quinazolines

Summary

Top Publications

  1. ncbi 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
    Edgar R Wood
    Department of Computational, Analytical and Structural Sciences, GlaxoSmithKline, Inc, Research Triangle Park, North Carolina 27709, USA
    Cancer Res 64:6652-9. 2004
  2. ncbi Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinib
    Thomas J Lynch
    Cancer Center, Massachusetts General Hospital and Harvard Medical School, Boston 02129, USA
    N Engl J Med 350:2129-39. 2004
  3. ncbi Gefitinib or carboplatin-paclitaxel in pulmonary adenocarcinoma
    Tony S Mok
    State Key Laboratory in Oncology in South China, Sir YK Pao Centre for Cancer, Department of Clinical Oncology, Chinese University of Hong Kong, Hong Kong
    N Engl J Med 361:947-57. 2009
  4. ncbi EGFR mutations in lung cancer: correlation with clinical response to gefitinib therapy
    J Guillermo Paez
    Departments of Medical Oncology and Cancer Biology, Dana Farber Cancer Institute, Boston, MA 02115, USA
    Science 304:1497-500. 2004
  5. ncbi Gefitinib or chemotherapy for non-small-cell lung cancer with mutated EGFR
    Makoto Maemondo
    Miyagi Cancer Center, Miyagi, Japan
    N Engl J Med 362:2380-8. 2010
  6. ncbi MET amplification leads to gefitinib resistance in lung cancer by activating ERBB3 signaling
    Jeffrey A Engelman
    Massachusetts General Hospital Cancer Center, Boston, MA 02114, USA
    Science 316:1039-43. 2007
  7. ncbi Gefitinib versus cisplatin plus docetaxel in patients with non-small-cell lung cancer harbouring mutations of the epidermal growth factor receptor (WJTOG3405): an open label, randomised phase 3 trial
    Tetsuya Mitsudomi
    Department of Thoracic Surgery, Aichi Cancer Center Hospital, Chikusa ku, Nagoya, Japan
    Lancet Oncol 11:121-8. 2010
  8. pmc EGF receptor gene mutations are common in lung cancers from "never smokers" and are associated with sensitivity of tumors to gefitinib and erlotinib
    William Pao
    Program in Cancer Biology and Genetics and Department of Medicine, Memorial Sloan Kettering Cancer Center, 1275 York Avenue, New York, NY 10021, USA
    Proc Natl Acad Sci U S A 101:13306-11. 2004
  9. ncbi Erlotinib in previously treated non-small-cell lung cancer
    Frances A Shepherd
    Department of Medical Oncology, University Health Network, Princess Margaret Hospital Site, University of Toronto, Canada
    N Engl J Med 353:123-32. 2005
  10. ncbi Screening for epidermal growth factor receptor mutations in lung cancer
    Rafael Rosell
    Catalan Institute of Oncology and Autonomous University of Barcelona, Hospital Germans Trias i Pujol, Barcelona, Spain
    N Engl J Med 361:958-67. 2009

Research Grants

  1. Antileishmanial Lead Optimization of Quinazolines
    Karl A Werbovetz; Fiscal Year: 2013
  2. DEVELOPMENT OF CANCER IMAGING AGENTS
    Henry VanBrocklin; Fiscal Year: 2000
  3. MOLECULAR AND ELECTRONIC STRUCTURES OF ANTIFOLATE DRUGS
    Vivian Cody; Fiscal Year: 1991
  4. INNOVATIVE TUMOR TARGETED THERAPIES FOR LUNG CANCER
    Roman Perez Soler; Fiscal Year: 2004
  5. CATIONIC LIPID/P53 GENE THERAPY IN LUNG CANCER PATIENTS
    Roman Perez Soler; Fiscal Year: 2003
  6. RADIATION AND DRUG EFFECTS ON TUMOR CELL SUBPOPULATIONS
    Dietmar Siemann; Fiscal Year: 2001
  7. Antiestrogenic Effects on Tumor Angiogenesis
    Kimberly Blackwell; Fiscal Year: 2006
  8. Creatine: Is It a Body Builder for Cancer Patients?
    Aminah Jatoi; Fiscal Year: 2004
  9. Mechanisms and Therapeutics in Cancer Anorexia/Cachexia
    Aminah Jatoi; Fiscal Year: 2004
  10. Neuropeptide Y for Cancer-Associated Anorexia
    Aminah Jatoi; Fiscal Year: 2003

Detail Information

Publications255 found, 100 shown here

  1. ncbi 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
    Edgar R Wood
    Department of Computational, Analytical and Structural Sciences, GlaxoSmithKline, Inc, Research Triangle Park, North Carolina 27709, USA
    Cancer Res 64:6652-9. 2004
    ..The differences in the off-rates of these drugs and the ability of GW572016 to inhibit ErbB-2 can be explained by the enzyme-inhibitor structures...
  2. ncbi Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinib
    Thomas J Lynch
    Cancer Center, Massachusetts General Hospital and Harvard Medical School, Boston 02129, USA
    N Engl J Med 350:2129-39. 2004
    ..However, about 10 percent of patients have a rapid and often dramatic clinical response. The molecular mechanisms underlying sensitivity to gefitinib are unknown...
  3. ncbi Gefitinib or carboplatin-paclitaxel in pulmonary adenocarcinoma
    Tony S Mok
    State Key Laboratory in Oncology in South China, Sir YK Pao Centre for Cancer, Department of Clinical Oncology, Chinese University of Hong Kong, Hong Kong
    N Engl J Med 361:947-57. 2009
    ..Previous, uncontrolled studies have suggested that first-line treatment with gefitinib would be efficacious in selected patients with non-small-cell lung cancer...
  4. ncbi EGFR mutations in lung cancer: correlation with clinical response to gefitinib therapy
    J Guillermo Paez
    Departments of Medical Oncology and Cancer Biology, Dana Farber Cancer Institute, Boston, MA 02115, USA
    Science 304:1497-500. 2004
    ..These results suggest that EGFR mutations may predict sensitivity to gefitinib...
  5. ncbi Gefitinib or chemotherapy for non-small-cell lung cancer with mutated EGFR
    Makoto Maemondo
    Miyagi Cancer Center, Miyagi, Japan
    N Engl J Med 362:2380-8. 2010
    ....
  6. ncbi MET amplification leads to gefitinib resistance in lung cancer by activating ERBB3 signaling
    Jeffrey A Engelman
    Massachusetts General Hospital Cancer Center, Boston, MA 02114, USA
    Science 316:1039-43. 2007
    ..Thus, we propose that MET amplification may promote drug resistance in other ERBB-driven cancers as well...
  7. ncbi Gefitinib versus cisplatin plus docetaxel in patients with non-small-cell lung cancer harbouring mutations of the epidermal growth factor receptor (WJTOG3405): an open label, randomised phase 3 trial
    Tetsuya Mitsudomi
    Department of Thoracic Surgery, Aichi Cancer Center Hospital, Chikusa ku, Nagoya, Japan
    Lancet Oncol 11:121-8. 2010
    ..However, whether gefitinib is better than standard platinum doublet chemotherapy in patients selected by EGFR mutation is uncertain...
  8. pmc EGF receptor gene mutations are common in lung cancers from "never smokers" and are associated with sensitivity of tumors to gefitinib and erlotinib
    William Pao
    Program in Cancer Biology and Genetics and Department of Medicine, Memorial Sloan Kettering Cancer Center, 1275 York Avenue, New York, NY 10021, USA
    Proc Natl Acad Sci U S A 101:13306-11. 2004
    ..Collectively, these data show that adenocarcinomas from never smokers comprise a distinct subset of lung cancers, frequently containing mutations within the TK domain of EGFR that are associated with gefitinib and erlotinib sensitivity...
  9. ncbi Erlotinib in previously treated non-small-cell lung cancer
    Frances A Shepherd
    Department of Medical Oncology, University Health Network, Princess Margaret Hospital Site, University of Toronto, Canada
    N Engl J Med 353:123-32. 2005
    ....
  10. ncbi Screening for epidermal growth factor receptor mutations in lung cancer
    Rafael Rosell
    Catalan Institute of Oncology and Autonomous University of Barcelona, Hospital Germans Trias i Pujol, Barcelona, Spain
    N Engl J Med 361:958-67. 2009
    ..We evaluated the feasibility of large-scale screening for EGFR mutations in such patients and analyzed the association between the mutations and the outcome of erlotinib treatment...
