This chapter explores the transformative role of artificial intelligence (AI) in drug repurposing and personalized medicine, emphasizing its potential to revolutionize healthcare delivery. AI-driven drug repurposing leverages machine learning and deep learning algorithms to identify new therapeutic uses for existing drugs, significantly reducing development timelines, financial risks, and resource requirements. Concurrently, personalized medicine, powered by genomic profiling and multi-omics data integration, tailors treatments to individual patients based on their unique genetic, environmental, and lifestyle factors. The chapter delves into the specific AI algorithms employed, such as neural networks, graph neural networks, and generative adversarial networks, and their applications in drug discovery, treatment alignment, and addressing rare diseases. It highlights AI’s ability to accelerate diagnosis, optimize clinical trials, and enable cost-effective solutions for rare and orphan diseases. The broader implications of AI in healthcare, including ethical considerations, data governance, and the integration of AI with clinical workflows, are also discussed. Through practical examples and case studies, the chapter underscores AI’s potential to enhance patient outcomes, reduce healthcare costs, and address previously unmet medical needs.