5305-5313
54. Kantarjian H et al (2010) Dasatinib versus imatinib in newly diagnosed chronic-phase chronic myeloid leukemia. N Engl J Med 362:2260-2270
55. Soulieres D et al (2004) Multicenter phase II study of erlotinib, an oral epidermal growth factor receptor tyrosine kinase inhibitor, in patients with recurrent or metastatic squamous cell cancer of the head and neck. J Clin Oncol 22:77-85
56. Buclin T et al (2011) Who is in charge of assessing therapeutic drug monitoring? The case of imatinib. Lancet Oncol 12:9-11
57. Van Erp NP et al (2009) Clinical pharmacokinetics of tyrosine kinase inhibitors. Cancer Treat Rev 35:692-706
58. Bouchet S et al (2010) Therapeutic drug monitoring of tyrosine-kinase inhibitors in the treatment of chronic myelogenous leukaemia: interests and limits. Therapie 65:213-218
59. Gambacorti-Passerini C et al (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
60. Le CP et al (2004) Pharmacokinetics and cellular uptake of imatinib and its main metabolite CGP74588. Cancer Chemother Pharmacol 53:313-323
61. Wang L et al (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
62. Haouala A et al (2010) Cardiovascular drug interactions with tyrosine kinase inhibitors. Cardiovasc Med 13:147-154
63. Haouala A et al (2011) Drug interactions with the tyrosine kinase inhibitors imatinib, dasatinib, and nilotinib. Blood 117:e75-e87
64. Gambillara E et al (2005) Severe pustular eruption associated with imatinib and voriconazole in a patient with chronic myeloid leukemia. Dermatology 211:363-365
65. Druker BJ et al (2006) Five-year follow-up of patients receiving imatinib for chronic myeloid leukemia. N Engl J Med 355:2408-2417
66. Takahashi N et al (2010) Correlation between imatinib pharmacokinetics and clinical response in Japanese patients with chronic-phase chronic myeloid leukemia. Clin Pharmacol Ther 88:809-813
67. Singh N et al (2009) Drug monitoring of imatinib levels in patients undergoing therapy for chronic myeloid leukaemia: comparing plasma levels of responders and non-responders. Eur J Clin Pharmacol 65:545-549
68. Awidi A et al (2010) Relationship of serum imatinib trough level and response in CML patients: long term follow-up. Leuk Res 34:1573-1575
69. Faber E et al (2010) Imatinib dose escalation in two patients with chronic myeloid leukemia, with low trough imatinib plasma levels measured at various intervals from the beginning of therapy and with suboptimal treatment response, leads to the achievement of higher plasma levels and major molecular response. Int J Hematol 91:897-902
70. Larson RA (2009) Therapeutic monitoring of drug plasma concentrations and improved clinical outcomes in CML. Clin Adv Hematol Oncol 7:S3-S5
71. Kantarjian H et al (2006) Nilotinib in imatinib-resistant CML and Philadelphia chromosomepositive ALL. N Engl J Med 354:2542-2551
72. Saglio G et al (2010) Nilotinib versus imatinib for newly diagnosed chronic myeloid leukemia. N Engl J Med 362:2251-2259
73. Milojkovic D et al (2009) Mechanisms of resistance to imatinib and second-generation tyrosine inhibitors in chronic myeloid leukemia. Clin Cancer Res 15:7519-7527
74. Wang X et al. (2008) Dasatinib pharmacokinetics and exposure-response (E-R): relationship to safety and efficacy in patients (pts) with chronic myeloid leukemia (CML). J Clin Oncol. 26 (No 15 S) (May 20 Suppl, Abstract 3590)
75. Mendel DB et al (2003) In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationship. Clin Cancer Res 9:327-337
76. Faivre S et al (2006) Safety, pharmacokinetic, and antitumor activity of SU11248, a novel oral multitarget tyrosine kinase inhibitor, in patients with cancer. J Clin Oncol 24:25-35
77. Billemont B, et al. (2009) Correlation of sorafenib plasma concentrations and clinical toxicity: a prospective population pharmacodynamic and pharmacokinetic study. J Clin Oncol 27 (No 15 S) (May 20 Suppl, e14585)
78. Ratain MJ et al (2007) The value meal: how to save $1, 700 per month or more on lapatinib. J Clin Oncol 25:3397-3398
79. Li J et al (2006) CYP3A Phenotyping approach to predict systemic exposure to EGFR tyrosine kinase inhibitors. J Natl Cancer Inst 98:1714-1723
80. Martin P et al (2012) Pharmacokinetics of vandetanib: three phase I studies in healthy subjects. Clin Ther 34(1):221-237
81. Zhang L et al (2011) Pharmacokinetics and tolerability of vandetanib in Chinese patients with solid, malignant tumors: an open-label, phase I, rising multiple-dose study. Clin Ther 33:315-327
82. Martin P et al (2011) Pharmacokinetic drug interactions with vandetanib during coadministration with rifampicin or itraconazole. Drugs R&D 11:37-51
83. Weil A et al (2010) Pharmacokinetics of vandetanib in subjects with renal or hepatic impairment. Clin Pharmacokinet 49:607-618
