Affiliation: Novartis Institutes for BioMedical Research
- Tyrosine kinase inhibitors: from rational design to clinical trialsP Traxler
Novartis Pharma AG, Oncology Research, CH 4002 Basel, Switzerland
Med Res Rev 21:499-512. 2001..In addition, potent inhibition of the PDGFR and c-Kit tyrosine kinases also indicates its possible clinical use in solid tumors...
- Tyrosine kinases as targets in cancer therapy - successes and failuresPeter Traxler
Novartis Pharma AG, Oncology Research, CH4002 Basel, Switzerland
Expert Opin Ther Targets 7:215-34. 2003....
- AEE788: a dual family epidermal growth factor receptor/ErbB2 and vascular endothelial growth factor receptor tyrosine kinase inhibitor with antitumor and antiangiogenic activityPeter Traxler
Oncology Research, Novartis Institutes for BioMedical Research, Klybeckstrasse, CH 4002 Basel, Switzerland
Cancer Res 64:4931-41. 2004..Consequently, AEE788 is currently in Phase I clinical trials in oncology...
- New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven angiogenesisG Bold
Oncology Research, and Process Research, Novartis Pharma AG, CH 4002 Basel, Switzerland
J Med Chem 43:2310-23. 2000..Since these 1-anilino-(4-pyridylmethyl)phthalazines are orally well absorbed, these compounds qualify for further profiling and as candidates for clinical evaluation...
- Protein kinases as targets for anticancer agents: from inhibitors to useful drugsDoriano Fabbro
Department of Oncology, Novartis Pharma Inc, WKL 125 4 10, CH 4002, Basel, Switzerland
Pharmacol Ther 93:79-98. 2002..Phase I/II studies demonstrated that STI571 is well tolerated, and that it showed promising hematological and cytogenetic responses in CML and clinical responses in the c-Kit-driven gastrointestinal tumors...
- Imatinib mesylate is a potent inhibitor of the ABCG2 (BCRP) transporter and reverses resistance to topotecan and SN-38 in vitroPeter J Houghton
Department of Molecular Pharmacology, St Jude Children s Research Hospital, Memphis, Tennessee 38105 2794, USA
Cancer Res 64:2333-7. 2004..These results suggest that imatinib mesylate inhibits the function of ABCG2 but is not a substrate for this transporter...
- Combination therapy of inhibitors of epidermal growth factor receptor/vascular endothelial growth factor receptor 2 (AEE788) and the mammalian target of rapamycin (RAD001) offers improved glioblastoma tumor growth inhibitionRanjit K Goudar
Department of Pathology, Duke University Medical Center, P O Box 2900, Durham, NC 27710, USA
Mol Cancer Ther 4:101-12. 2005..These studies suggest that simultaneous inhibition of growth factor receptor and mTOR pathways offer increased benefit in glioma therapy...
- Integral role of the EGF receptor in HGF-mediated hepatocyte proliferationLawrence A Scheving
Department of Pediatrics, Medical Center, Vanderbilt University School of Medicine, Nashville, TN 37232, USA
Biochem Biophys Res Commun 290:197-203. 2002..The mitogenic effect of HGF may be secondary to increased synthesis or processing of EGFR ligands such as TGF-alpha...
- Salicylanilides as inhibitors of the protein tyrosine kinase epidermal growth factor receptorChristoph Liechti
Department of Chemistry, University of Basel, St Johanns Ring 19, CH 4056 Basel, Switzerland
Eur J Med Chem 39:11-26. 2004..Some of them indeed proved to be potent and selective EGFR tyrosine kinase inhibitors. The most potent ones being 28, 16, 20, 6, and 15, with IC(50) in the 23-71 nM range...