The dose of anticancer drugs is currently adjusted to the patient body surface area, although patients have different abilities to clear anticancer drugs. The dose adjustment to physiological functions permits major toxic accidents to be avoided. The adjustment to tumour drug content is considered, but for ethical or technical reasons, it cannot be used routinely The best criterion for the dose adjustment seems to be drug plasma concentration. The relationship between plasma concentration and efficacy may not be excellent, since it depends on the presence of resistant cells and on the blood flow through the tumour. A relationship between plasma concentration and/or the area under the curve (AUC) with toxicity has been reported with all major anticancer drugs. Different methods of dose adjustment to the drug plasma concentration are reported. In conclusion, dose adjustment to the drug plasma concentration or to the AUC can improve the chemotherapy efficacy, while reducing toxicity.