Drug interactions are an ongoing concern in treatment of cancer, especially when cytotoxic drugs are being used. However, the clinical relevance of these interactions is not always investigated. Drug interactions can be pharmaceutical, pharmacokinetic, or pharmacodynamic. They can also be wanted (eg, use of ciclosporin to enhance the oral bioavailability of paclitaxel); unwanted (eg, combination of the antiviral agent sorivudine and oral fluorouracil analogues can lead to fatal complications); between cytotoxic drugs, cytotoxic drugs and non-cytotoxic drugs; or with pharmaceutical vehicles. Potential interactions between anticancer drugs and over-the-counter or alternative medicines and herbs should not be underestimated. More attention should be given to the recognition of potential drug interactions in the preclinical and early clinical development phase of a new anticancer drug. Here, we provide a comprehensive overview of drug interactions, with selected examples.