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

Journal of Clinical Oncology

Volumn 23, Issue 23, 2005, Pages 5305-5313

  Burris III, Howard A ^a   Hurwitz, Herbert I ^a   Dees, E Claire ^a   Dowlati, Afshin ^a   Blackwell, Kimberly L ^a   O'Neil, Bert ^a   Marcom, Paul K ^a   Ellis, Matthew J ^a   Overmoyer, Beth ^a   Jones, Suzanne F ^a   Harris, Jennifer L ^a   Smith, Deborah A ^a   Koch, Kevin M ^a   Stead, Andrew ^a   Mangum, Steve ^a   Spector, Neil L ^a  

^a CASE WESTERN RESERVE UNIVERSITY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

EPIDERMAL GROWTH FACTOR RECEPTOR; EPIDERMAL GROWTH FACTOR RECEPTOR 2; EPIDERMAL GROWTH FACTOR RECEPTOR KINASE INHIBITOR; LAPATINIB; ANTINEOPLASTIC AGENT; QUINAZOLINE DERIVATIVE; TUMOR MARKER;

ADULT; ADVANCED CANCER; AGED; ANTINEOPLASTIC ACTIVITY; AREA UNDER THE CURVE; ARTICLE; BREAST BIOPSY; BREAST METASTASIS; CANCER STAGING; CLINICAL TRIAL; COHORT ANALYSIS; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; DIARRHEA; DRUG BLOOD LEVEL; DRUG FORMULATION; DRUG SAFETY; DRUG TOLERABILITY; FEMALE; GASTROINTESTINAL DISEASE; GENE OVEREXPRESSION; HEART DISEASE; HUMAN; HUMAN TISSUE; INTERSTITIAL PNEUMONIA; MAJOR CLINICAL STUDY; MALE; MASTITIS; PHASE 1 CLINICAL TRIAL; PRIORITY JOURNAL; PROTEIN TARGETING; RANDOMIZED CONTROLLED TRIAL; RASH; TREATMENT DURATION; TREATMENT RESPONSE; BLOOD; DRUG ADMINISTRATION; DRUG ANTAGONISM; DRUG RESISTANCE; MAXIMUM TOLERATED DOSE; METABOLISM; METASTASIS; MIDDLE AGED; NEOPLASM; SAFETY; TREATMENT OUTCOME; TUMOR RECURRENCE;

ADULT; AGED; AGED, 80 AND OVER; ANTINEOPLASTIC AGENTS; DRUG ADMINISTRATION SCHEDULE; DRUG RESISTANCE, NEOPLASM; FEMALE; HUMANS; MALE; MAXIMUM TOLERATED DOSE; MIDDLE AGED; NEOPLASM METASTASIS; NEOPLASM RECURRENCE, LOCAL; NEOPLASMS; QUINAZOLINES; RECEPTOR, EPIDERMAL GROWTH FACTOR; RECEPTOR, ERBB-2; SAFETY; TREATMENT OUTCOME; TUMOR MARKERS, BIOLOGICAL;

EID: 23944476155     PISSN: 0732183X     EISSN: None     Source Type: Journal    
DOI: 10.1200/JCO.2005.16.584     Document Type: Article

References (44)

