Translational pharmaceutics is a relatively new cross-disciplinary construct that integrates discovery and development for efficiently enabling discovery activities to deliver commercially viable medicines. This article describes the role and deliverables of its various subfunctions, namely, preclinical formulations, physical chemistry, drug product prototyping and development, and biopharmaceutics. The integrated aspects of these deliverables, that enable drug discovery, while also influencing and enabling the selection of compounds for clinical testing, in a manner that embraces the principles of R&D essentialism and design thinking, are also described. This article also illustrates how cost and time savings can be achieved through the application of robust mathematical modeling where possible, to guide the generation of the most relevant experimental data, followed by risk-based decision-making to inform commercial product design. Although the article is mostly focused on traditional small molecules, the principles described here can be adapted to include other types of molecular and biologic entities, including the newer molecular modalities that are rapidly gaining importance in the industry.