Artificial Intelligence (AI) and machine learning (ML) have evolved as technology-driven game changers with the power to radically alter the functionality of the broader pharmaceutical research and development (R&D) spectrum. The pharmaceutical and healthcare enterprise sector is driven by big data, which are mostly complex in nature, thus necessitating the deployment of AI as a tool to optimize functionality. In fact, AI in various forms is being integrated into diverse operational aspects of the pharmaceutical and healthcare sector for seamless functionality. Administrative activities, patient engagement, and treatment adherence are some of the mission critical areas where AI is being leveraged. AI-powered automation is a proven choice to minimize human intervention across the pharmaceutical and healthcare domain; yet its usage as a performance optimizing tool is limited due to implementation constraints. Ethical implications of integrating AI in a highly sensitive area like healthcare often dominate the narrative putting leaders and managers in a deep dilemma. This chapter initially discusses AI from a pharmaceutical R&D standpoint, spanning frequently implemented techniques and other critical components of AI research. The subsequent parts of this chapter classify the applications of AI in the field and briefly introduce some of these applications.