Alzheimer’s disease (AD) is the most common form of dementia, and the prevalence of this currently untreatable disease is expected to rise in step with increased global life expectancy. AD is a multifaceted disorder commonly characterized by extracellular amyloid–beta (Aβ) aggregates, oxidative stress, metal ion dysregulation, and intracellular neurofibrillary tangles. This review will focus on medicinal inorganic chemistry strategies to target AD, with a focus on the Aβ peptide and its relation to metal ion dysregulation and oxidative stress. Multifunctional compounds designed to target multiple disease processes have emerged as promising therapeutic options, and recent reports detailing multifunctional metal-binding compounds, as well as discrete metal complexes, will be discussed.