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.