The initial results of DNA sequencing of the human genome were published in February 2001. Life sciences are now giving priority to the explication of the functions of genes and proteins over research into DNA sequencing. Life sciences are making great strides with the release of genomic information, and the results obtained will be utilized in drug research. Thus, drug discovery in the 21st century will be forced to shift to genomic approach. The information may be utilized in all the steps of conventional drug research. Above all, it is expected to be most useful in the identification of targets, the first step in drug research, as well as in clinical trials, the last step. Examples are emerging that elucidation of orphan receptors/ligands and transcriptome analyses are useful in identifying drug target molecules. To date, the science of drug discovery has made good use of the accomplishments of all the life sciences. In the future, genomic drug discovery is expected to open out an innovative drug research by merging conventional methods of drug discovery with such multidisciplinary technologies as bioinfomatics, structural biology, and computer and systems technology, based on genomic information. It is hoped that this will produce drugs of higher quality. Such advances are expected to improve the QOL and have a medicoeconomic effect.