Brain iron homeostasis plays an important role in maintaining normal brain development and controlling cellular oxidative stress. Accumulating studies have shown that the imbalance of brain iron homeostasis is closely involved in the pathogenesis of Alzheimer’s disease (AD). Here, we reviewed the research progress of the role of iron metabolism in the pathogenesis of AD, particularly focusing on the alterations of several key molecules responsible for cellular iron uptake, storage, release and regulation, and discussed potential therapeutic strategies for AD against the elevated brain iron and altered cellular iron metabolic pathways. This review may contribute to further studies focusing on the role of iron metabolism and related molecules in AD pathogenesis, and provide new insight for the development of AD drugs targeting these molecules.