The steady increase in the use of oral anticancer drugs in modern oncology has created a paradigm shift, challenging traditional attitudes towards cancer care and requiring new concepts of organization of oncology services. Important issues are the prolonged treatment period, management of toxicity, treatment adherence, reimbursement conditions and patient and family education. Although most patients generally prefer oral therapy over intravenous treatment for reasons of convenience, the daily use of oral anticancer drugs can be a challenging commitment for many patients. Reports on adherence and persistence among patients with cancer show that adherence ranges from 16% to 100%, depending on the type of therapy and the measurement/definition of adherence. Apart from demographic, disease and therapy related factors, the determinants that mostly influence (non-)adherence are the satisfaction with care activities performed at the initiation of the drug treatment, and the perceived necessity of treatment. Therefore, patient education addressing these issues is considered the cornerstone of successful oral anticancer treatment. Studies examining the role of different health care providers in the pharmacotherapeutic care of patients with cancer, treated with oral anti-cancer drugs, support the need for a multidisciplinary approach to achieve a maximum benefit for the individual patient and consequently for the whole health system. Limiting adverse events and developing appropriate supportive care are only some aspects that need to be considered in this.