Compelling evidence indicates that a key pathological event in Alzheimer's disease is the misfolding and aggregation of normal soluble amyloid-beta peptide into beta-sheet-rich oligomeric structures which have a neurotoxic activity and ability to form insoluble amyloid deposits that accumulate in the brain. beta-sheet breakers constitute a new class of drugs that are designed to specifically bind amyloid-beta peptide blocking and/or reversing the misfolding process. In this article we review this approach and summarize the data supporting the view that beta-sheet breakers could be serious candidates to combat this devastating disease.