1. Yarden Y, Sliwkowski MX: Untangling the ErbB signaling network. Nat Rev Mol Cell Biol 2:127-137, 2001
2. Klapper LN, Kirschbaum MH, Sela M, et al: Biochemical and clinical implications of ErbB/HER signaling network of growth factor receptors. Adv Cancer Res 77:25-79, 2000
3. Slamon DJ, Clark GM, Wong SG, et al: Human breast cancer: Correlation of relapse and survival with amplification of the HER-2/neu oncogene. Science 235:177-182, 1987
4. Slamon D, Godolphin W, Jones LA, et al: Studies of the HER-2/neu proto-oncogene in human breast and ovarian cancer. Science 244: 707-712, 1989
5. Bacus SS, Zelnich CR, Plowman G, et al: Expression of the erbB-2 family of growth factor receptors and their ligands in breast cancer: Implication for tumor biology and clinical behavior. Am J Clin Pathol 102:S13-S24, 1994
6. Sainsbury JR, Malcolm AJ, Appleton DR, et al: Presence of epidermal growth factor receptors as an indicator of poor prognosis in patients with breast cancer. J Clin Pathol 38:1225-1228, 1985
7. Olayioye MA, Graus-Porta D, Beerli RR, et al: ErbB-1 and ErbB-2 acquire distinct signaling properties dependent upon their dimerization partner. Mol Cell Biol 18:5042-5051, 1998
8. Ullrich A, Schlessinger J: Signal transduction by receptors with tyrosine kinase activity. Cell 61:203-212, 1990
9. Fukazawa T, Miyake S, Band V, et al: Tyrosine phosphorylation of Cbl upon epidermal growth factor (EGF) stimulation and its association with EGF receptor and downstream signaling proteins. J Biol Chem 271:14554-14559, 1996
10. Hackel PO, Zwick E, Prenzel N, et al: Epidermal growth factor receptors: Critical mediators of multiple receptor pathways. Curr Opin Cell Biol 11:184-189, 1999
11. Tzahar E, Waterman H, Chen X, et al: A hierarchical network of interreceptor interactions determines signal transduction by Neu differentiation factor/neuregulin and epidermal growth factor. Mol Cell Biol 16:5276-5287, 1996
12. Lange CA, Richer JK, Shen T, et al: Convergence of progesterone and epidermal growth factor signaling in breast cancer: Potentiation of mitogen-activated protein kinase pathways. J Biol Chem 273:31308-31316, 1998
13. Moyer JD, Barbacci EG, Iwata KK, et al: Induction of apoptosis and cell cycle arrest by OSI-774, an inhibitor of epidermal growth factor receptor tyrosine kinase. Cancer Res 57:4838-4848, 1997
14. Moasser MM, Basso A, Averbuch SD, et al: The tyrosine kinase inhibitor ZD1839 ("Iressa") inhibits HER2-driven signaling and suppresses the growth of HER2-overexpressing tumor cells. Cancer Res 61:7184-7188, 2001
15. HER2 monoclonal antibody has antiproliferative effects in vitro and sensitizes human breast tumor cells to tumor necrosis factor. Mol Cell Biol 9:1165-1172, 1989
16. Moulder SL, Yakes FM, Muthuswamy SK, et al: Epidermal growth factor receptor (HER1) tyrosine kinase inhibitor ZD1839 (Iressa) inhibits HER2/neu (erbB2)-overexpressing breast cancer cells in vitro and in vivo. Cancer Res 61:8887-8895, 2001
17. Ciardiello F, Caputo R, Bianco R, et al: Antitumor effect and potentiation of cytotoxic drugs activity in human cancer cells by ZD-1839 (Iressa), an epidermal growth factor receptor-selective tyrosine kinase inhibitor. Clin Cancer Res 6:2053-2063, 2000
18. Cobleigh MA, Vogel CL, Tripathy D, et al: Multinational study of the efficacy and safety of humanized anti-Her2 monoclonal antibody in women who have Her2-overexpressing metastatic breast cancer that has progressed after chemotherapy for metastatic disease. J Clin Oncol 17:2639-2648, 1999
19. Mendelsohn J, Baselga J: The EGF receptor as targets for cancer therapy. Oncogene 19:6550-6565, 2000
20. Hecht JR, Patnaik A, Malik I, et al: ABX-EGF monotherapy in patients (pts) with metastatic colorectal cancer (mCRC): An updated analysis. Proc Am Soc Clin Oncol 23:248, 2004 (abstr 3511)
21. Vanhoefer U, Tewes M, Rojo F, et al: Phase I study of the humanized antiepidermal growth factor receptor monoclonal antibody EMD72000 in patients with advanced solid tumors that express the epidermal growth factor receptor. J Clin Oncol 22:175-184, 2004
22. Trigo J, Hitt R, Koralewski P, et al: Cetuximab monotherapy is active in patients (pts) with platinum-refractory recurrent/metastatic squamous cell carcinoma of the head and neck (SCCHN): Results of a phase II study. Proc Am Soc Clin Oncol 23:487, 2004 (abstr 5502)
23. Xia W, Mullin RJ, Keith BR, et al: Anti-tumor activity of GW572016: A dual tyrosine kinase inhibitor blocks EGF activation of EGFR/erbB2 and downstream Erk1/2 and AKT pathways. Oncogene 21:6255-6263, 2002
