The development of polymeric materials as drug delivery systems has advanced from systems that rely on classical passive targeting to carriers that can sustain the precisely controlled release of payloads upon physicochemical triggers in desired microenvironment. Molecularly imprinted polymers (MIP), materials designed to capture specific molecules based on their molecular shape and charge distribution, are attractive candidates for fulfilling these purposes. In particular, drug-imprinted polymers coupled with active targeting mechanisms have been explored as potential drug delivery systems. In this review, we have curated important recent efforts in the development of drug-imprinted polymers in a variety of clinical applications, especially oncology and ophthalmology. MIP possesses properties that may complement the traditional delivery systems of these two disciplines, such as passive enhanced permeability and retention effect (EPR) in cancer tumors, and passive drug diffusion in delivering ophthalmic therapeutics. Furthermore, the prospects of MIP integration with the emerging gene therapies will be discussed.