In this review, fundamentals of nuclear quadrupole resonance (NQR) spectroscopy are briefly outlined. Examples of its applications in drug development are discussed to demonstrate that the NQR method is a sophisticated, non-destructive and valuable analytical technique for studying pharmaceuticals, providing effective assistance at the two main steps of drug development: the physical and chemical characterization of the active pharmaceutical ingredients (API) at the analytical step and API development. This review covers different aspects of the use of NQR spectroscopy for drug development and analysis and illustrates the power and versatility of this method in the determination of impurities, polymorphic forms, the drug's structure and conformation, characterization of the interactions between the drug and ligands, search for analogs (second- or third-generation drugs) and the drug's thermal stability. Lastly, NQR advantages and restrictions in the aspect of application in drug development studies are summarized.