The past few decades have brought on a dramatic change in the treatment of cancer; however, routine treatments fail to specifically clear tumorigenic cells and may be followed by cancer recurrence. Recent advances in developing multifunctional nanoparticles provide exciting new possibilities for drug delivery used in tumor-targeted therapy. Moreover, molecular imaging is an invaluable tool in evaluating new molecular targets, cancer diagnosis, predicting of tumor response to available therapies and monitoring response to therapy as well as developing new drugs prior to clinical translation. Combining of targeted cancer therapy and molecular imaging, termed as image-guided drug delivery, can achieve objectives of noninvasive assessment of drug biodistribution and real-time monitoring of therapeutic responses. Image-guided drug delivery has become an upcoming field with extensive prospect in cancer therapy and may provide an effective platform for personalized cancer care. This review will focus on the significance and recent advances in targeted and traceable therapeutic strategy for cancer therapy.