Pharmacokinetic parameters of antineoplastic drugs are usually generated from concentration/time profiles obtained after multiple venipunctures. With limited-sampling models (LSM) this number can be reduced to between one and three timed plasma samples. LSMs may facilitate population pharmacokinetic/pharmacodynamic studies, which eventually may lead to a dosing strategy based on the characteristics of the individual patient. In this article, the development, validation and application of several LSMs reported in the literature are reviewed.