Optical molecular imaging holds great promise for image guiding cancer therapy. The non-invasive guidance of
therapeutic strategies would enable the removal of cancerous tissue while avoiding side effects and systemic toxicity, preventing
damage of healthy tissues and decreasing the risk of postoperative problems. This review article highlights the advantages
and disadvantages of the optical imaging techniques that are currently available, including their recent applications
in image-guided cancer therapy. Three approaches for optical image-guided cancer therapy were discussed in this
review, namely, bioluminescence imaging (BLI), fluorescence imaging (FI) and Cerenkov luminescence imaging (CLI).
BLI is always used in small animal imaging for the in vivo tracking of therapeutic gene expression and cell-based therapy.
To the contrary, FI display high promising for clinical translation. The applications of FI include image-guided surgery,
radiotherapy, gene therapy, drug delivery and sentinel lymph node fluorescence mapping. CLI is a novel radioactive optical
hybrid imaging strategy and its use for animal and clinical translation was also discussed. Perspectives on the translation
of optical image-guided cancer therapy into clinical practice were provided.