84. Weisberg E et al (2007) Second generation inhibitors of BCR-ABL for the treatment of imatinib-resistant chronic myeloid leukaemia. Nat Rev Cancer 7:345-356
85. Santos FP et al (2010) Bafetinib, a dual Bcr-Abl/Lyn tyrosine kinase inhibitor for the potential treatment of leukemia. Curr Opin Investig Drugs 11:1450-1465
86. Keisner SV et al (2011) Pazopanib: the newest tyrosine kinase inhibitor for the treatment of advanced or metastatic renal cell carcinoma. Drugs 71:443-454
87. Abbas R et al (2011) Pharmacokinetics of oral neratinib during co-administration of ketoconazole in healthy subjects. Br J Clin Pharmacol 71:522-527
88. Abbas R et al (2011) Effect of ketoconazole on the pharmacokinetics of oral bosutinib in healthy subjects. J Clin Pharmacol 51:1721-1727
89. Jost LM et al (2006) Metabolism and disposition of vatalanib (PTK787/ZK-222584) in cancer patients. Drug Metab Dispos 34:1817-1828
90. Chiorean EG et al (2010) A phase I dose escalation and pharmacokinetic study of vatalanib (PTK787/ZK 222584) in combination with paclitaxel in patients with advanced solid tumors. Cancer Chemother Pharmacol 66:441-448
91. Reardon DA et al (2009) Phase I pharmacokinetic study of the vascular endothelial growth factor receptor tyrosine kinase inhibitor vatalanib (PTK787) plus imatinib and hydroxyurea for malignant glioma. Cancer 115:2188-2198
92. Fox E et al (2010) A phase 1 trial and pharmacokinetic study of cediranib, an orally bioavailable pan-vascular endothelial growth factor receptor inhibitor, in children and adolescents with refractory solid tumors. J Clin Oncol 28:5174-5181
93. Yamamoto N et al (2009) Phase I, dose escalation and pharmacokinetic study of cediranib (RECENTIN), a highly potent and selective VEGFR signaling inhibitor, in Japanese patients with advanced solid tumors. Cancer Chemother Pharmacol 64:1165-1172
94. Goss G et al (2009) A phase I and pharmacokinetic study of daily oral cediranib, an inhibitor of vascular endothelial growth factor tyrosine kinases, in combination with cisplatin and gemcitabine in patients with advanced non-small cell lung cancer: a study of the national cancer institute of Canada clinical trials group. Eur J Cancer 45:782-788
95. Li C et al (2009) In vitro metabolism of the novel, highly selective oral angiogenesis inhibitor motesanib diphosphate in preclinical species and in humans. Drug Metab Dispos 37:1378-1394
96. ®: Scienti fic Discussion page 11. European Medicines Agency 2005. www.ema. europa.eu, last accessed 12 Dec. 2011
97. Costa DB et al (2011) CSF concentration of the anaplastic lymphoma kinase inhibitor crizotinib. J Clin Oncol 29:e443-e445
98. Tan W, et al. (2010) Pharmacokinetics (PK) of PF-02341066. a dula ALK/MET inhibitor after multiple oral dose to advanced cancer patients. J Clin Oncol 28 (228 s) (supplement, abstract 2596)
99. Hidalgo M et al (2003) Pharmacokinetics and pharmacodynamics: maximizing the clinical potential of erlotinib (tarceva). Semin Oncol 30:25-33
100. Lu JF et al (2006) Clinical pharmacokinetics of erlotinib in patients with solid tumors and exposure-safety relationship in patients with non-small cell lung cancer. Clin Pharmacol Ther 80:136-145
101. Mohamed MK et al (2005) Skin rash and good performance status predict improved survival with ge fitinib in patients with advanced non-small cell lung cancer. Ann Oncol 16:780-785
102. Eskens FA et al (2006) The clinical toxicity pro file of vascular endothelial growth factor (VEGF) and vascular endothelial growth factor receptor (VEGFR) targeting angiogenesis inhibitors; a review. Eur J Cancer 42:3127-3139
103. Awidi A et al (2010) Determination of imatinib plasma levels in patients with chronic myeloid leukemia by high performance liquid chromatography-ultraviolet detection and liquid chromatography-tandem mass spectrometry: methods' comparison. Leuk Res 34:714-717
104. Bakhtiar R et al (2002) High-throughput quanti fication 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 Analyt Technol Biomed Life Sci 768:325-340
105. Boddy AV et al (2007) Pharmacokinetic investigation of imatinib using accelerator mass spectrometry in patients with chronic myeloid leukemia. Clin Cancer Res 13:4164-4169
106. Guetens G et al (2003) 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 1020:27-34
107. Klawitter J et al (2009) Development and validation of a sensitive assay for the quanti fication of imatinib using LC/LC-MS/MS in human whole blood and cell culture. Biomed Chromatogr 23:1251-1258
108. Parise RA et al (2003) Liquid chromatographic-mass spectrometric assay for quantitation of imatinib and its main metabolite (CGP 74588) in plasma. J Chromatogr B Analyt Technol Biomed Life Sci 791:39-44
