This chapter provides an eclectic introduction to the significance and relevance of entrepreneurship and innovation for regional and social development in varied contexts. It identifies the key concepts, facts, structures and the distribution of regional contexts for the transformative agendas for entrepreneurial and innovative activity. It provides a route map for the journey undertaken as part of the development of the book. It shows how people, organisations and environments are linked together in their roles in entrepreneurial economic and social development. The chapter demonstrates how the complex elements of evolving entrepreneurship and innovation can be curated to help us with a critical appreciation of the subject.