J G Christensen

Summary

Affiliation: Pfizer Global Research and Development
Country: USA

Publications

  1. ncbi request reprint 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
    Dirk B Mendel
    Preclinical Research and Exploratory Development, SUGEN, Inc, South San Francisco, California 94080, USA
    Clin Cancer Res 9:327-37. 2003
  2. ncbi request reprint An orally available small-molecule inhibitor of c-Met, PF-2341066, exhibits cytoreductive antitumor efficacy through antiproliferative and antiangiogenic mechanisms
    Helen Y Zou
    Departments of Cancer Biology, Pfizer Global Research and Development, La Jolla Laboratories, La Jolla, California 92121, USA
    Cancer Res 67:4408-17. 2007
  3. ncbi request reprint A preclinical review of sunitinib, a multitargeted receptor tyrosine kinase inhibitor with anti-angiogenic and antitumour activities
    J G Christensen
    Pfizer Global Research and Development, 10724 Science Center Drive, San Diego, CA 92121, USA
    Ann Oncol 18:x3-10. 2007
  4. doi request reprint Pharmacokinetic-pharmacodynamic modeling of biomarker response and tumor growth inhibition to an orally available cMet kinase inhibitor in human tumor xenograft mouse models
    Shinji Yamazaki
    Pharmacokinetics, Dynamics and Metabolism, La Jolla Laboratories, Pfizer Global Research and Development, 10777 Science Center Dr, San Diego, CA 92121, USA
    Drug Metab Dispos 36:1267-74. 2008
  5. pmc PHA665752, a small-molecule inhibitor of c-Met, inhibits hepatocyte growth factor-stimulated migration and proliferation of c-Met-positive neuroblastoma cells
    Hal E Crosswell
    Division of Pediatric Hematology Oncology, Children s Hospital and University Medical Group of the Greenville Hospital System, Greenville, SC 29605, USA
    BMC Cancer 9:411. 2009
  6. pmc Efficacy of c-Met inhibitor for advanced prostate cancer
    William H Tu
    Department of Urology, Stanford University School of Medicine, Stanford, CA 94305 5328, USA
    BMC Cancer 10:556. 2010
  7. doi request reprint Beyond VEGF: targeting tumor growth and angiogenesis via alternative mechanisms
    James Christensen
    Department of Cancer Biology, Pfizer Global Research and Development, La Jolla Laboratories, La Jolla, CA 92121, USA
    Adv Exp Med Biol 610:43-53. 2008
  8. ncbi request reprint Cytoreductive antitumor activity of PF-2341066, a novel inhibitor of anaplastic lymphoma kinase and c-Met, in experimental models of anaplastic large-cell lymphoma
    James G Christensen
    Department of Cancer Biology, Pfizer Global Research and Development, La Jolla Laboratories, 10724 Science Center Drive, La Jolla, CA 92121, USA
    Mol Cancer Ther 6:3314-22. 2007
  9. ncbi request reprint Plasma vascular endothelial growth factor and interleukin-8 as biomarkers of antitumor efficacy of a prototypical erbB family tyrosine kinase inhibitor
    James G Christensen
    Pfizer Global Research and Development, La Jolla Labs, CA 92121, USA
    Mol Cancer Ther 4:938-47. 2005
  10. ncbi request reprint c-Met as a target for human cancer and characterization of inhibitors for therapeutic intervention
    James G Christensen
    Research Pharmacology, Pfizer Inc, La Jolla, CA 92121, USA
    Cancer Lett 225:1-26. 2005

