The field of drug discovery is continually advancing with the emergence of new technologies and scientific developments. Moreover, there is a recent growing interest in exploiting natural products as a potential source of novel drug leads. This chapter provides an overview of the current state of new drug discovery, with a specific focus on natural products and integrative medicine. The drug discovery process is discussed, including target identification, lead generation, lead optimization, and preclinical and clinical development, along with the challenges associated with each step and potential solutions. The use of natural products as a source of novel drug leads is explored, including examples of natural products that have been transformed into drugs and current efforts to discover new natural product-based drugs. Furthermore, the chapter proposes valuable insights into the challenges and opportunities in this field, as well as potential solutions for discovering and developing new drug leads.