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SUSAN GOODIN, PHARM.D., FCCP, BCOP, is Director, Division of Pharmaceutical Sciences, the Cancer Institute of New Jersey, and Associate Professor of Medicine, the University of Medicine and Dentistry of New Jersey-Robert Wood Johnson Medical School, 195 Little Albany Street, New Brunswick, NJ 08901 (goodin{at}umdnj.edu).

Purpose. The mechanisms of action and drug interactions of oral chemotherapeutic agents are reviewed. Summary. The mechanisms of action, indications, and potential for drug interactions vary for oral chemotherapy. Traditional oral chemotherapy agents cause damage to cancer cells by non-specifically interfering with cellular division. Many of the newer agents have novel targets on cancer cells preferentially, resulting in a different spectrum of toxicity. Since cancer patients are at high risk for drug interactions, usually because of age-related organ dysfunction and the need for concomitant drug therapy for comorbid conditions, understanding these agents and potential for interactions is imperative for all healthcare providers. Conclusion. Knowledge of the mechanisms and metabolic pathways for the oral chemotherapeutic agents allows the potential to predict possible drug interactions and response while minimizing the risk of adverse outcomes. Index terms: Antineoplastic agents; Drug administration routes; Drug interactions; Mechanism of action; Metabolism; Neoplasms; Pharmacokinetics; Site of action; Toxicity