Recent advances have dramatically advanced our understanding of cancer at the molecular level. In turn, new therapeutic agents that target specific molecular defects in cancer have been developed, though cancer remains a significant health threat. Following an introduction to the molecular biology of cancer, a statistical approach to distinguish driver mutations from passengers based on non-random clustering will be discussed. Next, approaches to pharmaceutical intervention will be reviewed and an integrated approach to link targeted therapeutics with specific patient populations will be shown. Throughout, open questions will be presented with a focus on problems of potential mathematical interest.