A course centered around transition-metal catalysis in modern drug discovery was designed to illustrate the central role of organic chemistry in driving small-molecule drug development. The course highlighted both fundamental and applied concepts, first with a focus on the drug discovery process, followed by foundational principles in catalysis and modern catalytic methods. Finally, these topics were unified in the last portion of the course, where case studies served to highlight the use of transition-metal catalysis in the synthesis of modern drugs. Three graduate students designed and taught the course, with mentorship from a faculty member, leading to several notable teaching outcomes. Additionally, experts in the fields of catalysis and drug discovery served as guest lecturers throughout the duration of the course. This approach spotlighted the various careers that organic chemists play in the development of new medicines. We hope that this course motivates the creation of other courses in STEM that unify fundamental concepts with applications and career outcomes.