Abstract: Alzheimer’s disease (AD) is a neurodegenerative disorder involving multiple pathological processes, clinically characterized by memory loss and cognitive impairment. The pathological processes of AD are complex, and the etiology remains unclear. Currently, there are various hypotheses including β-amyloid (Aβ) deposition, tau protein hyperphosphorylation, neuroinflammation, and synaptic loss, upon which researchers base their drug development efforts. Prior to 2021, drugs approved by the U.S. Food and Drug Administration (FDA) had targeted neurotransmitter modulation, but their efficacy was limited. In recent years, the approval of two anti-Aβ monoclonal antibody drugs has brought some clinical benefits to patients, yet they have not fully met clinical needs, which had highlighted the urgent necessity for exploration of new mechanisms and targets in AD drug development. Presently, research on novel mechanisms and targets for AD drug development focuses primarily on several directions: anti-Aβ drugs, anti-Tau protein drugs, anti-neuroinflammation immunotherapies, mitochondrial function-improving drugs, neurogenesis-promoting drugs, and synapse-protective drugs. This paper provides an overview of AD drugs entering clinical trials in the past decade in these directions, details some representative drugs, and concludes with prospects, integrating findings from our research group.