Introduction: This paper aims to conduct a systematic analysis about the efforts made to modernize the Chinese 'herbal piece' using an innovation system approach. Methods: Archival documents and literature were comprehensively reviewed with the assistance of field interviews with industrial practitioners and academic researchers. Results: Data collected suggested that the construction of an innovation system has been the key to modernize the Chinese 'herbal piece'. The incorporation of the knowledge base of Traditional Chinese Medicine (TCM) theory and modern biotechnology has shaped the path leading to its innovation. Moreover, the entrepreneurial activities of leading firms have embedded these knowledge bases and with institutional support from the government and so the modernisation process has been accelerated. Conclusions: The modernisation of Chinese 'herbal piece' has been promoted by developing a specific innovation system. Efforts towards the modernisation process have included the integration of different knowledge bases, entrepreneurial activities, establishment of cooperative networks between academics and industry, as well as policy supports. Such efforts have transferred the Chinese 'herbal piece' from just a traditional heritage to a modern medicine. The modernisation of Chinese 'herbal pieces' in fact could provide opportunities for innovations in traditional medicine given the environmental pressures and health challenges.