Ecological transition is an urge for society for the prosperous and safe future of humankind. Within this context, environmentally friendly development of active pharmaceutical ingredients (API) represents a yet underinvestigated research area with an expected huge expansion in the years to come. The proposed course is intended to complement the information on well-established API preparations and formulations provided by the fundamental courses with recent green alternative solutions. The paramount green chemistry principles as well as the different green metrics developed over time will be introduced to evaluate potential criticalities of an API development process and to assess its impact in comparison to other processes. Special attention will be devoted to the actual and often overlooked impact of traditional volatile organic solvents and on possible and feasible options for their replacement. The course aims at providing the students with insights on yet unresolved challenges and on the most recent options available to redesign and rethink traditional API preparations and formulations in view of a conscious, sustainable and safe development.