24. Rusnak DW, Lackey K, Affleck K, et al: The effects of the novel, reversible epidermal growth factor receptor/ErbB-2 tyrosine kinase inhibitor, GW572016, on the growth of human normal and tumor-derived cell lines in vitro and in vivo. Mol Cancer Ther 1:85-94, 2001
25. Bence AK, Anderson EB, Doukas MA, et al: Phase I pharmacokinetic studies evaluating single and multiple doses of oral GW572016, a dual EGFR-ErbB2 inhibitor, in healthy subjects. Invest New Drugs 23:39-49, 2005
26. Versola M, Burris HA, Jones S, et al: Clinical activity of GW572016 in EGF10003 in patients with solid tumors. Proc Am Soc Clin Oncol 23: 2004 (abstr 3047)
27. Spector NL, Xia W, Burris H, III, et al: Study of the biological effects of lapatinib, a reversible inhibitor of ErbB1 and ErbB2 tyrosine kinases, on tumor growth and survival pathways in patients with advanced malignancies. J Clin Oncol 23:1-11, 2005
28. Hsieh S, Tobien T, Koch K, et al: Increasing throughput of parallel on-line extraction liquid chromatography/electrospray ionization tandem mass spectrometry system for GLP quantitative bioanalysis in drug development. Rapid Commun Mass Spectrom 18:285-292, 2004
29. Therasse P, Arbuck SG, Eisenhauer EA, et al: New guidelines to evaluate the response to treatment in solid tumors. J Natl Cancer Inst 92:205-216, 2000
30. Minami H, Nakagawa K, Kawada K, et al: A phase I study of GW572016 in patients with solid tumors. Proc Am Soc Clin Oncol 22:14S, 2004 (abstr 3048)
31. Koch KM, Lee D, Jones S, et al: Pharmacokinetics of GW572016 in an ascending dose
32. tolerability study of phase I cancer patients. Eur J Cancer 1:S169, 2003 (poster 559)
33. Wood ER, Truesdale AT, McDonald OB, et al: A unique structure for epidermal growth factor receptor bound to GW572016 (Lapatinib): Relationships among protein conformation, inhibitor off-rate, and receptor activity in tumor cells. Cancer Res 64:6652-6659, 2004
34. Baselga J, Rischin D, Ranson M, et al: Phase I safety, pharmacokinetic, and pharmacodynamic trial of ZD1839, a selective oral epidermal growth factor receptor tyrosine kinase inhibitor, in patients with five selected tumor types. J Clin Oncol 20:4292-4302, 2002
35. Hidalgo M, Siu LL, Nemunaitis J, et al: Phase I and pharmacologic study of OSI-774, an epidermal growth factor receptor tyrosine kinase inhibitor, in patients with advanced solid malignancies. J Clin Oncol 19:3267-3279, 2001
36. Hoekstra R, Dumez H, van Oosterom AT, et al: A phase I and pharmacological study of PKI166, an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, administered orally in a two weeks on, two weeks off scheme to patients with advanced cancer. Proc Am Soc Clin Oncol 21, 2002 (abstr 340)
37. Dumez H, Hoekstra R, Eskens F, et al: A phase I and pharmacological study of PKI166, an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, administered orally 3 times a week to patients with advanced cancer. Proc Am Soc Clin Oncol 21, 2002 (abstr 341)
38. Murren JR, Papadimitrakopoulou VA, Sizer KC, et al: A phase I dose-escalating study to evaluate the biological activity and pharmacokinetics of PKI166, a novel tyrosine kinase inhibitor, in patients with advanced cancers. Proc Am Soc Clin Oncol 21, 2002 (abstr 377)
39. Garrison MA, Tolcher A, McCreery H, et al: A phase I and pharmacokinetic study of oral CI-1033, a pan-erbB tyrosine kinase inhibitor, given orally on days 1, 8, and 15 every 28 days to patients with solid tumors. Proc Am Soc Clin Oncol 20:72a, 2001 (abstr 283)
40. Nemunaitis JJ, Eiseman C, Cunningham C, et al: A phase I trial of CI-1033, a pan-erbB tyrosine kinase inhibitor, given daily for 14 days every 3 weeks, in patients with solid advanced tumors. Proc Am Soc Clin Oncol 22:243, 2003 (abstr 974)
41. Rinehart JJ, Wilding G, Willson J, et al: A phase I clinical and pharmacokinetic study of oral CI-1033, a pan-erbB tyrosine kinase inhibitor, in patients with advanced solid tumors. Proc Am Soc Clin Oncol 21:11a, 2002 (abstr 41)
42. Shin DM, Nemunaitis JJ, Zinner RG, et al: A phase I biomarker study of CI-1033, a novel pan-erbB tyrosine kinase inhibitor in patients with solid tumors. Proc Am Soc Clin Oncol 20:82a, 2001 (abstr 324)
43. Seidman A, Hudis C, Pierri MK, et al: Cardiac dysfunction in the trastuzumab clinical trials experience. J Clin Oncol 20:1215-1221, 2002
44. Suter TM, Cook-Burns N, Barton C: Cardiotoxicity associated with trastuzumab (Herceptin) therapy in the treatment of metastatic breast cancer. Breast 13:173-183, 2004