It has been the golden criterion in the drug discovery and development industry for hundreds of years that a single and identical component with a clear mechanism of action is a desirable candidate for potential drugs. However, this conventional strategy of drug discovery and development is facing challenges, including a low success rate and high development cost.  In this review, we critically reviewed the state-of-the-art of drug discovery and development from multiple components of Chinese Medicine formulas. We reviewed the policies and status of the application of multi-component Chinese Medicine formula-based new drugs in the US, China, and the European Union, and illustrated several excellent cases of ongoing applications. We also discussed the biomedical technologies that may pave the way to facilitate drug discovery and development from multi-component Chinese Medicine formulas including network pharmacology, integrative OMICs, Crispr gene editing and chemometrics. Lastly, we discussed the possible problems and solutions in the pre-clinical and clinical research in drug discovery and development of multi-component Chinese Medicine formulas. We hope this review will facilitate the discussion on the role of multi-component Chinese Medicine formulas in the new drug discovery and development for the treatment of human diseases.