  11. ncbi EGFR mutation and resistance of non-small-cell lung cancer to gefitinib
    Susumu Kobayashi
    Division of Hematology Oncology, Beth Israel Deaconess Medical Center, Harvard Medical School, Boston, USA
    N Engl J Med 352:786-92. 2005
    ..Structural modeling and biochemical studies showed that this second mutation led to gefitinib resistance...
  12. pmc Acquired resistance of lung adenocarcinomas to gefitinib or erlotinib is associated with a second mutation in the EGFR kinase domain
    William Pao
    Program in Cancer Biology and Genetics, Memorial Sloan Kettering Cancer Center, New York, New York, USA
    PLoS Med 2:e73. 2005
    ..Despite initial responses, patients eventually progress by unknown mechanisms of "acquired" resistance...
  13. ncbi 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
    Malcolm J Moore
    Division of Medical Oncology, Princess Margaret Hospital, Toronto, Canada
    J Clin Oncol 25:1960-6. 2007
    ..We studied the effects of adding the HER1/EGFR-targeted agent erlotinib to gemcitabine in patients with unresectable, locally advanced, or metastatic pancreatic cancer...
  14. ncbi Lapatinib plus capecitabine for HER2-positive advanced breast cancer
    Charles E Geyer
    Allegheny Cancer Center, Allegheny General Hospital, Pittsburgh, PA 15212, USA
    N Engl J Med 355:2733-43. 2006
    ..In this trial, we compared lapatinib plus capecitabine with capecitabine alone in such patients...
  15. pmc MET amplification occurs with or without T790M mutations in EGFR mutant lung tumors with acquired resistance to gefitinib or erlotinib
    James Bean
    Human Oncology and Pathogenesis Program, Department of Neurosurgery, Memorial Sloan Kettering Cancer Center, New York, NY 10021, USA
    Proc Natl Acad Sci U S A 104:20932-7. 2007
    ..Taken together, these data suggest that MET amplification occurs independently of EGFR(T790M) mutations and that MET may be a clinically relevant therapeutic target for some patients with acquired resistance to gefitinib or erlotinib...
  16. ncbi Lapatinib with trastuzumab for HER2-positive early breast cancer (NeoALTTO): a randomised, open-label, multicentre, phase 3 trial
    Jose Baselga
    Massachusetts General Hospital Cancer Center, Harvard Medical School, Boston, MA 02114, USA
    Lancet 379:633-40. 2012
    ..We argue that the two anti-HER2 agents given together would be better than single-agent therapy...
  17. pmc The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP
    Cai Hong Yun
    Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, 25 Shattuck Street, Boston, MA 02115, USA
    Proc Natl Acad Sci U S A 105:2070-5. 2008
    ....
  18. ncbi Gefitinib plus best supportive care in previously treated patients with refractory advanced non-small-cell lung cancer: results from a randomised, placebo-controlled, multicentre study (Iressa Survival Evaluation in Lung Cancer)
    Nick Thatcher
    Medical Oncology, Christie Hospital NHS Trust, Manchester M20 4BX, UK
    Lancet 366:1527-37. 2005
    ..This placebo-controlled phase III study investigated the effect on survival of gefitinib as second-line or third-line treatment for patients with locally advanced or metastatic non-small-cell lung cancer...
  19. ncbi Erlotinib as maintenance treatment in advanced non-small-cell lung cancer: a multicentre, randomised, placebo-controlled phase 3 study
    Federico Cappuzzo
    Department of Medical Oncology, Ospedale Civile di Livorno, Livorno, Italy
    Lancet Oncol 11:521-9. 2010
    ....
  20. pmc Understanding resistance to EGFR inhibitors-impact on future treatment strategies
    Deric L Wheeler
    Department of Human Oncology, University of Wisconsin Comprehensive Cancer Center, Madison, WI 53705, USA
    Nat Rev Clin Oncol 7:493-507. 2010
    ..A greater understanding of the mechanisms that lead to EGFR resistance may provide valuable insights to help design new strategies that will enhance the impact of this promising class of inhibitors for the treatment of cancer...
  21. ncbi Cediranib with mFOLFOX6 versus bevacizumab with mFOLFOX6 as first-line treatment for patients with advanced colorectal cancer: a double-blind, randomized phase III study (HORIZON III)
    Hans Joachim Schmoll
    Department of Internal Medicine IV, Hematology and Oncology, University Clinic Halle Saale, Martin Luther University Halle Wittenberg, Ernst Grube Str 40, 06120 Halle, Germany
    J Clin Oncol 30:3588-95. 2012
    ....
  22. pmc KRAS mutations and primary resistance of lung adenocarcinomas to gefitinib or erlotinib
    William Pao
    Program in Cancer Biology and Genetics, Memorial Sloan Kettering Cancer Center, New York, New York, USA
    PLoS Med 2:e17. 2005
    ..Lung adenocarcinomas also harbor activating mutations in the downstream GTPase, KRAS, and mutations in EGFR and KRAS appear to be mutually exclusive...
  23. ncbi Gefitinib versus docetaxel in previously treated non-small-cell lung cancer (INTEREST): a randomised phase III trial
    Edward S Kim
    The University of Texas MD Anderson Cancer Center, Houston, TX, USA
    Lancet 372:1809-18. 2008
    ..We compared gefitinib with docetaxel in patients with locally advanced or metastatic non-small-cell lung cancer who had been pretreated with platinum-based chemotherapy...
  24. pmc Activating and resistance mutations of EGFR in non-small-cell lung cancer: role in clinical response to EGFR tyrosine kinase inhibitors
    A F Gazdar
    Hamon Center for Therapeutic Oncology Research and Department of Pathology, University of Texas Southwestern Medical Center, Dallas, Texas 75390, USA
    Oncogene 28:S24-31. 2009
    ..Various second-generation EGFR TKIs are currently being evaluated and may have the potential to overcome T790M-mediated resistance by virtue of their irreversible inhibition of the receptor TK domain...
  25. ncbi Lapatinib combined with letrozole versus letrozole and placebo as first-line therapy for postmenopausal hormone receptor-positive metastatic breast cancer
    Stephen Johnston
    Royal Marsden Hospital, London, United Kingdom
    J Clin Oncol 27:5538-46. 2009
    ....
  26. pmc BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models
    D Li
    Department of Medical Oncology, Dana Farber Cancer Institute, MA, USA
    Oncogene 27:4702-11. 2008
    ..These findings encourage further testing of BIBW2992 in lung cancer patients harboring EGFR or HER2 oncogenes...
  27. pmc Cardiovascular safety with linagliptin in patients with type 2 diabetes mellitus: a pre-specified, prospective, and adjudicated meta-analysis of a phase 3 programme
    Odd Erik Johansen
    Boehringer Ingelheim, Asker, Norway
    Cardiovasc Diabetol 11:3. 2012
    ..This study investigated the cardiovascular (CV) safety profile of the dipeptidyl peptidase (DPP)-4 inhibitor linagliptin versus comparator treatments...
  28. ncbi TRIBUTE: a phase III trial of erlotinib hydrochloride (OSI-774) combined with carboplatin and paclitaxel chemotherapy in advanced non-small-cell lung cancer
    Roy S Herbst
    University of Texas M D Anderson Cancer Center, Houston, USA
    J Clin Oncol 23:5892-9. 2005
    ..Erlotinib was combined with chemotherapy to determine if it could improve the outcome of patients with NSCLC...
  29. ncbi First-line gefitinib in patients with advanced non-small-cell lung cancer harboring somatic EGFR mutations
    Lecia V Sequist
    Massachusetts General Hospital Cancer Center, 32 Fruit St, Yawkey Suite 7B, Boston, MA 02114, USA
    J Clin Oncol 26:2442-9. 2008
    ..The multicenter iTARGET trial prospectively examined first-line gefitinib in advanced NSCLC patients harboring EGFR mutations and explored the significance of EGFR mutation subtypes and TKI resistance mechanisms...
  30. pmc AKT inhibition relieves feedback suppression of receptor tyrosine kinase expression and activity
    Sarat Chandarlapaty
    Program in Molecular Pharmacology, Memorial Sloan Kettering Cancer Center, New York, NY 10065, USA
    Cancer Cell 19:58-71. 2011
    ..Consistent with this model, we find that, in tumors in which AKT suppresses HER3 expression, combined inhibition of AKT and HER kinase activity is more effective than either alone...
  31. ncbi Phase III study of erlotinib in combination with cisplatin and gemcitabine in advanced non-small-cell lung cancer: the Tarceva Lung Cancer Investigation Trial
    Ulrich Gatzemeier
    Zentrum fur Pneumologie und Thoraxchirurgie, Krankenhaus D LVA, Germany
    J Clin Oncol 25:1545-52. 2007
    ....
