Drug development for neurodegenerative diseases such as Alzheimer's disease (AD) is a challenge, not only due to the cellular molecular mechanisms involved, but also because of the inherent difficulty of most molecules to cross the blood-brain-barrier (BBB). A promising approach to overcome these drawbacks is developing fluorinated molecules and supramolecular assemblies. This review focuses on the therapeutic potential of new fluorinated molecules, developed as active and selective agents for AD, to meet the desired pharmacokinetic/pharmacodynamic properties and BBB targeting. The methods to fluorinate organic molecules and a brief characterization of the mechanisms of AD progression and therapeutic approaches are described. The paradigm of cell biology knowledge and fluorine biochemistry such as, organofluorine inhibitors of amyloid fibrilogenesis, is highlighted.