Cancer remains the second leading cause of death both in industrialized and non-industrialized countries and is increasing in incidence elsewhere in the world as the population ages. The enormous advances in knowledge, science and technology in the 21st century have facilitated the process of globalization with the aim of better quality of life for all. The development of more effective, efficient, less risky and less toxic drugs for treatment of cancer has been a major human endeavor for the past 50 years. With the introduction of the “targeted drugs” and currently available treatment regimens, 5-year survival rate among the adults for all cancers has increased to approximately 65%. The improvement in the survival rate of childhood leukemia (ALL), being the most fatal childhood cancer, over the past 35 years is one of the great success stories of cancer treatment. In the 1960s, while less than 5 percent of children with ALL survived for more than five years, today, about 85% of children live five years or more. The 5th International Conference on Drug Discovery and Therapy is an effort to address all areas towards anti-cancer agents. Emphasis was given to drugs that have recently been introduced into the cancer therapy including: inhibitors of chromatin function, target-based inhibitors of signal transduction (tyrosine kinase inhibitors) Ê and cyclindependent kinases, and angiogenesis inhibitors acting on metalloproteinases, epithelial cell growth, and angiogenesis stimulation. There will be presentations from contributors working on hormone synthesis inhibitors and hormone-receptors blockers, RNA interference, role of pharmacogenomics in anti-cancer drug development and computer aided-strategies for anti-cancer drug design and development and related areas.