Recent progress in cancer treatment has increased the use of oral antineoplastic agents. It is now estimated that at least 25% of the existing antineoplastic agents are planned to be used as oral agents and this mode of administration is likely to increase in the coming years. The use of oral anti- neoplastic agents affects many aspects of cancer treatment, and despite advantages, it also poses challenges to health care professionals and patients, many of which refer to the adherence and safety. Low patient adherence demonstrates the need for better management and monitoring of patients on oral antineoplastic agents. Patient education is essential to maintain adherence to oral antineoplastic therapy, promoting a better understanding of the patient treatment regimen, treatment goals and potential side-effects, patient safety and implementation of self-care measurement. This article discusses the above-mentioned challenges, as well as the possibilities of patient and family education to improve adherence, outcomes of treatment and quality of life, and offers recommendations for practice and further research.