  32. ncbi PF00299804, an irreversible pan-ERBB inhibitor, is effective in lung cancer models with EGFR and ERBB2 mutations that are resistant to gefitinib
    Jeffrey A Engelman
    Massachusetts General Hospital Cancer Center, Harvard Medical School, Boston, MA, USA
    Cancer Res 67:11924-32. 2007
    ..These preclinical evaluations support further clinical development of PF00299804 for cancers with mutations and/or amplifications of ERBB family members...
  33. ncbi Efficacy and safety of linagliptin in persons with type 2 diabetes inadequately controlled by a combination of metformin and sulphonylurea: a 24-week randomized study
    D R Owens
    University Hospital Llandough, Cardiff, UK
    Diabet Med 28:1352-61. 2011
    ..0-10.0%)] by metformin and sulphonylurea combination treatment...
  34. pmc Structures of lung cancer-derived EGFR mutants and inhibitor complexes: mechanism of activation and insights into differential inhibitor sensitivity
    Cai Hong Yun
    Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, MA 02115, USA
    Cancer Cell 11:217-27. 2007
    ..Strikingly, direct binding measurements show that gefitinib binds 20-fold more tightly to the L858R mutant than to the wild-type enzyme...
  35. ncbi Genetic heterogeneity of the epidermal growth factor receptor in non-small cell lung cancer cell lines revealed by a rapid and sensitive detection system, the peptide nucleic acid-locked nucleic acid PCR clamp
    Yoshiaki Nagai
    Department of Respiratory Medicine, Saitama Medical School, Moroyama machi, Iruma gun, Saitama, Japan
    Cancer Res 65:7276-82. 2005
    ..Genetic heterogeneity of EGFR suggests that the EGFR gene is unstable in established cancers and the heterogeneity may explain variable clinical responses of lung cancers to gefitinib...
  36. pmc Efficacy of bevacizumab plus erlotinib versus erlotinib alone in advanced non-small-cell lung cancer after failure of standard first-line chemotherapy (BeTa): a double-blind, placebo-controlled, phase 3 trial
    Roy S Herbst
    Department of Thoracic Head and Neck Medical Oncology, The University of Texas, MD Anderson Cancer Center, Houston, TX, USA
    Lancet 377:1846-54. 2011
    ....
  37. ncbi Randomized study of Lapatinib alone or in combination with trastuzumab in women with ErbB2-positive, trastuzumab-refractory metastatic breast cancer
    Kimberly L Blackwell
    Duke University Medical Center, Durham, NC 27701, USA
    J Clin Oncol 28:1124-30. 2010
    ..EGF104900 compared the activity of lapatinib alone or in combination with trastuzumab in patients with ErbB2-positive, trastuzumab-refractory metastatic breast cancer (MBC)...
  38. ncbi A phase III randomized comparison of lapatinib plus capecitabine versus capecitabine alone in women with advanced breast cancer that has progressed on trastuzumab: updated efficacy and biomarker analyses
    David Cameron
    University of Leeds, Leeds, England, UK
    Breast Cancer Res Treat 112:533-43. 2008
    ..Updated efficacy and initial biomarker results from this trial are reported...
  39. pmc Vandetanib for the treatment of patients with locally advanced or metastatic hereditary medullary thyroid cancer
    Samuel A Wells
    Dept of Surgery, Washington University School of Medicine, Box 8109, 660 S Euclid Ave, St Louis, MO 63110, USA
    J Clin Oncol 28:767-72. 2010
    ..These results demonstrate that vandetanib may provide an effective therapeutic option in patients with advanced hereditary MTC, a rare disease for which there has been no effective therapy...
  40. ncbi Molecular predictors of outcome with gefitinib and docetaxel in previously treated non-small-cell lung cancer: data from the randomized phase III INTEREST trial
    Jean Yves Douillard
    M D Anderson Cancer Center, Thoracic Head and Neck Medical Oncology, Box 432, 1515 Holcombe Blvd, Houston, TX 77401, USA
    J Clin Oncol 28:744-52. 2010
    ....
  41. ncbi Mechanisms of tamoxifen resistance: increased estrogen receptor-HER2/neu cross-talk in ER/HER2-positive breast cancer
    Jiang Shou
    The Breast Center, Baylor College of Medicine, Houston, TX 77030, USA
    J Natl Cancer Inst 96:926-35. 2004
    ..We used a breast cancer model system with high expression of AIB1 and HER2 to investigate the possible mechanisms underlying this resistance...
  42. ncbi Epithelial versus mesenchymal phenotype determines in vitro sensitivity and predicts clinical activity of erlotinib in lung cancer patients
    Robert L Yauch
    Department of Molecular Diagnostics, Genentech, Inc, South San Francisco, California 94080, USA
    Clin Cancer Res 11:8686-98. 2005
    ..These data support a potential role for EMT as a determinant of EGFR activity in NSCLC tumor cells and E-cadherin expression as a novel biomarker predicting clinical activity of the EGFR inhibitor erlotinib in NSCLC patients...
  43. ncbi Epithelial to mesenchymal transition derived from repeated exposure to gefitinib determines the sensitivity to EGFR inhibitors in A549, a non-small cell lung cancer cell line
    Jin Kyung Rho
    Department of Internal Medicine, Korea Cancer Center Hospital, Korea Institute of Radiological and Medical Science, Seoul 139 706, Republic of Korea
    Lung Cancer 63:219-26. 2009
    ..Conversely, this was reversed through the removal of TGF-beta1. In conclusion, induction of EMT may contribute to the decreased efficacy of therapy in primary and acquired resistance to gefitinib...
  44. ncbi Epithelial to mesenchymal transition is a determinant of sensitivity of non-small-cell lung carcinoma cell lines and xenografts to epidermal growth factor receptor inhibition
    Stuart Thomson
    Departments of Translational Research and Oncology Research, OSI Pharmaceuticals, Inc, Farmingdale, NY 11735, USA
    Cancer Res 65:9455-62. 2005
    ..These data suggest that EMT may be a general biological switch rendering non-small cell lung tumors sensitive or insensitive to EGFR inhibition...
  45. ncbi Safety and efficacy of linagliptin as add-on therapy to metformin in patients with type 2 diabetes: a randomized, double-blind, placebo-controlled study
    M R Taskinen
    Department of Medicine, Helsinki University Central Hospital, Finland
    Diabetes Obes Metab 13:65-74. 2011
    ..To evaluate the efficacy and safety of the potent and selective dipeptidyl peptidase-4 (DPP-4) inhibitor linagliptin administered as add-on therapy to metformin in patients with type 2 diabetes with inadequate glycaemic control...
  46. ncbi Epithelial to mesenchymal transition in an epidermal growth factor receptor-mutant lung cancer cell line with acquired resistance to erlotinib
    Kenichi Suda
    Department of Thoracic Surgery, Aichi Cancer Center Hospital, Chikusa ku, Nagoya, Japan
    J Thorac Oncol 6:1152-61. 2011
    ..However, recent clinical studies revealed that gefitinib or erlotinib are highly effective in the treatment of non-small cell lung cancer with EGFR mutations...
  47. ncbi Multicenter phase II study of lapatinib in patients with brain metastases from HER2-positive breast cancer
    Nancy U Lin
    Dana Farber Cancer Institute, Boston, Massachusetts 02115, USA
    Clin Cancer Res 15:1452-9. 2009
    ..The current study was done to further evaluate the CNS activity of lapatinib. The study was later amended to allow patients who progressed on lapatinib the option of receiving lapatinib plus capecitabine...
  48. ncbi Gefitinib in combination with paclitaxel and carboplatin in advanced non-small-cell lung cancer: a phase III trial--INTACT 2
    Roy S Herbst
    Department of Thoracic Head and Neck Medical Oncology, University of Texas M D Anderson Cancer Center, 1515 Holcombe Blvd, Unit 432, Houston, TX 77030, USA
    J Clin Oncol 22:785-94. 2004
    ..This phase III, randomized, placebo-controlled, double-blind trial evaluated gefitinib plus paclitaxel and carboplatin in chemotherapy-naive patients with advanced NSCLC...
  49. ncbi Hepatocyte growth factor induces gefitinib resistance of lung adenocarcinoma with epidermal growth factor receptor-activating mutations
    Seiji Yano
    Division of Medical Oncology, Cancer Research Institute, Kanazawa University, Kanazawa, Ishikawa, Japan
    Cancer Res 68:9479-87. 2008
    ..Therefore, inhibition of HGF-MET signaling may be a considerable strategy for more successful treatment with gefitinib...
