Abstract: The continuous growth of Chinese pharmaceutical and healthcare market is driven by factors such as the intensifying aging population, rising prevalence of chronic diseases, improving consumption levels, and increasing health awareness. However, medical resources in China are limited and unevenly distributed. Additionally, the pharmaceutical supply chain is complex and the distribution of drugs is highly fragmented. These reasons leave patients in the dilemma of “difficulty in accessing medical care and high drug costs”. Organically connecting patients with pharmaceuticals and medical services pharmaceuticals a significant challenge. With the liberalization of healthcare policies and advancements in digital technologies, pharmaceutical and healthcare enterprises are attempting digital transformation to solve the dilemma by building digital platform ecosystems. To this end, the study extracts the iterative process by which pharmaceutical and healthcare enterprises achieve digital transformation and digital platform ecosystems through a case study of 111 Inc. Results find that: (1) the digital transformation of pharmaceutical and healthcare enterprises progresses through three stages including initial exploration, extended transformation, and ecological construction, achieving autonomous digital transformation from 0 to 1 and empowered digital transformation from 1 to N. (2) Enterprises with ecosystem-oriented strategies adopt a business model innovation-driven transformation mode during their digital transformation. They adjust digital resource allocation to address the needs of multiple eco-participants, break enterprise boundaries, empower digital connectivity, and co-build digital platform ecosystems. The conclusions of this study provide significant practical guidance for the digital transformation operation of healthcare enterprises and contribute to the digital development of the pharmaceutical and healthcare industry.