Population analysis of erlotinib in adults and children reveals pharmacokinetic characteristics as the main factor explaining tolerance particularities in children

Clinical Cancer Research

Volumn 17, Issue 14, 2011, Pages 4862-4871

  White Koning, Melanie ^a   Civade, Elodie ^a   Geoerger, Birgit ^b,c   Thomas, Fabienne ^a   Deley, Marie Cécile Le ^c   Hennebelle, Isabelle ^a   Delord, Jean Pierre ^a   Chatelut, Etienne ^a   Vassal, Gilles ^b,c  

^a UNIVERSITÉ DE TOULOUSE   (France)

^b France   (France)

^c INSTITUT GUSTAVE ROUSSY   (France)

Author keywords

[No Author keywords available]

Indexed keywords

ALANINE AMINOTRANSFERASE; CARBAMAZEPINE; DEXAMETHASONE; DRUG METABOLITE; ERLOTINIB; GLUCOCORTICOID; OSI 420; PHENYTOIN; PREDNISOLONE; PREDNISONE; UNCLASSIFIED DRUG;

ABCB1 GENE; ABCG2 GENE; ADOLESCENT; ADULT; AGE; AGED; AREA UNDER THE CURVE; ARTICLE; BODY WEIGHT; BRAIN CANCER; CANCER RADIOTHERAPY; CHILD; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CYP3A5 GENE; DRUG ABSORPTION; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG DOSE ESCALATION; DRUG EXPOSURE; DRUG TOLERANCE; FEMALE; GENE; GLIOMA; HEAD AND NECK CARCINOMA; HUMAN; MAJOR CLINICAL STUDY; MALE; PHASE 1 CLINICAL TRIAL; PRESCHOOL CHILD; PRIORITY JOURNAL; RECOMMENDED DRUG DOSE; SCHOOL CHILD; SINGLE NUCLEOTIDE POLYMORPHISM; SKIN TOXICITY;

ADOLESCENT; ADULT; AGED; AGED, 80 AND OVER; ANTINEOPLASTIC AGENTS; BRAIN NEOPLASMS; CARCINOMA, SQUAMOUS CELL; CHILD; CHILD, PRESCHOOL; CYTOCHROME P-450 CYP3A; EXANTHEMA; FEMALE; HEAD AND NECK NEOPLASMS; HUMANS; MALE; MIDDLE AGED; P-GLYCOPROTEIN; POLYMORPHISM, SINGLE NUCLEOTIDE; PROTEIN KINASE INHIBITORS; QUINAZOLINES; RECEPTOR, EPIDERMAL GROWTH FACTOR; YOUNG ADULT;

EID: 79960433378     PISSN: 10780432     EISSN: 15573265     Source Type: Journal    
DOI: 10.1158/1078-0432.CCR-10-3278     Document Type: Article

References (39)

