CHAPTER 16: Designing Polymeric Binders for Pharmaceutical Applications

The properties of polyvalent polymers to form supramolecular complexes with biological substrates offer many attractive therapeutic possibilities. Polymeric binders are macromolecules designed to exert a pharmacological effect by selectively interacting with exogenous or endogenous substrates. They can be employed to prevent the harmful effects of toxins, inhibit virus colonization or even trigger apoptosis of diseased cells. This chapter presents the fundamentals of developing polymeric binders as new drug entities. The basics of finding the right target, establishing structure–activity relationships and measuring efficacy are highlighted, with numerous examples of polymeric binders at different development stages, including commercialization. Orally administered scavengers represent the most advanced examples in clinical use. Their binding in the gastrointestinal tract results in either local or systemic therapeutic effects. Although they are designed to be non-absorbable, their low systemic exposure is not always devoid of side effects. The required approaches to confirm innocuousness of the macromolecules and the challenges encountered during the clinical phases are also presented.