Recent scientific advances have brought significant progress in cancer treatment, but also reveal the challenges and complexities of pharmacologically targeting cancer. These advances extend from genomics, to chemical biology, to acquiring knowledge of the unique susceptibilities of individual cancers that drive drug discovery. This symposium provides a state-of-the art overview of Cancer Pharmacology by international leaders in their respective fields. Topics include: using genomics to elucidate the determinants of anticancer drug toxicity and efficacy; discovering druggable pathways in novel, clinically relevant models of the most deadly CNS pediatric cancers; how deciphering the mechanism of action of a natural product, taxol, catalyzed breakthroughs in cancer therapy; and discovering small molecules that disrupt protein interactions, which cancers depend upon.