Population pharmacokinetic and pharmacodynamic analysis is an important tool to support optimal treatment in clinical oncology. The population approach is suitable to explain variability between patients and to establish relationships between drug exposure and a relevant pharmacodynamic parameter. This can facilitate the selection of dosing schedules, the development of strategies for dose individualization and the application of therapeutic drug monitoring of anticancer agents. This review discusses the role of population pharmacokinetics and pharmacodynamics in clinical oncology to enhance the efficiency of drug development and to support the development of safe and effective dosing regimens for optimal treatment of cancer patients. An overview of published population studies of investigational anticancer agents and established treatment regimens is presented.