  50. ncbi Gefitinib in combination with gemcitabine and cisplatin in advanced non-small-cell lung cancer: a phase III trial--INTACT 1
    Giuseppe Giaccone
    Vrije Universiteit Medical Center, Department of Oncology, De Boelelaan 1117, 1081 Amsterdam, The Netherlands
    J Clin Oncol 22:777-84. 2004
    ..Gefitinib has demonstrated encouraging efficacy in advanced NSCLC in phase II trials in pretreated patients, and a phase I trial of gefitinib in combination with gemcitabine and cisplatin showed favorable tolerability...
  51. ncbi AZD2171: a highly potent, orally bioavailable, vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor for the treatment of cancer
    Stephen R Wedge
    Cancer Bioscience, AstraZeneca, Alderley Park, Macclesfield, Cheshire, United Kingdom
    Cancer Res 65:4389-400. 2005
    ..AZD2171 is being developed clinically as a once-daily oral therapy for the treatment of cancer...
  52. pmc Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib
    Eunice L Kwak
    Center for Molecular Therapeutics, Massachusetts General Hospital Cancer Center, Harvard Medical School, Charlestown, MA 02129, USA
    Proc Natl Acad Sci U S A 102:7665-70. 2005
    ..Our findings suggest that one of these, HKI-272, may prove highly effective in the treatment of EGFR-mutant NSCLCs, including tumors that have become resistant to gefitinib or erlotinib...
  53. pmc Transcriptional and posttranslational up-regulation of HER3 (ErbB3) compensates for inhibition of the HER2 tyrosine kinase
    Joan T Garrett
    Department of Medicine, Breast Cancer Research Program, Vanderbilt Ingram Cancer Center, and Vanderbilt University Institute of Imaging Sciences, Vanderbilt University School of Medicine, Nashville, TN 37232, USA
    Proc Natl Acad Sci U S A 108:5021-6. 2011
    ..They also suggest that therapeutic inhibitors of HER3 should be used in combination with HER2 inhibitors and PI3K pathway inhibitors in patients with HER2- and PI3K-dependent cancers...
  54. ncbi Lapatinib versus trastuzumab in combination with neoadjuvant anthracycline-taxane-based chemotherapy (GeparQuinto, GBG 44): a randomised phase 3 trial
    Michael Untch
    HELIOS Klinikum, Berlin Buch, Berlin, Germany
    Lancet Oncol 13:135-44. 2012
    ..We compared the efficacy and safety of the addition of lapatinib versus trastuzumab to anthracycline-taxane-based neoadjuvant chemotherapy...
  55. pmc A phase I dose escalation study of BIBW 2992, an irreversible dual inhibitor of epidermal growth factor receptor 1 (EGFR) and 2 (HER2) tyrosine kinase in a 2-week on, 2-week off schedule in patients with advanced solid tumours
    F A L M Eskens
    Department of Medical Oncology, Erasmus University Medical Center, Rotterdam, The Netherlands
    Br J Cancer 98:80-5. 2008
    ..No partial or complete responses were observed, stable disease lasting more than four cycles was seen in seven patients. The recommended dose for studies with BIBW 2992 for 14 days followed by 14 days off medication is 70 mg OD...
  56. ncbi Expression of p95HER2, a truncated form of the HER2 receptor, and response to anti-HER2 therapies in breast cancer
    Maurizio Scaltriti
    Medical Oncology Program, Medical Oncology Department, Vall d Hebron University Hospital and Research Institute, Barcelona 08035, Spain
    J Natl Cancer Inst 99:628-38. 2007
    ....
  57. ncbi Prospective phase II study of gefitinib for chemotherapy-naive patients with advanced non-small-cell lung cancer with epidermal growth factor receptor gene mutations
    Akira Inoue
    Department of Respiratory Oncology and Molecular Medicine, Institute of Development, Aging, and Cancer, Tohoku University, 4 1, Seiryomachi, Aoba ku, Sendai 980 8575, Japan
    J Clin Oncol 24:3340-6. 2006
    ..This study was undertaken to investigate the efficacy and the feasibility of gefitinib for chemotherapy-naïve patients with advanced non-small-cell lung cancer (NSCLC) harboring epidermal growth factor receptor (EGFR) mutations...
  58. pmc PTEN loss contributes to erlotinib resistance in EGFR-mutant lung cancer by activation of Akt and EGFR
    Martin L Sos
    Max Planck Institute for Neurological Research with Klaus Joachim Zülch Laboratories of the Max Planck Society and the Medical Faculty of the University of Köln, Germany
    Cancer Res 69:3256-61. 2009
    ..These results suggest a novel resistance mechanism in EGFR-mutant NSCLC involving PTEN loss...
  59. ncbi Phase I trial of the irreversible EGFR and HER2 kinase inhibitor BIBW 2992 in patients with advanced solid tumors
    Timothy A Yap
    Drug Development Unit, The Royal Marsden National Health Service Foundation Trust, and the Institute of Cancer Research, Sutton, Surrey, United Kingdom
    J Clin Oncol 28:3965-72. 2010
    ..A phase I study of continuous once-daily oral BIBW 2992 was conducted to determine safety, maximum-tolerated dose, pharmacokinetics (PK), food effect, and preliminary antitumor efficacy...
  60. ncbi Novel D761Y and common secondary T790M mutations in epidermal growth factor receptor-mutant lung adenocarcinomas with acquired resistance to kinase inhibitors
    Marissa N Balak
    Human Oncology and Pathogenesis Program, Thoracic Oncology Service, Varmus Lab, Department of Pathology, Memorial Sloan Kettering Cancer Center, Weill Medical College of Cornell University, New York, New York 10021, USA
    Clin Cancer Res 12:6494-501. 2006
    ..We aimed to elucidate the frequency and nature of secondary EGFR mutations in patients with acquired resistance to TKI monotherapy...
  61. ncbi Effect of linagliptin monotherapy on glycaemic control and markers of β-cell function in patients with inadequately controlled type 2 diabetes: a randomized controlled trial
    S Del Prato
    Department of Endocrinology and Metabolism, Section of Metabolic Diseases, University of Pisa, Pisa, Italy
    Diabetes Obes Metab 13:258-67. 2011
    ....
  62. pmc Clinical definition of acquired resistance to epidermal growth factor receptor tyrosine kinase inhibitors in non-small-cell lung cancer
    David Jackman
    Vanderbilt Ingram Cancer Center, Vanderbilt University, Nashville, TN, USA
    J Clin Oncol 28:357-60. 2010
    ..These guidelines should minimize reporting of false-positive and false-negative activity in these clinical trials and would facilitate the identification of agents that truly overcome acquired resistance to gefitinib and erlotinib...
  63. pmc Erlotinib and bevacizumab in patients with recurrent or metastatic squamous-cell carcinoma of the head and neck: a phase I/II study
    Ezra E W Cohen
    Section of Hematology Oncology, Department of Medicine, University of Chicago, Chicago, IL, USA University of Chicago Cancer Research Center, Chicago, IL, USA
    Lancet Oncol 10:247-57. 2009
    ..In this multi-institutional phase I/II study we combined an EGFR inhibitor, erlotinib, with an anti-VEGF antibody, bevacizumab...
  64. ncbi Exon 19 deletion mutations of epidermal growth factor receptor are associated with prolonged survival in non-small cell lung cancer patients treated with gefitinib or erlotinib
    David M Jackman
    Lowe Center of Thoracic Oncology, Department of Medical Oncology, Dana Farber Cancer Institute, Boston, Massachusetts 02115, USA
    Clin Cancer Res 12:3908-14. 2006
    ..Our study explored the relationship between the two most common types of somatic EGFR mutations, exon 19 deletions and the L858R point mutation, and outcomes of patients following treatment with gefitinib or erlotinib...
  65. ncbi Novel mechanism of lapatinib resistance in HER2-positive breast tumor cells: activation of AXL
    Li Liu
    Department of Translational Research, GlaxoSmithKline, King of Prussia, Pennsylvania, USA
    Cancer Res 69:6871-8. 2009
    ....
  66. ncbi Analysis of epidermal growth factor receptor gene mutation in patients with non-small cell lung cancer and acquired resistance to gefitinib
    Takayuki Kosaka
    Department of Thoracic Surgery, Aichi Cancer Center Hospital, 1 1 Kanokoden, Chikusa ku, Nagoya 464 8681, Japan
    Clin Cancer Res 12:5764-9. 2006
    ..Part of this "acquired resistance" is attributable to a secondary mutation resulting in threonine to methionine at codon 790 (T790M) of EGFR...
