Cancer is one of the leading disease-caused deaths of the human population in many countries. After a great century of advances, cancer research has generated a rich and complex body of knowledge, revealing the molecular mechanisms and pathophysiology of human cancer. This knowledge provides us with the opportunity to find novel targets for drug development. Future drugs would have greater antitumor activity with less toxicity and side effects to patient than currently used medicines. The fruition of the hard work in the past years is just now being realized with many promising clinical trials.