The historical model of drug discovery and development has been considered unsustainable because of its low innovation capacity and low productivity. The influence of the pandemic and the energy crisis, supply chain disruption, and increasing regulatory requirements put pharmaceuticals in the new era, in which sustainable development has attracted increased amounts of attention, as a top priority. Sustainability has started to increase from being an encouraging factor to being a critical, vital factor across the entire value chain of drug development. The planet’s resources need to be protected for generations to prevent climate change as well as create sustainable value. Highly efficient and innovative research and development, agile marketing, sustainable product supply organization, and the renewal of strength to make a difference for patients are needed. There have been numerous challenges in shifting the current platform to sustainable pharmaceutical development because of the business model, technology, and healthcare burden. In this chapter, the detailed challenges involved in the sustainable development of drugs are discussed, as are the opportunities associated with each factor. Moreover, the challenges in sustainable pharmaceuticals are integrated into global development, which will be addressed quickly to explore such issues worldwide.