Although numerous anticancer drugs are widely used in the clinic, many questions remain about pharmacokinetics, biodistribution, toxicities, and efficacy. Positron emission tomography (PET) using radiolabeled drugs is a promising method to further understand the clinical behavior of anticancer agents. In addition, it may contribute to better guided treatment planning in individual patients with cancer. Among the available anticancer drugs, considerable experience has been gained with radiolabeling taxanes. At present, two radiolabeled taxanes, paclitaxel and docetaxel, are available as PET tracers.