  67. ncbi Mutations of the epidermal growth factor receptor gene predict prolonged survival after gefitinib treatment in patients with non-small-cell lung cancer with postoperative recurrence
    Tetsuya Mitsudomi
    Department of Thoracic Surgery, Aichi Cancer Center Hospital, 1 1 Kanokoden, Chikusa ku, Nagoya 464 8681, Japan
    J Clin Oncol 23:2513-20. 2005
    ..To evaluate the relationship between mutations of the epidermal growth factor receptor (EGFR) gene and the effectiveness of gefitinib treatment in patients with recurrent lung cancer after pulmonary resection...
  68. pmc Knockdown of oncogenic KRAS in non-small cell lung cancers suppresses tumor growth and sensitizes tumor cells to targeted therapy
    Noriaki Sunaga
    Hamon Center for Therapeutic Oncology Research, Simmons Cancer Center, Department of Pharmacology, University of Texas Southwestern Medical Center at Dallas, 5323 Harry Hines Blvd, Dallas, TX 75390, USA
    Mol Cancer Ther 10:336-46. 2011
    ..Our findings suggest that targeting oncogenic KRAS by itself will not be sufficient treatment, but may offer possibilities of combining anti-KRAS strategies with other targeted drugs...
  69. ncbi Phase III trial of bevacizumab in combination with gemcitabine and erlotinib in patients with metastatic pancreatic cancer
    Eric Van Cutsem
    University Hospital Gasthuisberg Leuven, Digestive Oncology Unit, Herestraat 49, B 3000 Leuven, Belgium
    J Clin Oncol 27:2231-7. 2009
    ..Phase II results for bevacizumab plus gemcitabine provided the rationale for a phase III trial of gemcitabine-erlotinib plus bevacizumab or placebo...
  70. ncbi Effect of renal impairment on the pharmacokinetics of the dipeptidyl peptidase-4 inhibitor linagliptin(*)
    U Graefe-Mody
    Boehringer Ingelheim Pharma GmbH and Co KG, Ingelheim, Germany
    Diabetes Obes Metab 13:939-46. 2011
    ....
  71. ncbi Chemogenomic profiling provides insights into the limited activity of irreversible EGFR Inhibitors in tumor cells expressing the T790M EGFR resistance mutation
    Martin L Sos
    Max Planck Institute for Neurological Research with Klaus Joachim Zülch Laboratories of the Max Planck Society, Center of Integrated Oncology and Department I of Internal Medicine, University of Koln, Cologne, Germany
    Cancer Res 70:868-74. 2010
    ....
  72. ncbi Efficacy and safety of initial combination therapy with linagliptin and pioglitazone in patients with inadequately controlled type 2 diabetes: a randomized, double-blind, placebo-controlled study
    R Gomis
    Endocrinology and Diabetes Service, IDIBAPS, CIBERDEM, Hospital Clinic Villarroel, Barcelona, Spain
    Diabetes Obes Metab 13:653-61. 2011
    ..5-11.0%)...
  73. ncbi Cediranib plus FOLFOX/CAPOX versus placebo plus FOLFOX/CAPOX in patients with previously untreated metastatic colorectal cancer: a randomized, double-blind, phase III study (HORIZON II)
    Paulo M Hoff
    FACP, Instituto do Câncer do Estado de São Paulo, Faculdade de Medicina da Universidade de Sao Paulo, Av Dr Arnaldo 251, Sao Paulo, Brazil
    J Clin Oncol 30:3596-603. 2012
    ....
  74. ncbi ZD1839 (Iressa): an orally active inhibitor of epidermal growth factor signaling with potential for cancer therapy
    Alan E Wakeling
    Department of Cancer and Infection Research, AstraZeneca Pharmaceuticals, Alderley Park, Macclesfield, Cheshire SK10 4TG, United Kingdom
    Cancer Res 62:5749-54. 2002
    ..These studies indicate the potential utility of ZD1839 in the treatment of many human tumors and indicate that continuous once-a-day p.o. dosing might be a suitable therapeutic regimen...
  75. ncbi Multi-institutional randomized phase II trial of gefitinib for previously treated patients with advanced non-small-cell lung cancer (The IDEAL 1 Trial) [corrected]
    Masahiro Fukuoka
    Fourth Department of Internal Medicine, Kinki University School of Medicine, 377 2 Ohnohigashi Osakasayama, Osaka 589, Japan
    J Clin Oncol 21:2237-46. 2003
    ....
  76. ncbi Dual-agent molecular targeting of the epidermal growth factor receptor (EGFR): combining anti-EGFR antibody with tyrosine kinase inhibitor
    Shyhmin Huang
    Department of Human Oncology, University of Wisconsin School of Medicine and Comprehensive Cancer Center, 600 Highland Avenue, Madison, WI 53792 0600, USA
    Cancer Res 64:5355-62. 2004
    ..This approach suggests potential new strategies to maximize effective target inhibition, which may improve the therapeutic ratio for anti-EGFR-targeted therapies in developing clinical trials...
  77. pmc Acquired resistance to EGFR tyrosine kinase inhibitors in cancer cells is mediated by loss of IGF-binding proteins
    Marta Guix
    Department of Medicine, Vanderbilt University School of Medicine, Nashville, Tennessee 37232 6307, USA
    J Clin Invest 118:2609-19. 2008
    ..Moreover, combined therapeutic inhibition of EGFR and IGFIR may abrogate this acquired mechanism of drug resistance and is thus worthy of prospective clinical investigation...
  78. pmc Loss of phosphatase and tensin homolog or phosphoinositol-3 kinase activation and response to trastuzumab or lapatinib in human epidermal growth factor receptor 2-overexpressing locally advanced breast cancers
    Bhuvanesh Dave
    Lester and Sue Smith Breast Center, Dan L Duncan Cancer Center, Baylor College of Medicine, Houston, TX, USA
    J Clin Oncol 29:166-73. 2011
    ..Understanding of the cellular response to HER2-targeted therapies is needed to tailor treatments and to identify patients less likely to benefit...
  79. ncbi Phase III trial of maintenance gefitinib or placebo after concurrent chemoradiotherapy and docetaxel consolidation in inoperable stage III non-small-cell lung cancer: SWOG S0023
    Karen Kelly
    University of Kansas Medical Center, Kansas City, KS 66160, USA
    J Clin Oncol 26:2450-6. 2008
    ..Early clinical studies with gefitinib showed promising efficacy and mild toxicity in patients with advanced non-small-cell lung cancer (NSCLC). Thus, gefitinib was an ideal agent to evaluate in a maintenance setting in stage III disease...
  80. pmc Targeting the epidermal growth factor receptor in non-small cell lung cancer cells: the effect of combining RNA interference with tyrosine kinase inhibitors or cetuximab
    Gang Chen
    Laboratory of Medical and Molecular Oncology and Department of Medical Oncology, Universitair Ziekenhuis Brussel, Vrije Universiteit Brussel, Laarbeeklaan 101, 1090, Brussels, Belgium
    BMC Med 10:28. 2012
    ....
  81. ncbi Efficacy of gefitinib, an inhibitor of the epidermal growth factor receptor tyrosine kinase, in symptomatic patients with non-small cell lung cancer: a randomized trial
    Mark G Kris
    Thoracic Oncology Service, Division of Solid Tumor Oncology, Department of Medicine, Memorial Sloan Kettering Cancer Center and the Weill Medical College of Cornell University, New York, NY 10021, USA
    JAMA 290:2149-58. 2003
    ....
  82. ncbi Phase I/II trial of cetuximab and erlotinib in patients with lung adenocarcinoma and acquired resistance to erlotinib
    Yelena Y Janjigian
    Gastrointestinal and Thoracic Oncology Services, Division of Solid Tumor Oncology, Department of Medicine and Radiology, Memorial Sloan Kettering Cancer Center, Weill Medical College of Cornell University, New York, New York 10065, USA
    Clin Cancer Res 17:2521-7. 2011
    ..To evaluate the toxicity and efficacy of cetuximab and erlotinib in patients with acquired resistance to erlotinib, we conducted this phase I/II clinical trial...
  83. pmc BIM mediates EGFR tyrosine kinase inhibitor-induced apoptosis in lung cancers with oncogenic EGFR mutations
    Daniel B Costa
    Division of Hematology Oncology, Beth Israel Deaconess Medical Center, Harvard Medical School, Boston, Massachusetts, USA
    PLoS Med 4:1669-79; discussion 1680. 2007
    ..The objective of this study was to identify the mechanism of EGFR TKI-induced apoptosis and secondary resistant mutations that affect this process...
