Current assessment of the effect of anticancer drugs relies on measurement of tumor volume using structural imaging modalities such as CT/MRI. Functional imaging allows assessment of tumor physiology and metabolism in vivo. These measurements are more directly related to the anticancer drug target and may provide more specific and sensitive methods of assessing anticancer drug activity and response. Positron emission tomography (PET) is a sensitive, quantitative method of imaging radiotracers labeled with biologically important radionuclides. PET can be used to measure alterations in perfusion in response to pharmacological manipulation of tumor vasculature to improve drug delivery and in the future to assess novel therapeutic agents targeted directly at the tumor vasculature. 2-[11C]-thymidine, a marker of proliferation, and [18F]-FDG, a marker of glucose metabolism reflecting tumor cell viability, may provide more sensitive methods of assessing anticancer drugs for in vivo activity for Phase I and II trials. In addition, 2-[11C]-thymidine may be used to demonstrate the pharmacodynamic effects of specific enzyme inhibitors. Improved identification and measurement of in vivo activity in Phase MI trials may assist drug selection prior to commencement of very costly Phase III assessment.
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