The 21st international symposium of the American Association for Cancer Research (AACR), the NCI and the European Organization for Research and Treatment of Cancer (EORTC), held in Boston, included topics covering the development of therapeutics and molecular targets in the field of cancer research. This conference report highlights selected presentations on the development of novel drugs for cancer. Investigational drugs discussed include XL-139 (Bristol-Myers Squibb Co/Exelixis Inc), SPC-3042 (Enzon Pharmaceuticals Inc/ Santaris Pharma A/S), CH-5137291 (Chugai Pharmaceutical Co Ltd), SN-29966/SN-29926/SN-3000 (Proacta Inc), withaferin-A (University of Kansas), Reolysin (Oncolytics Biotech Inc), EZN-3889 and EZN-3892 (Enzon Pharmaceuticals/Santaris Pharma), and CBP-501 (CanBas Co Ltd/Takeda Pharmaceutical Co Ltd).