Collaborators

Detail Information

Publications28

  1. ncbi request reprint 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
    Dirk B Mendel
    Preclinical Research and Exploratory Development, SUGEN, Inc, South San Francisco, California 94080, USA
    Clin Cancer Res 9:327-37. 2003
    ..The pharmacokinetic/pharmacodynamic relationship established for SU11248 in these preclinical studies has aided in the design, selection, and evaluation of dosing regimens being tested in human trials...
  2. ncbi request reprint An orally available small-molecule inhibitor of c-Met, PF-2341066, exhibits cytoreductive antitumor efficacy through antiproliferative and antiangiogenic mechanisms
    Helen Y Zou
    Departments of Cancer Biology, Pfizer Global Research and Development, La Jolla Laboratories, La Jolla, California 92121, USA
    Cancer Res 67:4408-17. 2007
    ..Collectively, these results show the therapeutic potential of targeting c-Met with selective small-molecule inhibitors for the treatment of human cancers...
  3. ncbi request reprint A preclinical review of sunitinib, a multitargeted receptor tyrosine kinase inhibitor with anti-angiogenic and antitumour activities
    J G Christensen
    Pfizer Global Research and Development, 10724 Science Center Drive, San Diego, CA 92121, USA
    Ann Oncol 18:x3-10. 2007
    ..It also highlights the importance of the multiple pathways that may be involved in cancer progression and the importance of these pathways in selected malignancies...
  4. doi request reprint Pharmacokinetic-pharmacodynamic modeling of biomarker response and tumor growth inhibition to an orally available cMet kinase inhibitor in human tumor xenograft mouse models
    Shinji Yamazaki
    Pharmacokinetics, Dynamics and Metabolism, La Jolla Laboratories, Pfizer Global Research and Development, 10777 Science Center Dr, San Diego, CA 92121, USA
    Drug Metab Dispos 36:1267-74. 2008
    ..The present results will be helpful in determining the appropriate dosing regimen and in guiding dose escalation to rapidly achieve efficacious systemic exposure in the clinic...
  5. pmc PHA665752, a small-molecule inhibitor of c-Met, inhibits hepatocyte growth factor-stimulated migration and proliferation of c-Met-positive neuroblastoma cells
    Hal E Crosswell
    Division of Pediatric Hematology Oncology, Children s Hospital and University Medical Group of the Greenville Hospital System, Greenville, SC 29605, USA
    BMC Cancer 9:411. 2009
    ..The effect of the tumor suppressor protein PTEN on migration and proliferation of tumor cells treated with PHA665752 was also evaluated...
  6. pmc Efficacy of c-Met inhibitor for advanced prostate cancer
    William H Tu
    Department of Urology, Stanford University School of Medicine, Stanford, CA 94305 5328, USA
    BMC Cancer 10:556. 2010
    ..Therefore, we directly assessed the efficacy of c-Met inhibition during androgen ablation on the growth and progression of prostate cancer...
  7. doi request reprint Beyond VEGF: targeting tumor growth and angiogenesis via alternative mechanisms
    James Christensen
    Department of Cancer Biology, Pfizer Global Research and Development, La Jolla Laboratories, La Jolla, CA 92121, USA
    Adv Exp Med Biol 610:43-53. 2008
  8. ncbi request reprint Cytoreductive antitumor activity of PF-2341066, a novel inhibitor of anaplastic lymphoma kinase and c-Met, in experimental models of anaplastic large-cell lymphoma
    James G Christensen
    Department of Cancer Biology, Pfizer Global Research and Development, La Jolla Laboratories, 10724 Science Center Drive, La Jolla, CA 92121, USA
    Mol Cancer Ther 6:3314-22. 2007
    ..Collectively, these data illustrate the potential clinical utility of inhibitors of NPM-ALK in treatment of patients with ALK-positive ALCL...
  9. ncbi request reprint Plasma vascular endothelial growth factor and interleukin-8 as biomarkers of antitumor efficacy of a prototypical erbB family tyrosine kinase inhibitor
    James G Christensen
    Pfizer Global Research and Development, La Jolla Labs, CA 92121, USA
    Mol Cancer Ther 4:938-47. 2005
    ....
  10. ncbi request reprint c-Met as a target for human cancer and characterization of inhibitors for therapeutic intervention
    James G Christensen
    Research Pharmacology, Pfizer Inc, La Jolla, CA 92121, USA
    Cancer Lett 225:1-26. 2005