  84. ncbi Phase III study of gefitinib compared with intravenous methotrexate for recurrent squamous cell carcinoma of the head and neck [corrected]
    J Simon W Stewart
    Charing Cross Hospital, London, UK
    J Clin Oncol 27:1864-71. 2009
    ..To compare survival in patients with recurrent or metastatic squamous cell carcinoma of the head and neck (SCCHN) treated with gefitinib 250 or 500 mg/day or standard methotrexate...
  85. pmc Vandetanib plus docetaxel versus docetaxel as second-line treatment for patients with advanced non-small-cell lung cancer (ZODIAC): a double-blind, randomised, phase 3 trial
    Roy S Herbst
    Department of Thoracic Head and Neck Medical Oncology, University of Texas MD Anderson Cancer Center, 1515 Holcombe Boulevard, Unit 432, Houston, TX 77030 4009, USA
    Lancet Oncol 11:619-26. 2010
    ..These results supported investigation of the combination in this larger, definitive phase 3 trial (ZODIAC)...
  86. pmc Phosphatidylinositol 3-kinase hyperactivation results in lapatinib resistance that is reversed by the mTOR/phosphatidylinositol 3-kinase inhibitor NVP-BEZ235
    Pieter J A Eichhorn
    Medical Oncology Program, Vall d Hebron Institut de Oncologia, Barcelona, Spain
    Cancer Res 68:9221-30. 2008
    ..Our data show that deregulation of the PI3K pathway, either through loss-of-function mutations in PTEN or dominant activating mutations in PIK3CA, leads to lapatinib resistance, which can be effectively reversed by NVP-BEZ235...
  87. ncbi 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
    Howard A Burris
    The Sarah Cannon Research Institute, 250 25th Avenue N, Suite 110, Nashville, TN 37203, USA
    J Clin Oncol 23:5305-13. 2005
    ....
  88. pmc Lapatinib plus capecitabine in women with HER-2-positive advanced breast cancer: final survival analysis of a phase III randomized trial
    David Cameron
    University of Leeds, Leeds, UK
    Oncologist 15:924-34. 2010
    ..Here, we report final analyses of overall survival...
  89. pmc Acquired resistance to epidermal growth factor receptor kinase inhibitors associated with a novel T854A mutation in a patient with EGFR-mutant lung adenocarcinoma
    James Bean
    Human Oncology and Pathogenesis Program, Memorial Sloan Kettering Cancer Center, New York, NY 10021, USA
    Clin Cancer Res 14:7519-25. 2008
    ..We aimed to identify additional second-site alterations associated with acquired resistance...
  90. pmc Predictors of survival in patients with bone metastasis of lung cancer
    Hideshi Sugiura
    Department of Orthopaedic Surgery, Aichi Cancer Center, 1 1 Kanokoden, Chikusa ku, Nagoya, Japan
    Clin Orthop Relat Res 466:729-36. 2008
    ..The data preliminarily suggest treatment with an epithelial growth factor receptor inhibitor may improve survival after bone metastasis...
  91. ncbi Intermittent erlotinib in combination with pemetrexed: phase I schedules designed to achieve pharmacodynamic separation
    Angela M Davies
    University of California Davis Cancer Center, Sacramento, California, USA
    J Thorac Oncol 4:862-8. 2009
    ..Pharmacodynamic separation by intermittent delivery of epidermal growth factor receptor tyrosine kinase inhibitors with chemotherapy may increase efficacy by overcoming hypothesized antagonism...
  92. ncbi Chemotherapy-induced epidermal growth factor receptor activation determines response to combined gefitinib/chemotherapy treatment in non-small cell lung cancer cells
    Sandra Van Schaeybroeck
    Department of Oncology, Centre for Cancer Research and Cell Biology, Queen s University Belfast, University Floor, Belfast City Hospital, Lisburn Road, Belfast BT9 7AB, Northern Ireland, United Kingdom
    Mol Cancer Ther 5:1154-65. 2006
    ..These novel findings suggest that modulation of EGFR activity following drug treatment determines response to gefitinib in combination with chemotherapy in NSCLC cells...
  93. ncbi Epidermal growth factor receptor mutations and their correlation with gefitinib therapy in patients with non-small cell lung cancer: a meta-analysis based on updated individual patient data from six medical centers in mainland China
    Yi long Wu
    Lung Cancer Research Institute and Cancer Center, Guangdong Provincial People s Hospital, Guangzhou, China
    J Thorac Oncol 2:430-9. 2007
    ..We investigated the relevance of demographic characteristics and EGFR mutations, correlations between the efficacy of gefitinib and EGFR mutations in NSCLC, and to identify individuals who would likely benefit from gefitinib...
  94. ncbi Gefitinib and the modulation of the signaling pathways downstream of epidermal growth factor receptor in human liver cancer cells
    Jun Ichi Okano
    Second Department of Internal Medicine, Tottori University School of Medicine, 36 1 Nishi cho, Yonago 683 8504, Japan
    J Gastroenterol 41:166-76. 2006
    ..We examined whether abrogation of the TGF-alpha/EGFR signaling pathway with a selective EGFR tyrosine kinase inhibitor, gefitinib, could inhibit the proliferation of human hepatocellular carcinoma (HCC) cells...
  95. ncbi Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer
    Xiong Cai
    Curis Inc, 45 Moulton Street, Cambridge, Massachusetts 02138, USA
    J Med Chem 53:2000-9. 2010
    ....
  96. ncbi Phase I clinical study of AZD2171, an oral vascular endothelial growth factor signaling inhibitor, in patients with advanced solid tumors
    Joachim Drevs
    Tumor Biology Center, MR Development and Application Center, Albert Ludwigs University, Freiburg, Germany
    J Clin Oncol 25:3045-54. 2007
    ..This phase I study was designed to evaluate the safety and tolerability of increasing doses of AZD2171, with additional assessments of pharmacokinetics, pharmacodynamics, and efficacy...
  97. ncbi Predictive factors for interstitial lung disease, antitumor response, and survival in non-small-cell lung cancer patients treated with gefitinib
    Masahiko Ando
    Department of Preventive Services, Kyoto University School of Public Health, Kyoto, Japan
    J Clin Oncol 24:2549-56. 2006
    ..We examined the prevalence of and risk factors for gefitinib-induced ILD associated with practical use of the drug in Japanese with non-small-cell lung cancer (NSCLC)...
  98. pmc A "vascular normalization index" as potential mechanistic biomarker to predict survival after a single dose of cediranib in recurrent glioblastoma patients
    A Gregory Sorensen
    A A Martinos Center for Biomedical Imaging, Massachusetts General Hospital, Boston, MA 02114, USA
    Cancer Res 69:5296-300. 2009
    ..54; P = 0.004) and progression-free survival (rho = 0.6; P = 0.001). The vascular normalization index described here should be validated in randomized clinical trials...
  99. ncbi Interstitial lung disease in Japanese patients with lung cancer: a cohort and nested case-control study
    Shoji Kudoh
    Nippon Medical School, Tokyo, Japan
    Am J Respir Crit Care Med 177:1348-57. 2008
    ..Interstitial lung disease (ILD) occurs in Japanese patients with non-small cell lung cancer (NSCLC) receiving gefitinib...
  100. ncbi Erlotinib induces cell cycle arrest and apoptosis in hepatocellular cancer cells and enhances chemosensitivity towards cytostatics
    Alexander Huether
    Gastroenterology Infectious Diseases Rheumatology, Medical Clinic I, Charite Universitatsmedizin Berlin, Campus Benjamin Franklin, Hindenburgdamm 30, 12200, Berlin, Germany
    J Hepatol 43:661-9. 2005
    ..Several reports indicate that EGFRs are expressed frequently in HCC, most likely contributing to the aggressive growth characteristics of these tumors...
  101. ncbi Gefitinib and chemotherapy combination studies in five novel human non small cell lung cancer xenografts. Evidence linking EGFR signaling to gefitinib antitumor response
    Jean Gabriel Judde
    Institut Curie, Section de Recherche, Paris, France
    Int J Cancer 120:1579-90. 2007
    ..The data indicate that the antitumor activity of gefitinib in NSCLC, alone or in combination with chemotherapy, is tumor-dependent and is influenced by downstream signaling events independent of EGFR status...

