Polymers have been extensively utilized in the design of nanometer-sized delivery vehicles of chemotherapeutics for clinical cancer therapy. Polymeric nanoparticulate delivery vehicles, with chemotherapeutics being either conjugated or encapsulated, have been developed into a variety of different architectures, including polymer-drug conjugates with linear or branched polymers, micelles, and polymersomes. This review describes the progress that has been made in the field of polymeric nanomedicine that brings the science closer to clinical realization of nanopolymeric therapeutics for its application in cancer treatment.