109. Rochat B et al (2008) Imatinib metabolite pro filing in parallel to imatinib quanti fication in plasma of treated patients using liquid chromatography-mass spectrometry. J Mass Spectrom 43:736-752
110. Titier K et al (2005) Quanti fication of imatinib in human plasma by high-performance liquid chromatography-tandem mass spectrometry. Ther Drug Monit 27:634-640
111. Parise RA et al (2009) A high-performance liquid chromatography-mass spectrometry assay for quantitation of the tyrosine kinase inhibitor nilotinib in human plasma and serum. J Chromatogr B Analyt Technol Biomed Life Sci 877:1894-1900
112. Tanaka C et al (2010) Clinical pharmacokinetics of the BCR-ABL tyrosine kinase inhibitor nilotinib. Clin Pharmacol Ther 87:197-203
113. De Bruijn P et al (2010) Bioanalytical method for the quanti fication of sunitinib and its n-desethyl metabolite SU12662 in human plasma by ultra performance liquid chromatography/tandem triple-quadrupole mass spectrometry. J Pharm Biomed Anal 51:934-941
114. Minkin P et al (2008) Quanti fication of sunitinib in human plasma by high-performance liquid chromatography-tandem mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci 874:84-88
115. Jain L et al (2008) Development of a rapid and sensitive LC-MS/MS assay for the determination of sorafenib in human plasma. J Pharm Biomed Anal 46:362-367
116. Zhao M et al (2007) A rapid and sensitive method for determination of sorafenib in human plasma using a liquid chromatography/tandem mass spectrometry assay. J Chromatogr B Analyt Technol Biomed Life Sci 846:1-7
117. Bai F et al (2006) Determination of lapatinib (GW572016) in human plasma by liquid chromatography electrospray tandem mass spectrometry (LC-ESI-MS/MS). J Chromatogr B Analyt Technol Biomed Life Sci 831:169-175
118. Bai F et al (2011) Determination of vandetanib in human plasma and cerebrospinal fluid by liquid chromatography electrospray ionization tandem mass spectrometry (LC-ESI-MS/MS). J Chromatogr B Analyt Technol Biomed Life Sci 879:2561-2566
119. Lankheet AG et al (2009) A validated assay for the quantitative analysis of vatalanib in human EDTA plasma by liquid chromatography coupled with electrospray ionization tandem mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci 877:3625-3630
120. Sparidans RW et al (2009) Liquid chromatography-tandem mass spectrometric assay for the light sensitive tyrosine kinase inhibitor axitinib in human plasma. J Chromatogr B Analyt Technol Biomed Life Sci 877:4090-4096
121. Novakova L et al (2006) Advantages of application of UPLC in pharmaceutical analysis. Talanta 68:908-918
122. Haouala A et al (2009) Therapeutic drug monitoring of the new targeted anticancer agents imatinib, nilotinib, dasatinib, sunitinib, sorafenib and lapatinib by LC tandem mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci 877:1982-1996
123. Baratte S et al (2004) Quantitation of SU1 1248, an oral multi-target tyrosine kinase inhibitor, and its metabolite in monkey tissues by liquid chromatograph with tandem mass spectrometry following semi-automated liquid-liquid extraction. J Chromatogr A 1024:87-94
124. Anja Goedl P. P. Fizer, Personal communication. 12 Dec. 2007
125. Yamazaki S et al (2011) Prediction of oral pharmacokinetics of cMet kinase inhibitors in humans: physiologically based pharmacokinetic model versus traditional one-compartment model. Drug Metab Dispos 39:383-393
126. Christopher LJ et al (2008) Metabolism and disposition of dasatinib after oral administration to humans. Drug Metab Dispos 36:1357-1364
127. Furlong MT et al (2012) A validated LC-MS/MS assay for the simultaneous determination of the anti-leukemic agent dasatinib and two pharmacologically active metabolites in human plasma: application to a clinical pharmacokinetic study. J Pharm Biomed Anal 58:130-135
128. He K et al (2008) N-in-1 dosing pharmacokinetics in drug discovery: experience, theoretical and practical considerations. J Pharm Sci 97:2568-2580
129. Wu JT et al (2000) Direct plasma sample injection in multiple-component LC-MS-MS assays for high-throughput pharmacokinetic screening. Anal Chem 72:61-67
130. Hsieh Y et al (2002) Direct cocktail analysis of drug discovery compounds in pooled plasma samples using liquid chromatography-tandem mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci 767:353-362
131. Kuo BS et al (1998) Sample pooling to expedite bioanalysis and pharmacokinetic research. J Pharm Biomed Anal 16:837-846
132. Kummar S et al (2010) Utilizing targeted cancer therapeutic agents in combination: novel approaches and urgent requirements. Nat Rev Drug Discov 9:843-856
133. De Francia S et al (2009) New HPLC-MS method for the simultaneous quanti fication of the antileukemia drugs imatinib, dasatinib, and nilotinib in human plasma. J Chromatogr B Analyt Technol Biomed Life Sci 877:1721-1726
