Identifying a suitable drug target is crucial in modern drug discovery methods. Advancement in omics technologies, such as high-throughput genotyping, rigorous statistical analysis and large coordinated genome data of patients, has significantly improved the identification and validation of potential drug targets. This is especially true of next-generation sequencing methods and advanced proteomics approaches, which have played vital roles in therapeutic target identification. This special issue collects together 12 articles focused on omics technologies and their integration towards drug target identification, validation and subsequent therapeutic implications. Data sets obtained from genome sequence generally provide a list of differentially expressed genes associated with disease states. After a series of computational and biochemical experiments, these differentially expressed genes are considered markers or therapeutic targets. However, in-depth analysis of such data types is limited because of a single or a limited number of approaches. Thus, integrating different omics data types will be an attractive strategy to investigate the real cause of disease, biomarker discovery and identification of therapeutic targets that could be further validated through clinical and molecular studies.