Facing new human disease patterns and the post-genome era of the 21st century, life science and the development of new drugs has entered a competitive and challenging era. In the future, the target for the development of new drugs will relate to the control of genes involved in major human diseases using functional genomics and bioinformatics. By chemical synthesis and modification and through the help of structural biology and molecule simulation as well as the introduction of combinational chemistry, we can create new lead compounds. With the help of transgenic animals, we are able to manifest the genes related to human diseases and the symptoms of the diseases and use the pathological patterns within these animals for the development of new drugs. Through the establishment of an intercollegiate research team and curriculum, we can integrate life science and clinical medicine, train professional personnel in innovative drug development and start a modern pharmaceutical science education and research system in response to the post-genome era.