134. Demetri GD et al (2009) Phase I dose-escalation and pharmacokinetic study of dasatinib in patients with advanced solid tumors. Clin Cancer Res 15:6232-6240
135. Chahbouni A et al (2009) Simultaneous quanti fication of erlotinib, ge fitinib, and imatinib in human plasma by liquid chromatography tandem mass spectrometry. Ther Drug Monit 31:683-687
136. Honeywell R et al (2010) Simple and selective method for the determination of various tyrosine kinase inhibitors used in the clinical setting by liquid chromatography tandem mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci 878:1059-1068
137. Gotze L et al (2012) Development and clinical application of a LC-MS/MS method for simultaneous determination of various tyrosine kinase inhibitors in human plasma. Clin Chim Acta 413:143-149
138. Bouchet S et al (2011) Simultaneous determination of nine tyrosine kinase inhibitors by 96-well solid-phase extraction and ultra performance LC/MS-MS. Clin Chim Acta 412:1060-1067
139. Neeman M et al. (2011) A LC-MS/MS for the assay of verumafenib, bosutinib, ge fitinib and erlotinib in plasma from cancer patients, Master thesis, School of Pharmaceutical Sciences, University of Geneva and Lausanne, Switzerland
140. Rudin CM et al (2008) Pharmacogenomic and pharmacokinetic determinants of erlotinib toxicity. J Clin Oncol 26:1119-1127
141. Roche S et al (2009) Development of a high-performance liquid chromatographic-mass spectrometric method for the determination of cellular levels of the tyrosine kinase inhibitors lapatinib and dasatinib. J Chromatogr B Analyt Technol Biomed Life Sci 877:3982-3990
142. Hegedus C et al (2009) Interaction of nilotinib, dasatinib and bosutinib with ABCB1 and ABCG2: implications for altered anti-cancer effects and pharmacological properties. Br J Pharmacol 158:1153-1164
143. Haouala A et al (2010) SiRNA-mediated knock-down of P-glycoprotein expression reveals distinct cellular disposition of anticancer tyrosine kinases inhibitors. Drug Metab Lett 4:114-119
144. D'Avolio A et al (2012) HPLC-MS method for the simultaneous quanti fication of the antileukemia drugs imatinib, dasatinib and nilotinib in human peripheral blood mononuclear cell (PBMC). J Pharm Biomed Anal 59:109-116
145. Dahmane E et al (2010) An ultra performance liquid chromatography-tandem MS assay for tamoxifen metabolites pro filing in plasma: first evidence of 4'-hydroxylated metabolites in breast cancer patients. J Chromatogr B Analyt Technol Biomed Life Sci 878:3402-3414
146. Jordan VC (2003) Tamoxifen: a most unlikely pioneering medicine. Nat Rev Drug Discov 2:205-213
147. Jordan VC (2006) Tamoxifen (ICI46, 474) as a targeted therapy to treat and prevent breast cancer. Br J Pharmacol 147(Suppl 1):S269-S276
148. Jordan VC (2007) New insights into the metabolism of tamoxifen and its role in the treatment and prevention of breast cancer. Steroids 72:829-842
149. Osborne CK (1998) Tamoxifen in the treatment of breast cancer. N Engl J Med 339:1609-1618
150. Tamoxifen for early breast cancer: an overview of the randomised trials. Early Breast Cancer Trialists' Collaborative Group (1998). Lancet 351:1451-1467
151. Early Breast Cancer Trialists' Collaborative Group (EBCTCG) (2005) Effects of chemotherapy and hormonal therapy for early breast cancer on recurrence and 15-year survival: an overview of the randomised trials. Lancet 365:1687-1717
152. Goldhirsch A et al (2007) Progress and promise: highlights of the international expert consensus on the primary therapy of early breast cancer 2007. Ann Oncol 18:1133-1144
153. Goldhirsch A et al (2009) Thresholds for therapies: highlights of the St gallen international expert consensus on the primary therapy of early breast cancer 2009. Ann Oncol 20:1319-1329
154. Visvanathan K et al (2009) American society of clinical oncology clinical practice guideline update on the use of pharmacologic interventions including tamoxifen, raloxifene, and aromatase inhibition for breast cancer risk reduction. J Clin Oncol 27:3235-3258
155. Mathew J et al (2009) Neoadjuvant endocrine treatment in primary breast cancer - review of literature. Breast 18:339-344
156. Chia YH et al (2010) Neoadjuvant endocrine therapy in primary breast cancer: indications and use as a research tool. Br J Cancer 103:759-764
157. Cuzick J et al (2011) Preventive therapy for breast cancer: a consensus statement. Lancet Oncol 12(5):496-503
158. Jensen EV et al (2003) The estrogen receptor: a model for molecular medicine. Clin Cancer Res 9:1980-1989
159. Riggs BL et al (2003) Selective estrogen-receptor modulators - mechanisms of action and application to clinical practice. N Engl J Med 348:618-629
