The application of newly developed thermodynamic guidelines for drug development has yielded unprecedented results in the design and optimization of drug candidates against important diseases. By experimentally monitoring not only binding affinity but the thermodynamic forces that determine binding, enthalpy and entropy, it is possible to significantly accelerate the development process, as these forces reflect different types of drug-target interactions. A thermodynamic platform allows faster potency and selectivity optimization in conformity with existing rules for the design of drug-like molecules and oral bioavailability.