Abstract: Chinese medicine and targeted therapy belong to two different disciplinary systems. They have both differences and multiple connections and potential for integration. This is mainly reflected in the interconnectedness of the theoretical system， the syntropy of the purpose and the complementarity of the practical means. Targeted treatment of functional substance of Chinese medicine can be understood from two perspectives. On the one hand， many active ingredients derived from Chinese medicine have difficulties in druggability， which can be solved using the modern targeted technology for enhancing the efficacy and reducing the side effects. On the other hand， under the guiding thought of Chinese medicine， many functional substances of Chinese medicine endow drugs or preparations orientation to the specific regions， leading to the improved therapeutic effect. In this review， we summarize the research progress in recent years from the above two aspects in order to understand and discover the intrinsic relationship between them and the potential value of development， which will promote the integration development of Chinese medicine and pharmaceutics.