This document is a review of the course of genomic drug discovery and its clinical applications. Several key steps in the course of genomic drug discovery are followed as genomic research, gene discovery including susceptibility genes for diseases and drug response genes, functional and structural genomics, new specific drug target validation, rational drug design, lead hit & optimization, preclinical studies and efficient clinical studies with polymorphism analysis and SNPs generation. The most critical points and successful promises of drug discovery lie in the potential to understand disease processes at the molecular level, to determine the optimal molecular targets for drug design, and to select the lead compounds that modulate a protein's activity and have optimal absorption, distribution, metabolism, excretion and toxicity properties, using bioinformatics and structural genomics. Genomic research in the human genome project will lead not only to identification of more relevant drug targets leading to more specific drug therapies, but also to DNA-based diagnosis, leading to earlier treatment or change in lifestyles and tailor-made treatments specific to disease-subtype, including treatments which avoid side-effects. Furthermome, this is focused on the successful new drug discovery on molecular target therapy of cancers, e. g. (1) imatinib (Glivec
®) for chronic myelogenous leukemia and acute lymphocytic leukemia with Ph
1 chromosome, (2) trastuzumab (Herceptin
®) for breast cancer with HER2 overexpression, (3) rituximab(Rituxan
®) for malignant B-cell lymphoma and the (4) ZD 1839 (Iressa
®) for non-small cell lung cancer.
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