Despite the considerable effort made in the past decades, multiple aspects of cancer management remain a challenge for the scientific community. The severe toxicity and poor bioavailability of conventional chemotherapeutics, and the multidrug resistance have turned the attention of researchers towards the quest of drug carriers engineered to offer an efficient, localized, temporized, and doze-controlled delivery of antitumor agents of proven clinical value. Molecular imprinting of chemotherapeutics is very appealing in the design of drug delivery systems since the specific and selective binding sites created within the polymeric matrix turn these complex structures into value-added carriers with tunable features, notably high loading capacity, and a good control of payload release. Our work aims to summarize the present state-of-the art of molecularly imprinted polymer-based drug delivery systems developed for anticancer therapy, with emphasis on the particularities of the chemotherapeutics' release and with a critical assessment of the current challenges and future perspectives of these unique drug carriers.Polymers 2019, 11, 2085 2 of 33 normal and abnormal cells, the severe toxicity and poor bioavailability of conventional drugs, and the multidrug resistance are issues that still need to be addressed by the scientific community.Polymers 2019, 11, x FOR PEER REVIEW 2 of 34 of both normal and abnormal cells, the severe toxicity and poor bioavailability of conventional drugs, and the multidrug resistance are issues that still need to be addressed by the scientific community.