Most anticancer drugs are characterised by a narrow therapeutic window; hence, a small change in dose can lead to poor antitumour effects or an unacceptable degree of toxicity, which may result in dose reductions and even delays and a poor prognosis. Therefore, any exploration aimed at optimizing the dosage of drugs is worthwhile. Classically cytotoxic chemotherapy has been dosed by adjusting doses by BSA. Recently, this traditional method of calculating the dose of drugs has been questioned. Firstly, the deduction of the BSA formula and its application outside the phase I clinical trial are lack of reasonable basis. In addition,a number of studies have demonstrated that BSA dosing is associated with high pharmacokinetic variability and failed to reduce interpatient variability. It gives the false impression that we are practicing personalized medicine by using a patient-specific metric. According to the research, there is a close connection between body composition and the pharmacokinetics of anticancer agents which make the body composition as a prognostic factor of chemotherapy toxicity and outcome. With the rapid development of body composition analysis methods such as bioelectrical impedance analysis and computerized tomographic scanning, the research on drug dose calculation based on body composition analysis has become a hot issue in the interdisciplinary field. In this paper, we aim to provide an overview about the relationships among the body composition, the pharmacokinetics and toxicity of anticancer agents, and the current research on body composition analysis in the clinical transformation process of dose standardization of anticancer agents is reviewed.