The broad scope of malignancies treated in interventional oncology is mirrored by the breadth of oncotherapeutics, drugs used to treat cancer. Many of these treatments are administered endovascularly, though a group of therapies can be delivered percutaneously. Perhaps the best taxonomy of oncotherapeutics is based on their biological inactivity or activity and the mechanism by which they interact with treated and targeted tissues. As the fields of interventional oncology and oncotherapeutics continue to grow and expand, this framework may provide a more organized approach in helping distinguish and select the best therapy for patients.