In 2019, the emerging RNA virus, severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), gained the ability to infect human beings, then turned into human-to-human transmission, and eventually led to a pandemic of coronavirus disease 2019 (COVID-19), causing serious damage not only to global public health but also economic activities for years. Now, fast-mutating SARS-CoV-2 continues to produce new variants that threaten the world. As such, there is still a high demand for the development of effective treatments for combating new variants of SARS-CoV-2 infection and mitigating diverse post-COVID symptoms, including those who are long-COVID patients. This book introduces cutting-edge ways for drug discovery and pharmacological approaches to develop treatments and medications for COVID-19 based on modern technologies that highlight the applications of integrated multiple omics and advanced bioinformatics tools. It also lists a range of promising bioactive compounds derived from traditional herbal medicines and natural products. The book explains the expanding strategy to integrate a series of approaches including genomics, metagenomics, transcriptomics, proteomics, metabolomics, epigenomics, and bioinformatics to organize a system of multiple omics. International and reliable multi-omics databases, bioinformatics tools, and software are also comprehensively summarized and thus can be easily accessed by researchers. Artificial intelligence (AI) as a revolutionary tool in the fields of drug discovery, vaccine development, and computational medicine for COVID-19 is also addressed. The coordination and integration of AI tools within the system of multiple omics and the limitations and future directions of AI-assisted strategies for COVID-19-related research are comprehensively discussed as well.