Therapeutically targeted anticancer agents: inhibitors of receptor tyrosine kinases.
The rationale to target receptor protein tyrosine kinases (RPTKs) as an approach to cancer chemotherapy has continued to become more compelling with time. Preclinical and clinical data strongly support the involvement of specific RPTKs in the formation and progression of a subset of solid and liquid tumors. The advances in our understanding of the oncogenic activation of these receptors have been matched by the identification of new structural classes of kinase inhibitors that exhibit enormous improvements with regard to potency, specificity and efficacy. This article summarizes current knowledge of the most promising RPTK inhibitors in clinical trials or known to be in late stage preclinical development.
García-Echeverría
Carlos
C
Oncology Research, Novartis Pharma AG, CH-4002 Basel, Switzerland. carlos.garcia-echeverria@pharma.novartis.com
Fabbro
Doriano
D
D020533:Angiogenesis Inhibitors / Q000737:chemistry / Q000627:therapeutic use*; D000818:Animals; D002986:Clinical Trials as Topic; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000627:therapeutic use*; D066246:ErbB Receptors / Q000037:antagonists & inhibitors; D006801:Humans; D015394:Molecular Structure; D009369:Neoplasms / Q000188:drug therapy / Q000201:enzymology / Q000235:genetics; D020794:Receptor Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors*; D015398:Signal Transduction / Q000187:drug effects
D020533:Angiogenesis Inhibitors; D004791:Enzyme Inhibitors; D066246:ErbB Receptors; D020794:Receptor Protein-Tyrosine Kinases