    ..This review will address the potential for development of c-Met inhibitors for treatment of human cancers with particular emphasis on recent findings with small-molecule inhibitors...
  11. ncbi request reprint A selective small molecule inhibitor of c-Met kinase inhibits c-Met-dependent phenotypes in vitro and exhibits cytoreductive antitumor activity in vivo
    James G Christensen
    Preclinical Research and Exploratory Development, SUGEN, Inc, South San Francisco, CA 94080, USA
    Cancer Res 63:7345-55. 2003
    ..Collectively, these results demonstrate the feasibility of selectively targeting c-Met with ATP-competitive small-molecules and suggest the therapeutic potential of targeting c-Met in human cancers...
  12. doi request reprint PF-03732010: a fully human monoclonal antibody against P-cadherin with antitumor and antimetastatic activity
    Cathy C Zhang
    Translational Research Group in Oncology Research Unit, Pfizer Global Research and Development, La Jolla Laboratories, San Diego, California 92121, USA
    Clin Cancer Res 16:5177-88. 2010
    ..We characterized the biological properties of PF-03732010, a human monoclonal antibody against P-cadherin, in cell-based assays and tumor models...
  13. pmc Small-molecule p21-activated kinase inhibitor PF-3758309 is a potent inhibitor of oncogenic signaling and tumor growth
    Brion W Murray
    Pfizer Oncology, Pfizer, San Diego, CA 92121, USA
    Proc Natl Acad Sci U S A 107:9446-51. 2010
    ....
  14. doi request reprint PF-00477736 mediates checkpoint kinase 1 signaling pathway and potentiates docetaxel-induced efficacy in xenografts
    Cathy Zhang
    Oncology Research Unit, Pfizer Global Research and Development, La Jolla Laboratories, San Diego, California, USA
    Clin Cancer Res 15:4630-40. 2009
    ..Specifically, we investigated the correlation between PF-00477736-mediated modulation of biomarkers and the sensitization of docetaxel efficacy...
  15. ncbi request reprint High levels of HER-2 expression alter the ability of epidermal growth factor receptor (EGFR) family tyrosine kinase inhibitors to inhibit EGFR phosphorylation in vivo
    J G Christensen
    SUGEN, Inc, 230 East Grand Avenue, South San Francisco, CA 94080, USA
    Clin Cancer Res 7:4230-8. 2001
    ..The potential clinical implications of this observation are discussed...
  16. doi request reprint Enzymatic characterization of c-Met receptor tyrosine kinase oncogenic mutants and kinetic studies with aminopyridine and triazolopyrazine inhibitors
    Sergei L Timofeevski
    Pfizer Global Research and Development, La Jolla, Pfizer Inc, 10777 Science Center Drive, San Diego, California 92121, USA
    Biochemistry 48:5339-49. 2009
    ....
  17. pmc Multiple circulating proangiogenic factors induced by sunitinib malate are tumor-independent and correlate with antitumor efficacy
    John M L Ebos
    Sunnybrook Health Sciences Centre, Molecular and Cellular Biology Research, 2075 Bayview Avenue, Toronto, Ontario, Canada
    Proc Natl Acad Sci U S A 104:17069-74. 2007
    ..They may also be relevant to drug-associated toxicities, drug resistance, and observed rapid tumor (re)growth seen after cessation of therapy...
  18. ncbi request reprint Functional expression and mutations of c-Met and its therapeutic inhibition with SU11274 and small interfering RNA in non-small cell lung cancer
    Patrick C Ma
    Section of Hematology Oncology, Department of Medicine, University of Chicago Medical Center, Pritzker School of Medicine, Chicago, Illinois, USA
    Cancer Res 65:1479-88. 2005
    ..These results indicate that c-Met inhibition will be an important therapeutic strategy against NSCLC to improve its clinical outcome...
  19. pmc Amplification of MET may identify a subset of cancers with extreme sensitivity to the selective tyrosine kinase inhibitor PHA-665752
    Gromoslaw A Smolen
    Cancer Center and Department of Pathology, Molecular Pathology Research Unit, Massachusetts General Hospital, Harvard Medical School, Charlestown, MA 02129, USA
    Proc Natl Acad Sci U S A 103:2316-21. 2006
    ..MET amplification may thus identify a subset of epithelial cancers that are uniquely sensitive to disruption of this pathway and define a patient group that is appropriate for clinical trials of targeted therapy using MET inhibitors...
  20. ncbi request reprint Sunitinib malate for the treatment of solid tumours: a review of current clinical data