1. Li J, Zhao M, He P, Hidalgo M, Baker SD. Differential metabolism of gefitinib and erlotinib by human cytochrome P450 enzymes. Clin Cancer Res 2007;13:3731-7.
2. Ling J, Johnson KA, Miao Z, Rakhit A, Pantze MP, Hamilton M, et al. Metabolism and excretion of erlotinib, a small molecule inhibitor of epidermal growth factor receptor tyrosine kinase, in healthy male volunteers. Drug Metabol Dispos: Biol Fate Chem 2006;34:420-6. (Pubitemid 43290900)
3. Li J, Cusatis G, Brahmer J, Sparreboom A, Robey RW, Bates SE, et al. Association of variant ABCG2 and the pharmacokinetics of epidermal growth factor receptor tyrosine kinase inhibitors in cancer patients. Cancer Biol Ther 2007;6:432-8. (Pubitemid 47328313)
4. Shi Z, Peng XX, Kim IW, Shukla S, Si QS, Robey RW, et al. Erlotinib (Tarceva, OSI-774) antagonizes ATP-binding cassette subfamily B member 1 and ATP-binding cassette subfamily G member 2-mediated drug resistance. Cancer Res 2007;67:11012-20. (Pubitemid 350145931)
5. Johnson JR, Cohen M, Sridhara R, Chen YF, Williams GM, Duan J, et al. Approval summary for erlotinib for treatment of patients with locally advanced or metastatic non-small cell lung cancer after failure of at least one prior chemotherapy regimen. Clin Cancer Res 2005;11:6414-21. (Pubitemid 41338977)
6. Moore MJ, Goldstein D, Hamm J, Figer A, Hecht JR, Gallinger S, et al. Erlotinib plus gemcitabine compared with gemcitabine alone in patients with advanced pancreatic cancer: a phase III trial of the National Cancer Institute of Canada Clinical Trials Group. J Clin Oncol 2007;25:1960-6. (Pubitemid 46972777)
7. Geoerger B, Gaspar N, Opolon P, Morizet J, Devanz P, Lecluse Y, et al. EGFR tyrosine kinase inhibition radiosensitizes and induces apoptosis in malignant glioma and childhood ependymoma xenografts. Int J Cancer 2008;123:209-16. (Pubitemid 351705211)
8. Sarkaria JN, Yang L, Grogan PT, Kitange GJ, Carlson BL, Schroeder MA, et al. Identification of molecular characteristics correlated with glioblastoma sensitivity to EGFR kinase inhibition through use of an intracranial xenograft test panel. Mol Cancer Ther 2007;6:1167-74.
9. Broniscer A, Panetta JC, O'Shaughnessy M, Fraga C, Bai F, Krasin MJ, et al. Plasma and cerebrospinal fluid pharmacokinetics of erlotinib and its active metabolite OSI-420. Clin Cancer Res 2007;13:1511-5. (Pubitemid 46450442)
10. Jakacki RI, Hamilton M, Gilbertson RJ, Blaney SM, Tersak J, Krailo MD, et al. Pediatric phase I and pharmacokinetic study of erlotinib followed by the combination of erlotinib and temozolomide: a Children's Oncology Group Phase I Consortium Study. J Clin Oncol 2008;26:4921-7.
11. Broniscer A, Baker SJ, Stewart CF, Merchant TE, Laningham FH, Schaiquevich P, et al. Phase I and pharmacokinetic studies of erlotinib administered concurrently with radiotherapy for children, adolescents, and young adults with high-grade glioma. Clin Cancer Res 2009;15:701-7.
12. Geoerger B, Hargrave D, Thomas F, Ndiaye A, Frappaz D, Andreiuolo F, et al. Innovative Therapies for Children with Cancer pediatric phase I study of erlotinib in brainstem glioma and relapsing/refractory brain tumors. Neuro-oncology 2010.
13. Debiec-Rychter M, Sciot R, Le Cesne A, Schlemmer M, Hohenberger P, van Oosterom AT, et al. KIT mutations and dose selection for imatinib in patients with advanced gastrointestinal stromal tumours. Eur J Cancer 2006;42:1093-103. (Pubitemid 44275331)
14. Delbaldo C, Chatelut E, Re M, Deroussent A, Seronie-Vivien S, Jambu A, et al. Pharmacokinetic-pharmacodynamic relationships of imatinib and its main metabolite in patients with advanced gastrointestinal stromal tumors. Clin Cancer Res 2006;12:6073-8. (Pubitemid 44703771)
15. Larson RA, Druker BJ, Guilhot F, O'Brien SG, Riviere GJ, Krahnke T, et al. Imatinib pharmacokinetics and its correlation with response and safety in chronic-phase chronic myeloid leukemia: a subanalysis of the IRIS study. Blood 2008;111:4022-8.
16. Picard S, Titier K, Etienne G, Teilhet E, Ducint D, Bernard MA, et al. Trough imatinib plasma levels are associated with both cytogenetic and molecular responses to standard-dose imatinib in chronic myeloid leukemia. Blood 2007;109:3496-9. (Pubitemid 46572540)
17. Demetri GD, Wang Y, Wehrle E, Racine A, Nikolova Z, Blanke CD, et al. Imatinib plasma levels are correlated with clinical benefit in patients with unresectable/metastatic gastrointestinal stromal tumors. J Clin Oncol 2009;27:3141-7.
18. Widmer N, Decosterd LA, Leyvraz S, Duchosal MA, Rosselet A, Debiec-Rychter M, et al. Relationship of imatinib-free plasma levels and target genotype with efficacy and tolerability. Br J Cancer 2008;98:1633-40. (Pubitemid 351684684)
