Objectives: To review published literature to determine what is known about adherence to oral antineoplastic agents in children with cancer, to identify adherence-related challenges, and to examine the implications of these challenges for clinical practice. Data Sources: Published literature identified through the MEDLINE, CINAHL, and PsycINFO databases. Conclusion: Oral antineoplastic agents are frequently used in childhood cancer treatment; supportive care regimens for children with cancer also rely heavily on the administration of oral medications. Adherence in pediatric oncology is a complex process involving both parent and child, and requires knowledge and understanding of proper and safe home medication administration in the context of multiple developmental and behavioral concerns that may change over time. Implications for Nursing Practice: Nurses play an important role in adherence by providing patient and family education and psychosocial support targeted to the child's diagnosis, developmental stage, and specifics of the child's treatment regimen. © 2011 Elsevier Inc.