160. Nilsson S et al (2005) Oestrogen receptors and selective oestrogen receptor modulators: molecular and cellular pharmacology. Basic Clin Pharmacol Toxicol 96:15-25
161. Orlando L et al (2010) Molecularly targeted endocrine therapies for breast cancer. Cancer Treat Rev 36(Suppl 3):S67-S71
162. Johnson MD et al (2004) Pharmacological characterization of 4-hydroxy-N-desmethyl tamoxifen, a novel active metabolite of tamoxifen. Breast Cancer Res Treat 85:151-159
163. Lim YC et al (2005) Endoxifen (4-hydroxy-N-desmethyl-tamoxifen) has anti-estrogenic effects in breast cancer cells with potency similar to 4-hydroxy-tamoxifen. Cancer Chemother Pharmacol 55:471-478
164. Lim YC et al (2006) Endoxifen, a secondary metabolite of tamoxifen, and 4-OH-tamoxifen induce similar changes in global gene expression patterns in MCF-7 breast cancer cells. J Pharmacol Exp Ther 318:503-512
165. Goetz MP et al (2008) Tamoxifen pharmacogenomics: the role of CYP2D6 as a predictor of drug response. Clin Pharmacol Ther 83:160-166
166. Wu X et al (2009) The tamoxifen metabolite, endoxifen, is a potent antiestrogen that targets estrogen receptor alpha for degradation in breast cancer cells. Cancer Res 69:1722-1727
167. Wu X et al (2011) Estrogen receptor-beta sensitizes breast cancer cells to the anti-estrogenic actions of endoxifen. Breast Cancer Res 13:R27
168. Crewe HK et al (1997) Variable contribution of cytochromes P450 2D6, 2 C9 and 3A4 to the 4-hydroxylation of tamoxifen by human liver microsomes. Biochem Pharmacol 53:171-178
169. Coller JK et al (2002) The in fluence of CYP2B6, CYP2C9 and CYP2D6 genotypes on the formation of the potent antioestrogen Z-4-hydroxy-tamoxifen in human liver. Br J Clin Pharmacol 54:157-167
170. Crewe HK et al (2002) Metabolism of tamoxifen by recombinant human cytochrome P450 enzymes: formation of the 4-hydroxy, 4'-hydroxy and N-desmethyl metabolites and isomerization of trans-4-hydroxytamoxifen. Drug Metab Dispos 30:869-874
171. Desta Z et al (2004) Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6. J Pharmacol Exp Ther 310:1062-1075
172. Jin Y et al (2005) CYP2D6 Genotype, antidepressant use, and tamoxifen metabolism during adjuvant breast cancer treatment. J Natl Cancer Inst 97:30-39
173. Madlensky L et al (2011) Tamoxifen metabolite concentrations, CYP2D6 genotype, and breast cancer outcomes. Clin Pharmacol Ther 89:718-725
174. Zheng Y et al (2007) Elimination of antiestrogenic effects of active tamoxifen metabolites by glucuronidation. Drug Metab Dispos 35:1942-1948
175. Kaku T et al (2004) Quaternary ammonium-linked glucuronidation of tamoxifen by human liver microsomes and UDP-glucuronosyltransferase 1A4. Biochem Pharmacol 67:2093-2102
176. Ogura K et al (2006) Quaternary ammonium-linked glucuronidation of trans-4-hydroxytamoxifen, an active metabolite of tamoxifen, by human liver microsomes and UDP-glucuronosyltransferase 1A4. Biochem Pharmacol 71:1358-1369
177. Sun D et al (2006) Characterization of tamoxifen and 4-hydroxytamoxifen glucuronidation by human UGT1A4 variants. Breast Cancer Res 8:R50
178. Benoit-Biancamano MO, et al. (2009) A pharmacogenetics study of the human glucuronosyltransferase UGT1A4. Pharmacogenet Genomics [Epub ahead of print]
179. Sun D et al (2007) Glucuronidation of active tamoxifen metabolites by the human UDP glucuronosyltransferases. Drug Metab Dispos 35:2006-2014
180. Blevins-Primeau AS et al (2009) Functional significance of UDP-glucuronosyltransferase variants in the metabolism of active tamoxifen metabolites. Cancer Res 69:1892-1900
181. Chen G et al (2002) 4-Hydroxytamoxifen sulfation metabolism. J Biochem Mol Toxicol 16:279-285
182. Nishiyama T et al (2002) Reverse geometrical selectivity in glucuronidation and sulfation of cis- and trans-4-hydroxytamoxifens by human liver UDP-glucuronosyltransferases and sulfotransferases. Biochem Pharmacol 63:1817-1830
183. Falany JL et al (2006) Sulfation of raloxifene and 4-hydroxytamoxifen by human cytosolic sulfotransferases. Drug Metab Dispos 34:361-368
184. Nowell S et al (2006) Pharmacogenetics of human cytosolic sulfotransferases. Oncogene 25:1673-1678
185. Lien EA et al (1988) Identi fication of 4-hydroxy-N-desmethyltamoxifen as a metabolite of tamoxifen in human bile. Cancer Res 48:2304-2308
186. Lien EA et al (1989) Distribution of 4-hydroxy-N-desmethyltamoxifen and other tamoxifen metabolites in human biological fluids during tamoxifen treatment. Cancer Res 49:2175-2183
187. Kisanga ER et al (2005) Excretion of hydroxylated metabolites of tamoxifen in human bile and urine. Anticancer Res 25:4487-4492
188. Ring A et al (2004) Mechanisms of tamoxifen resistance. Endocr Relat Cancer 11:643-658
189. Hoskins J et al (2009) CYP2D6 And tamoxifen: DNA matters in breast cancer. Nat Rev Cancer 9:576-586
