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Pharmacological anticancer therapy in elderly people has to account for pharmacokinetic aspects in view of age-related changes in organ function and disease-related alterations. Age-related changes in organ function might still be physiological and have to be discriminated from concomitant diseases and their pharmacotherapy. Although efficacy is retained with pharmacological anticancer therapies in elderly patients, plasma drug concentrations and the incidence of adverse reactions often increase. Thus, altered organ function in elderly will be reviewed with respect to clinically relevant outcomes. Furthermore, possible consequences of therapeutic drug monitoring will be discussed focusing on novel targeted therapies with small molecules. Examples of therapeutic drug monitoring during targeted therapies may represent an easy tool to overcome the individual pharmacokinetic situation of elderly cancer patients and may contribute to enhanced safety, when implemented in clinical routine.