J
Josef Brueggen
Researcher at Novartis
Publications - 22
Citations - 3433
Josef Brueggen is an academic researcher from Novartis. The author has contributed to research in topics: Tyrosine kinase & In vivo. The author has an hindex of 14, co-authored 22 publications receiving 3283 citations.
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Journal ArticleDOI
Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity
Sauveur-Michel Maira,Frédéric Stauffer,Josef Brueggen,Pascal Furet,Christian Schnell,Christine Fritsch,Saskia M. Brachmann,Patrick Chène,Alain De Pover,Kevin Schoemaker,Doriano Fabbro,Daniela Gabriel,Marjo Simonen,Leon Murphy,Peter Finan,William R. Sellers,Carlos Garcia-Echeverria +16 more
TL;DR: The preclinical data show that NVP-BEZ235 is a potent dual PI3K/mTOR modulator with favorable pharmaceutical properties, and the compound was well tolerated, displayed disease stasis when administered orally, and enhanced the efficacy of other anticancer agents when used in in vivo combination studies.
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In vivo antitumor activity of NVP-AEW541—A novel, potent, and selective inhibitor of the IGF-IR kinase
Carlos Garcia-Echeverria,Mark A. Pearson,Andreas Marti,Thomas Meyer,Juergen Mestan,Johann Zimmermann,Jiaping Gao,Josef Brueggen,Hans-Georg Capraro,Robert Cozens,Dean B. Evans,Doriano Fabbro,Pascal Furet,Diana Graus Porta,Janis Liebetanz,Georg Martiny-Baron,Stephan Ruetz,Francesco Hofmann +17 more
TL;DR: NVP-AEW541 represents a class of selective, small molecule IGF-IR kinase inhibitors with proven in vivo antitumor activity and potential therapeutic application and abrogates IGF-I-mediated survival and colony formation in soft agar at concentrations that are consistent with inhibition of IGF-ir autophosphorylation.
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Discovery of 3-(2,6-Dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), A Potent and Selective Inhibitor of the Fibroblast Growth Factor Receptor Family of Receptor Tyrosine Kinase
Vito Guagnano,Pascal Furet,Carsten Spanka,Vincent Bordas,Mickaël Le Douget,Christelle Stamm,Josef Brueggen,Michael Rugaard Jensen,Christian Schnell,Herbert A. Schmid,Markus Wartmann,Joerg Berghausen,Peter Drueckes,Alfred Zimmerlin,Dirksen E. Bussiere,Jeremy Murray,Diana Graus Porta +16 more
TL;DR: In vivo evaluation of compound 1h showed significant antitumor activity in RT112 bladder cancer xenografts models overexpressing wild-type FGFR3 and support the potential therapeutic use of 1h as a new anticancer agent.
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Role of α1 Acid Glycoprotein in the In Vivo Resistance of Human BCR-ABL+ Leukemic Cells to the Abl Inhibitor STI571
Carlo Gambacorti-Passerini,Rossella Barni,Philipp le Coutre,Massimo Zucchetti,Gonçalo Cabrita,Loredana Cleris,Francesca Rossi,Elisabetta Gianazza,Josef Brueggen,Robert Cozens,Pietro Pioltelli,Enrico Pogliani,Gianmarco Corneo,Franca Formelli,Maurizio D'Incalci +14 more
TL;DR: AGP in the plasma of relapsed animals binds to STI571, preventing this compound from inhibiting the Bcr/Abl tyrosine kinase, and molecules such as erythromycin that compete with STi571 for binding to AGP may enhance the therapeutic potential of this drug.
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AEE788: a dual family epidermal growth factor receptor/ErbB2 and vascular endothelial growth factor receptor tyrosine kinase inhibitor with antitumor and antiangiogenic activity.
Peter Traxler,Peter R. Allegrini,Ralf Brandt,Josef Brueggen,Robert Cozens,Doriano Fabbro,Konstantina Grosios,Heidi Lane,Paul M.J. McSheehy,Juergen Mestan,Thomas J. Meyer,Careen Tang,Markus Wartmann,Jeanette Marjorie Wood,Giorgio Caravatti +14 more
TL;DR: Data indicate that AEE788 has potential as an anticancer agent targeting deregulated tumor cell proliferation as well as angiogenic parameters, and is currently in Phase I clinical trials in oncology.