190. Zhou SF (2009) Polymorphism of human cytochrome P450 2D6 and its clinical signi ficance: part I. Clin Pharmacokinet 48:689-723
191. Zhou SF (2009) Polymorphism of human cytochrome P450 2D6 and its clinical signi ficance: part II. Clin Pharmacokinet 48:761-804
192. Lim HS et al (2007) Clinical implications of CYP2D6 genotypes predictive of tamoxifen pharmacokinetics in metastatic breast cancer. J Clin Oncol 25:3837-3845
193. Gjerde J et al (2008) Effects of CYP2D6 and SULT1A1 genotypes including SULT1A1 gene copy number on tamoxifen metabolism. Ann Oncol 19:56-61
194. ∗10 genotype and survival of breast cancer patients receiving tamoxifen treatment. Ann of Oncol Off J Eur Soc Med Oncol/ESMO 19:1423-1429
195. Kiyotani K et al (2010) Signi ficant effect of polymorphisms in CYP2D6 and ABCC2 on clinical outcomes of adjuvant tamoxifen therapy for breast cancer patients. J Clin Oncol 28:1287-1293
196. Murdter TE et al (2011) Activity levels of tamoxifen metabolites at the estrogen receptor and the impact of genetic polymorphisms of phase I and II enzymes on their concentration levels in plasma. Clin Pharmacol Ther 89:708-717
197. Goetz MP et al (2005) Pharmacogenetics of tamoxifen biotransformation is associated with clinical outcomes of efficacy and hot flashes. J Clin Oncol 23:9312-9318
198. Goetz MP et al (2007) The impact of cytochrome P450 2D6 metabolism in women receiving adjuvant tamoxifen. Breast Cancer Res Treat 101:113-121
199. Schroth W et al (2007) Breast cancer treatment outcome with adjuvant tamoxifen relative to patient CYP2D6 and CYP2C19 genotypes. J Clin Oncol 25:5187-5193
200. ∗10 on recurrence-free survival in breast cancer patients receiving adjuvant tamoxifen therapy. Cancer Sci 99:995-999
201. Newman WG et al (2008) Impaired tamoxifen metabolism reduces survival in familial breast cancer patients. Clin Cancer Res 14:5913-5918
202. Schroth W et al (2009) Association between CYP2D6 polymorphisms and outcomes among women with early stage breast cancer treated with tamoxifen. JAMA 302:1429-1436
203. ∗4 polymorphism affects breast cancer survival in tamoxifen users. Breast Cancer Res Treat 118:125-130
204. Ramon y Cajal T et al (2010) Impact of CYP2D6 polymorphisms in tamoxifen adjuvant breast cancer treatment. Breast Cancer Res Treat 119:33-38
205. Serrano D et al (2011) Efficacy of tamoxifen based on cytochrome P450 2D6, CYP2C19 and SULT1A1 genotype in the Italian tamoxifen prevention trial. Pharmacogenomics J 11:100-107
206. Nowell S et al (2005) Association of genetic variation in tamoxifen-metabolizing enzymes with overall survival and recurrence of disease in breast cancer patients. Breast Cancer Res Treat 91:249-258
207. Wegman P et al (2005) Genotype of metabolic enzymes and the bene fit of tamoxifen in postmenopausal breast cancer patients. Breast Cancer Res 7:R284-R290
208. Wegman P et al (2007) Genetic variants of CYP3A5, CYP2D6, SULT1A1, UGT2B15 and tamoxifen response in postmenopausal patients with breast cancer. Breast Cancer Res 9:R7
209. Okishiro M et al (2009) Genetic polymorphisms of CYP2D6 10 and CYP2C19 2, 3 are not associated with prognosis, endometrial thickness, or bone mineral density in Japanese breast cancer patients treated with adjuvant tamoxifen. Cancer 115:952-961
210. Lash T et al (2009) Genotype-guided tamoxifen therapy: time to pause for re flection? Lancet Oncol 10:825-833
211. Nowell S et al (2002) Association between sulfotransferase 1A1 genotype and survival of breast cancer patients receiving tamoxifen therapy. J Natl Cancer Inst 94:1635-1640
212. Teft WA et al (2011) Endoxifen, the active metabolite of tamoxifen, is a substrate of the efflux transporter P-glycoprotein (multidrug resistance 1). Drug Metab Dispos 39:558-562
213. Iusuf D et al (2011) P-glycoprotein (ABCB1) transports the primary active tamoxifen metabolites endoxifen and 4-hydroxytamoxifen and restricts their brain penetration. J Pharmacol Exp Ther 337:710-717
214. Kiyotani K et al (2012) Pharmacogenomics of tamoxifen: roles of drug metabolizing enzymes and transporters. Drug Metab Pharmacokinet 27(1):122-131
215. Partridge AH et al (2003) Nonadherence to adjuvant tamoxifen therapy in women with primary breast cancer. J Clin Oncol 21:602-606
216. McCowan C et al (2008) Cohort study examining tamoxifen adherence and its relationship to mortality in women with breast cancer. Br J Cancer 99:1763-1768
217. Dezentje VO et al (2010) Effect of concomitant CYP2D6 inhibitor use and tamoxifen adherence on breast cancer recurrence in early-stage breast cancer. J Clin Oncol 28:2423-2429
218. Beer B et al (2010) Development and validation of a liquid chromatography-tandem mass spectrometry method for the simultaneous quanti fication of tamoxifen, anastrozole, and letrozole in human plasma and its application to a clinical study. Anal Bioanal Chem 398:1791-1800