Research Grants74

  1. Antileishmanial Lead Optimization of Quinazolines
    Karl A Werbovetz; Fiscal Year: 2013
    ..Pharmacokinetics and tissue distribution of the most promising 2,4-diaminoquinazolines will be determined in mice to verify plasma and target organ exposure. ..
  2. DEVELOPMENT OF CANCER IMAGING AGENTS
    Henry VanBrocklin; Fiscal Year: 2000
    ..Specificity will be determined by testing the quinazolines ability to inhibit erbB-2 and erbB-3 tyrosine kinase activity...
  3. MOLECULAR AND ELECTRONIC STRUCTURES OF ANTIFOLATE DRUGS
    Vivian Cody; Fiscal Year: 1991
    ..members from four antifolate classes (lipophilic diaminopyrimidines, soluble diamino s-triazines, lipophilic quinazolines, and side chain modified antifolate pteridines), (2) description of their molecular and electronic properties ..
  4. INNOVATIVE TUMOR TARGETED THERAPIES FOR LUNG CANCER
    Roman Perez Soler; Fiscal Year: 2004
    ..Four such candidates have already been identified. It is anticipated that a total of ten young clinical investigators will be mentored during a five-year period. ..
  5. CATIONIC LIPID/P53 GENE THERAPY IN LUNG CANCER PATIENTS
    Roman Perez Soler; Fiscal Year: 2003
    ..The results of this study will provide initial but very valuable information on the potential use of this new strategy in the treatment of bronchial premalignancy, carcinoma in situ, and endobronchial lung tumors. ..
  6. RADIATION AND DRUG EFFECTS ON TUMOR CELL SUBPOPULATIONS
    Dietmar Siemann; Fiscal Year: 2001
    ..Ultimately we hope that these approaches can be reliably developed to an extent where the use of human tumor biopsy material may lead to radiotherapy treatments more tailored to the individual patient. ..
  7. Antiestrogenic Effects on Tumor Angiogenesis
    Kimberly Blackwell; Fiscal Year: 2006
    ..The results of this project will have profound implications, especially as clinicians begin to use the newer estrogen receptor modulating drugs for the prevention and treatment of breast cancer. ..
  8. Creatine: Is It a Body Builder for Cancer Patients?
    Aminah Jatoi; Fiscal Year: 2004
    ..obtain longitudinal toxicity and quality of life data on this same cohort of 50 patients and will make direct comparisons between treatment arms on toxicity incidence and severity and on maximal quality of life scores ..
  9. Mechanisms and Therapeutics in Cancer Anorexia/Cachexia
    Aminah Jatoi; Fiscal Year: 2004
    ..This K23 grant application will serve as a springboard to allow her to delve into the pathophysiology of this syndrome and to develop into an independent clinical investigator. ..
  10. Neuropeptide Y for Cancer-Associated Anorexia
    Aminah Jatoi; Fiscal Year: 2003
    ..These two pilot studies will allow us to lay the groundwork for such larger trials. Our ultimate goal is to help cancer patients who suffer from anorexia. ..
  11. PEDIATRIC BRAIN TUMOR CLINICAL TRIAL CONSORTIUM
    Michael Prados; Fiscal Year: 2003
    ..The aim of these treatment approaches is to increase disease-free and overall survival in children with brain tumors. ..
  12. NABTC CENTRAL OPERATION GRANT (UCSF PROJECT LEADER)
    Michael Prados; Fiscal Year: 2008
    ..The NABTC will treat patients using novel therapeutic agents with the ultimate goal to increase quality, and hopefully, overall survival in this patient population. ..
  13. TGF-Beta Signaling Pathways in Prostate Tumorigenesis
    Natasha Kyprianou; Fiscal Year: 2005
    ..abstract_text> ..
  14. Rapamycin as an Antineoplastic Agent
    Ezra Cohen; Fiscal Year: 2006
    ..At the conclusion of the trial RAPA toxicity and effect on p-S6K will be defined over a range of doses as well as the MTD for use in future studies that will develop this agent. ..
  15. Anoikis Effect by Quinazolines on Prostate Growth
    Natasha Kyprianou; Fiscal Year: 2008
    ..Specific Aim 3 will establish that the quinazolines, doxazosin and terazosin, suppress prostate vasculature and inhibit tissue angiogenesis in patients after a1 ..
  16. Predictive Markers of Glioblastoma Response to VEGF Trap
    John de Groot; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable]..
  17. 7T Translational MRI System
    ALMA SORENSEN; Fiscal Year: 2007
    ..We list 24 funded projects in support of this additional instrumentation. [unreadable] [unreadable] [unreadable]..
  18. Functional Infrared Imaging Predicts Radiation Mucositis
    Ezra Cohen; Fiscal Year: 2008
    ..Such a tool would have wide applicability in this patient population and would have tremendous impact on their treatment. [unreadable] [unreadable] [unreadable]..
  19. High Resolution PET Camera for Brain Imaging
    ALMA SORENSEN; Fiscal Year: 2006
    ..Placement of the HRRT in the proposed environment will provide a unique facility to advance brain imaging research that in turn will provide insights for a variety of illnesses and biomedical questions. [unreadable] [unreadable]..
  20. Development of Natural Product as Antimalarial Agent
    Shuren Zhu; Fiscal Year: 2007
    ..Investigational new drug (IND) application will then be filed with FDA. [unreadable] [unreadable] [unreadable]..
  21. Silicon Graphics Prism Extreme 128P/1TB
    ALMA SORENSEN; Fiscal Year: 2006
    ..unreadable] [unreadable] [unreadable]..
  22. Imaging Archive for Magnetic Resonance Imaging Systems
    ALMA SORENSEN; Fiscal Year: 2005
    ..Overall, this needed resource will greatly facilitate many NIH-funded investigators and investigations for years to come. ..
  23. CEA BASED VACCINE THERAPY IN PATIENTS WITH ADVANCED CA
    John Marshall; Fiscal Year: 2005
    ..So far, the applicant's experience with the first generation CEA-based vaccines has generated a great deal of excitement, and yet he anticipates even more from the newer vaccine constructs. ..
  24. Sharing canonical human stroke data
    Ona Wu; Fiscal Year: 2010
    ..Linking our existing portals with BIRN resources has the potential to greatly facilitate data sharing which will benefit the understanding of stroke and speed discovery of new therapeutic interventions. ..
  25. Symposium:Men's Health Issues in Basic Urologic Research
    Natasha Kyprianou; Fiscal Year: 2002
    ..Funding is requested to partially defray the travel and lodging costs fore the invited speakers and to partially cover the costs of travel awards to young investigators. ..
  26. A 3.0 Tesla MRI System in a Neuroscience ICU
    ALMA SORENSEN; Fiscal Year: 2004
    ..Since these subjects are difficult to bring to the instrumentation, we seek to gain these insights by bringing the instrumentation to them. The proposed instrument will bring state-of-the-art performance to a unique setting. ..
  27. Pre-Clinical Development of Natural Product Analogues as Antimalarial Agents
    Shuren Zhu; Fiscal Year: 2007
    ..Investigational new drug (IND) application will then be filed with FDA. Radix Pharmaceuticals has strategic alliance with commercial partners for Phase III development. [unreadable] [unreadable] [unreadable]..
  28. Imaging Biomarkers for Cancer Drug Development
    ALMA SORENSEN; Fiscal Year: 2004
    ..The planning grant revolves around three aims: to confer a multidisciplinary partnership to work towards this goal; to select a set of demonstration projects, and to develop an operating plan for the partnership. ..
  29. MRI DIFFUSION/PERFUSION MISMATCH IN HUMAN ACUTE STROKE
    ALMA SORENSEN; Fiscal Year: 2008
    ..unreadable] [unreadable]..
  30. First International Inflammatory Breast Cancer Conference
    Massimo Cristofanilli; Fiscal Year: 2008
    ..For project details please see "Conference Plan". [unreadable] [unreadable] [unreadable]..
  31. TGF BETA RECEPTOR DYNAMICS
    Edward Leof; Fiscal Year: 2008
    ..Answers to these questions are critical if the processes mediating the various cellular phenotypes induced by TGF-beta are to be elucidated. ..
  32. Molecular Epidemiology of Esophageal Cancer Prognosis
    Geoffrey Liu; Fiscal Year: 2008
    ..Furthermore, the proposed studies address directly a prioritized research area identified by the NCI Stomach and Esophageal Cancers Progress Review Group (Year 2002). ..
  33. Dose and Treatment Selection in Clinical Trials
    Ying Kuen Cheung; Fiscal Year: 2010
    ....
