The production of plant-derived pharmaceuticals, particularly artemisinin (from Artemisia annua L.) and Taxol (from Taxus brevifolia Nutt.), is a critical area of innovation that holds huge potentials in addressing drug availability and global health challenges. Artemisinin, discovered in 1970s, has been used as an effective antimalarial drug. Similarly, Taxol has been used in the treatment of cancer as a chemotherapeutic agent. Although these two compounds are of immense therapeutic importance, their production faces several challenges including low natural product yields and complicated extraction procedures, as well as challenges related to environmental impact, economic viability, and regulatory issues. The present chapter explores the geographical distribution, ethnobotanical significance, and pharmacological relevance of Artemisia and Taxus. Focuses are also laid on strategies to alleviate the challenges, such as phytohormone application, biotic and abiotic elicitation, transgenic technologies, precursor feeding, and bioreactor cultivation. It emphasizes on sustainable practices like greener extraction methods, continuous manufacturing processes and advancements in greenhouse cultivation using LED lighting. Despite the current advancements made in enhancing the production of artemisinin and Taxol through the use of biotechnological applications, further research is needed to ensure sustainable production and improved availability of these clinical drugs worldwide.