219. Hershman DL et al (2010) Early discontinuation and nonadherence to adjuvant hormonal therapy in a cohort of 8, 769 early-stage breast cancer patients. J Clin Oncol 28:4120-4128
220. Hershman DL et al (2011) Early discontinuation and non-adherence to adjuvant hormonal therapy are associated with increased mortality in women with breast cancer. Breast Cancer Res Treat 126:529-537
221. Kelly C et al (2010) Selective serotonin reuptake inhibitors and breast cancer mortality in women receiving tamoxifen: a population based cohort study. BMJ 340:c693
222. Lammers LA et al (2010) The impact of CYP2D6-predicted phenotype on tamoxifen treatment outcome in patients with metastatic breast cancer. Br J Cancer 103:765-771
223. Ahern TP et al (2009) No increase in breast cancer recurrence with concurrent use of tamoxifen and some CYP2D6-inhibiting medications. Cancer Epidemiol Biomarkers Prev 18:2562-2564
224. Cronin-Fenton D et al (2010) Selective serotonin reuptake inhibitors and adjuvant tamoxifen therapy: risk of breast cancer recurrence and mortality. Future Oncol 6:877-880
225. Lash T et al (2010) Breast cancer recurrence risk related to concurrent use of SSRI antidepressants and tamoxifen. Acta Oncol 49(3):305-312
226. Irvin WJ Jr et al (2011) Genotype-guided tamoxifen dosing increases active metabolite exposure in women with reduced CYP2D6 metabolism: a multicenter study. J Clin Oncol 29:3232-3239
227. Kiyotani K et al (2012) Dose-adjustment study of tamoxifen based on CYP2D6 genotypes in Japanese breast cancer patients. Breast Cancer Res Treat 131(1):137-145
228. Barginear MF et al (2011) Increasing tamoxifen dose in breast cancer patients based on CYP2D6 genotypes and endoxifen levels: effect on active metabolite isomers and the antiestrogenic activity score. Clin Pharmacol Ther 90:605-611
229. Lien EA et al (1987) Determination of tamoxifen and four metabolites in serum by low-dispersion liquid chromatography. Clin Chem 33:1608-1614
230. Lee KH et al (2003) Quanti fication of tamoxifen and three metabolites in plasma by highperformance liquid chromatography with fluorescence detection: application to a clinical trial. J Chromatogr B Analyt Technol Biomed Life Sci 791:245-253
231. Zhu YB et al (2008) Optimizing high-performance liquid chromatography method with fluorescence detection for quanti fication of tamoxifen and two metabolites in human plasma: application to a clinical study. J Pharm Biomed Anal 46:349-355
232. Esteve-Romero J et al (2010) Tamoxifen monitoring studies in breast cancer patients by micellar liquid chromatography. Anal Bioanal Chem 397:1557-1561
233. Carter SJ et al (2001) Biomonitoring of urinary tamoxifen and its metabolites from breast cancer patients using nonaqueous capillary electrophoresis with electrospray mass spectrometry. Electrophoresis 22:2730-2736
234. Mihailescu R et al (2000) Identi fication of tamoxifen and metabolites in human male urine by GC/MS. Biomed Chromatogr 14:180-183
235. Zweigenbaum J et al (2000) Bioanalytical high-throughput selected reaction monitoring-LC/MS determination of selected estrogen receptor modulators in human plasma: 2000 samples/day. Anal Chem 72:2446-2454
236. Sheth HR et al (2003) Aging may be associated with concentrations of tamoxifen and its metabolites in breast cancer patients. J Womens Health 12:799-808
237. Tucker AN et al (2005) Polymorphisms in cytochrome P4503A5 (CYP3A5) may be associated with race and tumor characteristics, but not metabolism and side effects of tamoxifen in breast cancer patients. Cancer Lett 217:61-72
238. Gjerde J et al (2005) Identi fication and quanti fication of tamoxifen and four metabolites in serum by liquid chromatography-tandem mass spectrometry. J Chromatogr A 1082:6-14
239. Williams LD et al (2006) Quanti fication of tamoxifen and metabolites and soy iso flavones in human plasma using liquid chromatography with electrospray ionization tandem mass spectrometry. J AOAC Int 89:1168-1173
240. Wu AH et al (2007) Tamoxifen, soy, and lifestyle factors in Asian American women with breast cancer. J Clin Oncol 25:3024-3030
241. Furlanut M et al (2007) Tamoxifen and its main metabolites serum and tissue concentrations in breast cancer women. Ther Drug Monit 29:349-352
242. Teunissen SF et al (2009) Development and validation of a quantitative assay for the analysis of tamoxifen with its four main metabolites and the flavonoids daidzein, genistein and glycitein in human serum using liquid chromatography coupled with tandem mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci 877:2519-2529
243. Ahmad A et al (2010) Orally administered endoxifen is a new therapeutic agent for breast cancer. Breast Cancer Res Treat 122:579-584