19. Houk BE, Bello CL, Poland B, Rosen LS, Demetri GD, Motzer RJ. Relationship between exposure to sunitinib and efficacy and tolerability endpoints in patients with cancer: results of a pharmacokinetic/pharmacodynamic meta-analysis. Cancer Chemother Pharmacol 2010;66:357-71.
20. Thomas F, Rochaix P, Benlyazid A, Sarini J, Rives M, Lefebvre JL, et al. Pilot study of neoadjuvant treatment with erlotinib in nonmetastatic head and neck squamous cell carcinoma. Clin Cancer Res 2007;13:7086-92. (Pubitemid 350276892)
21. Thomas F, Rochaix P, White-Koning M, Hennebelle I, Sarini J, Benlyazid A, et al. Population pharmacokinetics of erlotinib and its pharmacokinetic/ pharmacodynamic relationships in head and neck squamous cell carcinoma. Eur J Cancer 2009;45:2316-23.
22. Smith M, Bernstein M, Bleyer WA, Borsi JD, Ho P, Lewis IJ, et al. Conduct of phase I trials in children with cancer. J Clin Oncol 1998;16:966-78. (Pubitemid 28108729)
23. Ivanova A. Dose finding in oncology-non-parametric methods. New York, NY: 2006.
24. O'Quigley J, Shen LZ. Continual reassessment method: a likelihood approach. Biometrics 1996;52:673-84. (Pubitemid 26187071)
25. Zhao M, He P, Rudek MA, Hidalgo M, Baker SD. Specific method for determination of OSI-774 and its metabolite OSI-420 in human plasma by using liquid chromatography-tandem mass spectrometry. J Chromatogr 2003;793:413-20. (Pubitemid 37271981)
26. Cascorbi I, Gerloff T, Johne A, Meisel C, Hoffmeyer S, Schwab M, et al. Frequency of single nucleotide polymorphisms in the P-glycoprotein drug transporter MDR1 gene in white subjects. Clin Pharmacol Ther 2001;69:169-74. (Pubitemid 32225417)
27. Asano T, Takahashi KA, Fujioka M, Inoue S, Okamoto M, Sugioka N, et al. ABCB1 C3435T and G2677T/A polymorphism decreased the risk for steroid-induced osteonecrosis of the femoral head after kidney transplantation. Pharmacogenetics 2003;13:675-82. (Pubitemid 38316511)
28. Yates CR, Zhang W, Song P, Li S, Gaber AO, Kotb M, et al. The effect of CYP3A5 and MDR1 polymorphic expression on cyclosporine oral disposition in renal transplant patients. J Clin Pharmacol 2003;43:555-64. (Pubitemid 36613114)
29. Petain A, Kattygnarath D, Azard J, Chatelut E, Delbaldo C, Geoerger B, et al. Population pharmacokinetics and pharmacogenetics of imatinib in children and adults. Clin Cancer Res 2008;14:7102-9.
30. Tod M, Jullien V, Pons G. Facilitation of drug evaluation in children by population methods and modelling. Clin Pharmacokinetics 2008;47:231-43. (Pubitemid 351367434)
31. Christiansen SR, Broniscer A, Panetta JC, Stewart CF. Pharmacokinetics of erlotinib for the treatment of high-grade glioma in a pediatric patient with cystic fibrosis: case report and review of the literature. Pharmacotherapy 2009;29:858-66.
32. Miller AA, Murry DJ, Owzar K, Hollis DR, Lewis LD, Kindler HL, et al. Phase I and pharmacokinetic study of erlotinib for solid tumors in patients with hepatic or renal dysfunction: CALGB 60101. J Clin Oncol 2007;25:3055-60. (Pubitemid 47218052)
33. VanSchaik RHN. CYP3A5 variant allele frequencies in Dutch Caucasians. Clin Chem 2002;48:1668-71.
34. Kuehl P, Zhang J, Lin Y, Lamba J, Assem M, Schuetz J, et al. Sequence diversity in CYP3A promoters and characterization of the genetic basis of polymorphic CYP3A5 expression. Nat Genet 2001;27:383-91. (Pubitemid 32268418)
35. Elmeliegy MA, Carcaboso AM, Tagen M, Bai F, Stewart CF. Role of ATP-binding cassette and solute carrier transporters in erlotinib CNS penetration and intracellular accumulation. Clin Cancer Res 17;89-99.
36. Marchetti S, de Vries NA, Buckle T, Bolijn MJ, van Eijndhoven MA, Beijnen JH, et al. Effect of the ATP-binding cassette drug transporters ABCB1, ABCG2, and ABCC2 on erlotinib hydrochloride (Tarceva) disposition in in vitro and in vivo pharmacokinetic studies employing Bcrp1-/-/Mdr1a/1b-/- (triple-knockout) and wild-type mice. Mol Cancer Ther 2008;7:2280-7.
37. Wacker B, Nagrani T, Weinberg J, Witt K, Clark G, Cagnoni PJ. Correlation between development of rash and efficacy in patients treated with the epidermal growth factor receptor tyrosine kinase inhibitor erlotinib in two large phase III studies. Clin Cancer Res 2007;13:3913-21. (Pubitemid 47037599)
38. Mellinghoff IK, Wang MY, Vivanco I, Haas-Kogan DA, Zhu S, Dia EQ, et al. Molecular determinants of the response of glioblastomas to EGFR kinase inhibitors. New Engl J Med 2005;353:2012-24. (Pubitemid 41609094)
39. Lynch TJ, Bell DW, Sordella R, Gurubhagavatula S, Okimoto RA, Brannigan BW, et al. Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinib. N Engl J Med 2004;350:2129-39. (Pubitemid 38637993)