Traditionally, pharmaceutical analysis referred to the chemical analysis of drug molecules. However, over the years, modern pharmaceutical analysis has evolved beyond this to encompass combination techniques, high-throughput technologies, chemometrics, microdosing studies, miniaturization and nanotechnology. These analytical advances are now being employed in all stages of drug discovery and the focus of this review will be on how these technologies are being employed within this process. With new, improved and evolving technologies, as well as new applications for existing technology, the search for new drugs for the prevention and treatment of human diseases continues.