Molecular imaging is emerging as an incredibly powerful tool in oncology research. With unprecedented specificity to capture some of the key cancer hallmarks (e.g., proliferation), it can assess pharmacodynamic effects of various therapies on tumor response. A general overview of molecular imaging, its potential and limitations will be presented in the lecture. An example of a pharmacodynamic study using 3′-deoxy-3′[(18)F]-fluorothymidine, [(18)F]-FLT PET/CT in assessing response to anti-angiogenic therapies (VEGFR TKI) will be shown. Patient-specific modeling of tumor response to VEGFR TKI based on FLT PET/CT molecular imaging will be used to illustrate intimate connection between tumor modeling and molecular imaging-based clinical trials.