@entity7 receptor XXXX kinase inhibitors: @entity17482 / @entity17482 .

@entity1 @entity137 @entity390 @entity101 @entity7 @entity5 @entity17482 @entity19 @entity391 @entity319 @entity14 @entity6758 @entity669 @entity2055
@entity17482 / @entity17482 (PTK/ZK) is an oral potent and selective inhibitor of the @entity7 ( @entity7 )-mediated @entity6758 and @entity319 receptor @entity669 kinases. PTK/ZK has been shown to reduce growth and microvasculature in subcutaneously implanted @entity1 @entity5 xenografts in @entity19 . A clinical difficulty in evaluating angiogenesis inhibitors has been the usefulness of conventional study endpoints. Therefore, dynamic contrast-enhanced magnetic resonance imaging (DCE-MRI) has been studied as a pharmacodynamic marker of efficacy of PTK/ZK. Phase I studies are under way evaluating the optimum dose and schedule of oral PTK/ZK administered continuously to @entity1 with advanced @entity5 of types known to overexpress @entity7 . To date, particularly in @entity1 with liver metastases from @entity14 treated with PTK/ZK, DCE-MRI has been a useful predictor of the biological response of @entity7 -receptor inhibition. @entity137 have been manageable and have included lightheadedness, @entity2055 , @entity390 , @entity391 , and @entity101 . Stabilization of disease for >/= 6 months has been seen in heavily pretreated @entity1 receiving PTK/ZK at higher doses. Preliminary data suggest that PTK/ZK can be administered safely on a continuous daily dosing schedule, efficacy data look promising, and DCE-MRI correlates with biological response. DCE-MRI will be used to guide dose optimization of PTK/ZK and perhaps of other angiogenesis inhibitors in future studies.