  34. Engineering new RNA-binding proteins by selection and design
    Gabriele Varani; Fiscal Year: 2010
    ..abstract_text> ..
  35. Molecular Basis Of Renal Cell Carcinoma Response to SU11428
    Robert J Motzer; Fiscal Year: 2011
    ..These tumor and cell line-based studies lay a foundation for further molecular studies aimed at understanding the sensitivity/resistance of RCC to SU11248. ..
  36. Combinatorial Chemistry and Cancer Target
    Peter Vogt; Fiscal Year: 2008
    ..The collaborating groups of this Program Project have become an integrated unit that incorporates a wide range of expertise and interests and applies them to the common goal, new anticancer compounds. ..
  37. Role of ErbB/Stat3 in the establishment and progression of pancreatic cancer
    James Freeman; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable]..
  38. Deciphering synergistic combinatorial targets in glioma
    W K Alfred Yung; Fiscal Year: 2010
    ....
  39. CGRP Regulation of iNOS and MAP Kinases/Phosphatases in Trigeminal Ganglia Glia
    Paul L Durham; Fiscal Year: 2010
    ....
  40. Controlling the Max Network
    Peter Vogt; Fiscal Year: 2008
    ..The proposed work on stabilizers in the Myc-Max network could open the door to a new way of influencing and directing cell growth. ..
  41. Biochemical markers of bone turnover in metastatic prostate cancer
    Primo N Lara; Fiscal Year: 2010
    ....
  42. Determinants of Resistance to Erlotinib in NSCLC
    Roman Perez Soler; Fiscal Year: 2010
    ..To confirm the predictive value of the algorithm in a group of patients with chemoresistant NSCLC selected for their high probability of achieving a response or stable disease with single agent erlotinib therapy. ..
  43. Defining Molecular Markers for Tumor Hypoxia
    QUYNH THU XUAN LE; Fiscal Year: 2010
    ..abstract_text> ..
  44. Signal Transduction Pathways in Glioblastoma
    Arnab Chakravarti; Fiscal Year: 2009
    ....
  45. Resistance and Response Mechanisms to Prostate Cancer Therapy
    TOMASZ BEER; Fiscal Year: 2009
    ..We will test the effectiveness of novel treatments that exploit newly discovered targets in the laboratory and lay the foundation for human trials to develop effective prostate cancer treatment. ..
  46. Antitumor Antimitotics That Reverse Tumor Resistance
    Aleem Gangjee; Fiscal Year: 2010
    ..The study will also further define the mechanism of action of the novel series and could afford agents for clinical use. ..
  47. Immunotherapy with peptide MHC tetramer isolated T cells
    Herbert Lyerly; Fiscal Year: 2005
    ..It is anticipated that these studies would provide an important proof of principle for this general concept which would have wide application for antigen specific adoptive immunotherapy of vial disorders and cancer. ..
  48. PHASE I TRIAL OF A PEPTIDE VACCINE AGAINST EGFRVIII
    Bruce Montgomery; Fiscal Year: 2005
    ..To characterize effects of human anti-EGFRvIII antibodies on EGFRvIII signaling. 4. To determine the level of EGFR specific T cell response after immunization with EGFRvIII peptide. ..
  49. Chemotherapy and anti-EGFR Antibody C225 in Lung Cancer
    Roman Perez Soler; Fiscal Year: 2004
    ..abstract_text> ..
  50. DENDRITIC CELL MOBILIZATION AND ACTIVE IMMUNOTHERAPY
    Herbert Lyerly; Fiscal Year: 2005
    ....
  51. TRIPTYCENE ANALOGS--NOVEL BIFUNCTIONAL ANTICANCER DRUGS
    Jean Pierre Perchellet; Fiscal Year: 2004
    ..abstract_text> ..
  52. Correlation of EGFR Mutations and Response to Gefitinib
    Naiyer Rizvi; Fiscal Year: 2006
    ..Further characterization of tumors harboring these mutations, may have significant therapeutic implications for patients with NSCLC and change the paradigm whereby we treat patients with NSCLC. ..
  53. Venous thromboembolism among California cancer patients
    Helen Chew; Fiscal Year: 2003
    ..abstract_text> ..
  54. Oregon Prostate Cancer Conference 2001
    TOMASZ BEER; Fiscal Year: 2003
    ....
  55. Regulation of CSF-1 in Ovarian Cancer
    SETSUKO CHAMBERS; Fiscal Year: 2006
    ..Moreover, the results of these studies will provide the scientific basis for a future trial of anti-androgen therapy as a chemopreventative agent in patients at high risk for the development of ovarian cancer. ..
  56. Phase II Study of 44Gy from 131I-81C6 for CNS Tumors
    David Reardon; Fiscal Year: 2004
    ..To further define the toxicity of this approach and Specific Aim 3.To determine the impact of this therapy on quality of life. ..
  57. Hypoxia-induced Proteins as Lung Cancer Biomarkers
    Philip Mack; Fiscal Year: 2006
    ..abstract_text> ..
  58. Minimally Invasive Surgical Therapies Treatment Consort*
    Claus Roehrborn; Fiscal Year: 2005
    ..The MIST Study Group will be a blueprint for a technology assessment group applicable to other areas of urology and other medical or surgical subspecialties. ..
  59. Long-Circulating Liposomal Camptothecins CAP and EAP
    Roman Perez Soler; Fiscal Year: 2003
    ..Ultimately, we will seek formulation(s) that display optimized drug retention and in vivo and in vitro performance. PROPOSED COMMERCIAL APPLICATION: Not Available ..
  60. Structure of ribonucleoprotein: telomerase
    Gabriele Varani; Fiscal Year: 2007
    ..The design and execution of new biochemical and functional experiments, grounded onto the structural results, that will address the biological function of these protein-RNA complexes. ..
  61. Direct Cellular Effects of Blood Coagulation Proteases
    LAURENT MOSNIER; Fiscal Year: 2007
    ..End of Abstract) [unreadable] [unreadable] [unreadable] [unreadable] [unreadable]..
  62. Activation of NF-kB by Human Papillomaviruses
    CRAIG WOODWORTH; Fiscal Year: 2006
    ..Therefore, our results will provide basic information on how HPV might alter host response to infection. [unreadable] [unreadable]..
  63. Cytomation MoFlo High Performance Flow Cytometer
    Herbert Lyerly; Fiscal Year: 2002
    ..Advisory committees, institutional support, financial support for continued maintenance and management plans are in place to insure that the instrument will be fully and appropriately utilized. ..
  64. Nitric Oxide Control of CGRP in Trigeminal Neurons
    Paul Durham; Fiscal Year: 2002
    ..abstract_text> ..
  65. COLUMBIA UNIVERSITY SOUTHWEST ONCOLOGY GROUP PROGRAM
    Daniel Petrylak; Fiscal Year: 2003
    ..Based on substantial laboratory strength, we intend to integrate Columbia laboratory resources as core support for SWOG clinical studies. ..
  66. Functional Genomics Tools for HER2 heterodimers and Androgen Receptor Signaling
    Anjali Jain; Fiscal Year: 2007
    ..Androgen receptor is one such protein. Our research proposes to develop methods to search for compounds that specifically block the androgen receptor in prostate cancer cells. [unreadable]..
  67. CGRP CONTROL IN TRIGEMINAL NEURONS IN VITRO AND IN VIVO
    Paul Durham; Fiscal Year: 2006
    ..abstract_text> ..
  68. A Phase 2 study of AZD2171 in Recurrent Glioblastoma
    Tracy Batchelor; Fiscal Year: 2006
    ..unreadable] [unreadable]..
  69. Clinical Trial Development in Chronic Pelvic Pain Syndr*
    Daniel Shoskes; Fiscal Year: 2007
    ..As an example of a potential clinical trial, a study of water induced thermotherapy is outlined. ..
  70. NABTT-New Approaches to Brain Tumor Therapy (CNSC)
    Tracy Batchelor; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable]..
  71. Antitumor Mechanisms of SRC Inhibitors in Lung Cancer
    Eric Haura; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable]..
  72. A Phase 2 Trial of Dasatinib in Patients with NSCLC and Acquired Resistance to Er
    Vincent Miller; Fiscal Year: 2008
    ..The proposed work is a clinical trial to determine whether dasatinib is an effective treatment for patients with NSCLC and acquired resistance to erlotinib or gefitinib. [unreadable] [unreadable] [unreadable]..
  73. Molecular Determinants of Acquired Erlotinib Resistance
    Vincent Miller; Fiscal Year: 2006
    ..abstract_text> ..