244. Ahmad A et al (2010) Endoxifen, a new cornerstone of breast cancer therapy: demonstration of safety, tolerability, and systemic bioavailability in healthy human subjects. Clin Pharmacol Ther 88:814-817
245. Jaremko M et al (2010) Tamoxifen metabolite isomer separation and quanti fication by liquid chromatography-tandem mass spectrometry. Anal Chem 82:10186-10193
246. Teunissen SF et al (2011) Development and validation of a quantitative assay for the determination of tamoxifen and its five main phase I metabolites in human serum using liquid chromatography coupled with tandem mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci 879:1677-1685
247. Binkhorst L et al (2011) Quanti fication of tamoxifen and three of its phase-I metabolites in human plasma by liquid chromatography/triple-quadrupole mass spectrometry. J Pharm Biomed Anal 56:1016-1023
248. Poon GK et al (1993) Analysis of phase I and phase II metabolites of tamoxifen in breast cancer patients. Drug Metab Dispos 21:1119-1124
249. Poon GK et al (1995) Identi fication of tamoxifen metabolites in human Hep G2 cell line, human liver homogenate, and patients on long-term therapy for breast cancer. Drug Metab Dispos 23:377-382
250. Jones RM et al (1996) On-line high-performance liquid chromatographic-electrospray ionization mass spectrometric method for the study of tamoxifen metabolism. J Chromatogr A 722:249-255
251. Lim CK et al (1997) Identi fication and mechanism of formation of potentially genotoxic metabolites of tamoxifen: study by LC-MS/MS. J Pharm Biomed Anal 15:1335-1342
252. Boocock DJ et al (2002) Identi fication of human CYP forms involved in the activation of tamoxifen and irreversible binding to DNA. Carcinogenesis 23:1897-1901
253. Mazzarino M et al (2008) A mass spectrometric approach for the study of the metabolism of clomiphene, tamoxifen and toremifene by liquid chromatography time-of-flight spectroscopy. Eur J Mass Spectrom 14:171-180
254. Mazzarino M et al (2010) Mass spectrometric characterization of tamoxifene metabolites in human urine utilizing different scan parameters on liquid chromatography/tandem mass spectrometry. Rapid Commun Mass Spectrom 24:749-760
255. Teunissen SF et al (2010) Bioanalytical methods for determination of tamoxifen and its phase I metabolites: a review. Anal Chim Acta 683:21-37
256. Matuszewski BK et al (2003) Strategies for the assessment of matrix effect in quantitative bioanalytical methods based on HPLC-MS/MS. Anal Chem 75:3019-3030
257. Matuszewski BK (2006) Standard line slopes as a measure of a relative matrix effect in quantitative HPLC-MS bioanalysis. J Chromatogr B Analyt Technol Biomed Life Sci 830:293-300
258. Lindegardh N et al (2008) Development and validation of a liquid chromatographic-tandem mass spectrometric method for determination of piperaquine in plasma stable isotope labeled internal standard does not always compensate for matrix effects. J Chromatogr B Analyt Technol Biomed Life Sci 862:227-236
259. Bonfiglio R et al (1999) The effects of sample preparation methods on the variability of the electrospray ionization response for model drug compounds. Rapid Commun Mass Spectrom 13:1175-1185
260. Viswanathan CT et al (2007) Quantitative bioanalytical methods validation and implementation: best practices for chromatographic and ligand binding assays. Pharm Res 24:1962-1973
261. Polson C et al (2003) Optimization of protein precipitation based upon effectiveness of protein removal and ionization effect in liquid chromatography-tandem mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci 785:263-275
262. Souverain S et al (2004) Protein precipitation for the analysis of a drug cocktail in plasma by LC-ESI-MS. J Pharm Biomed Anal 35:913-920
263. Ismaiel OA et al (2010) Investigation of endogenous blood plasma phospholipids, cholesterol and glycerides that contribute to matrix effects in bioanalysis by liquid chromatography/mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci 878:3303-3316
264. Van Eeckhaut A et al (2009) Validation of bioanalytical LC-MS/MS assays: evaluation of matrix effects. J Chromatogr B Analyt Technol Biomed Life Sci 877:2198-2207
265. Hewavitharana AK (2011) Matrix matching in liquid chromatography-mass spectrometry with stable isotope labelled internal standards-is it necessary? J Chromatogr A 1218:359-361
266. Imatinib Concentration Monitoring Evaluation (I-COME). http://www.controlled-trials.com/ISRCTN 31181395
267. European Treatment and Outcome Study (EUTOS). http://www.eutos.org
268. ASQUALAB, Paris, France. http://www.asqualab.com
269. Guiducci C et al. ISyPeM: Intelligent Integrated Systems for Personalised Medicine. http://www.nano-tera.ch/projects/405.php