This review focuses on trends in the macromolecular recognition of biologically significant molecules (e.g., drugs, amino acids, steroids, nucleotide bases, carbohydrates, etc.) via molecular imprinting methods. An extensive list of prior art including type of functional monomers and crosslinkers for each biomolecule imprinted polymer is presented. Representative samples of receptor-ligand dissociation constants and polymer capacities are presented as well as typical values that occur in classes of biological recognition systems. Imprinting technology has direct impact in enhanced drug loading of controlled-release carriers for the sustained release of therapeutic agents as well as robust biosensors for novel therapeutic and diagnostic devices. This review also discusses the future of designed recognition, configurational biomimesis within polymeric gels, and highlights recent efforts toward integrating imprinted polymers in controlled drug delivery systems and sensing devices. In particular, the application of imprinted polymers for sustained release, enhanced loading capacity, and enantioselective loading or release are discussed. This article also highlights the most important problems to be solved in the design of synthetic recognition-based networks for biological molecules.