    Robert J Motzer
    Memorial Sloan Kettering Cancer Center, 1275 York Avenue, New York, NY 10021, USA
    Expert Opin Investig Drugs 15:553-61. 2006
    ..Sunitinib has also demonstrated promising clinical activity in the treatment of other advanced solid tumours. The present review provides an updated summary of emerging clinical experience with this promising new anticancer agent...
  21. pmc Inhibition of c-Met as a therapeutic strategy for esophageal adenocarcinoma
    Gregory A Watson
    Department of Surgery, University of Pittsburgh, Pittsburgh, PA, USA
    Neoplasia 8:949-55. 2006
    ..Factors other than receptor overexpression, such as c-Met-dependent PI3K/Akt signaling, may be predictive of an individual tumor's response to c-Met inhibition...
  22. ncbi request reprint A novel small molecule met inhibitor induces apoptosis in cells transformed by the oncogenic TPR-MET tyrosine kinase
    Martin Sattler
    Department of Medical Oncology, Dana Farber Cancer Institute, Boston, Massachusetts 02115, USA
    Cancer Res 63:5462-9. 2003
    ..The characterization of SU11274 as an effective inhibitor of Met tyrosine kinase activity illustrates the potential of targeting for Met therapeutic use in cancers associated with activated forms of this kinase...
  23. doi request reprint Genomic alterations of anaplastic lymphoma kinase may sensitize tumors to anaplastic lymphoma kinase inhibitors
    Ultan McDermott
    Center for Molecular Therapeutics, Massachusetts General Hospital Cancer Center, Harvard Medical School, Charlestown, MA 02129, USA
    Cancer Res 68:3389-95. 2008
    ..These findings suggest that a subset of lung cancers, lymphomas, and neuroblastomas that harbor genomic ALK alterations may be clinically responsive to pharmacologic ALK inhibition...
  24. doi request reprint An in vivo model of Met-driven lymphoma as a tool to explore the therapeutic potential of Met inhibitors
    Paolo Accornero
    Department of Anatomy, Pharmacology, and Forensic Medicine, University of Torino, Torino, Italy
    Clin Cancer Res 14:2220-6. 2008
    ..A far superior model would be a transgenic line developing spontaneous Met-driven tumors with high penetrance and short latency...
  25. pmc Antiangiogenic and anti-invasive effects of sunitinib on experimental human glioblastoma
    Sophie De Bouard
    GRECAN, Centre Francois Baclesse, Universié de Caen Basse Normandie, 14076 Caen, France
    Neuro Oncol 9:412-23. 2007
    ..Sunitinib exhibited potent antiangiogenic activity that was associated with a meaningful prolongation of survival of mice bearing intracerebral GBM. These data support the potential utility of sunitinib in the treatment of GBM...
  26. ncbi request reprint A selective c-met inhibitor blocks an autocrine hepatocyte growth factor growth loop in ANBL-6 cells and prevents migration and adhesion of myeloma cells
    Håkon Hov
    Department of Cancer Research and Molecular Medicine, Norwegian University of Science and Technology, Trondheim, Norway
    Clin Cancer Res 10:6686-94. 2004
    ..We wanted to examine the role of the hepatocyte growth factor (HGF) receptor c-Met in multiple myeloma by applying a novel selective small molecule tyrosine kinase inhibitor, PHA-665752, directed against the receptor...
  27. ncbi request reprint Preclinical efficacy of the c-Met inhibitor CE-355621 in a U87 MG mouse xenograft model evaluated by 18F-FDG small-animal PET
    Jeffrey R Tseng
    Molecular Imaging Program at Stanford, Bio X Program, and Department of Radiology, Stanford University, Stanford, California 94305 5427, USA
    J Nucl Med 49:129-34. 2008
    ..The purpose of this study was to evaluate the efficacy of CE-355621, a novel antibody against c-Met, in a subcutaneous U87 MG xenograft mouse model using (18)F-FDG small-animal PET...
  28. ncbi request reprint A selective small molecule c-MET Inhibitor, PHA665752, cooperates with rapamycin
    Patrick C Ma
    Section of Hematology Oncology, Department of Medicine, Pritzker School of Medicine, University of Chicago Medical Center, 5841 South Maryland Avenue, Chicago, IL 60637, USA
    Clin Cancer Res 11:2312-9. 2005
    ..Here, we characterized a small molecule c-MET inhibitor, PHA665752, and tested its cooperation with the mammalian target of rapamycin inhibitor as potential targeted therapy...