Every drug development is a complex and long journey. Clinical pharmacology is an essential discipline in modern drug development. With its applications, computational modelling, and simulation techniques, it can significantly contribute to the efficiency in drug development today. In this perspective, we highlight why pharmacokinetics and pharmacodynamics are important, what developers need to consider in their clinical development programme, how modelling influences the development process, and discuss recent trends such as artificial intelligence and machine learning that have the potential to reshape future drug development.