In the vast tapestry of modern medicine, plant-based pharmaceuticals are a testament to the enduring synergy between nature’s bounty and human ingenuity. This chapter embarks on an expansive exploration of phytopharmaceuticals, delving deep into their historical roots, current applications, and the intricate scientific principles that underpin their development and production. As we navigate the multifaceted world of plant-derived drugs, we will uncover the complex interplay of traditional knowledge and cutting-edge biotechnology that characterizes this field. The journey of a plant-based pharmaceutical from a seed in the soil to a pill in a patient’s hand is a remarkable odyssey, encompassing disciplines as diverse as botany, chemistry, pharmacology, and biotechnology. It is a journey that spans continents and centuries, from the ancient herbal traditions of diverse cultures to the sterile laboratories of modern pharmaceutical companies. This chapter aims to provide a comprehensive overview of this journey, illuminating plant-based pharmaceutical production's challenges, triumphs, and future prospects.