The invention described herein provides biocompatible molecularly imprinted polymers (MIPs) that are non-toxic, water soluble, small molecular weight, and degradable in a living body. The MIPs are capable of binding to all or a portion of a specific target macromolecule associated with a disease located within the living body and they are derivatized for stealth for in vivo applications to avoid the reticuloendothelial system. The MIPs of the invention are functionalized to an amine or carboxyl group and are derivatized with an imaging and/or therapeutic agent for taking images of the disease and/or for providing therapy. The macromolecule can be selected from a group consisting of proteins, glycoproteins, lipoproteins, peptidoglycans, peptides, polypeptides, polynucleotides, and polysaccharides. The invention described herein also provides methods and kits wherein MIPs of the invention can be employed as targeted imaging and therapeutic agents.