Abstract: Alzheimer's disease (AD) is a common progressive multifarious neurodegenerative disease with a high prevalence, which brings huge burden to families and society. Since the mechanism of AD is still unclear, research and development of anti-AD drugs are facing big challenges with very little progress in searching for effective therapies and drugs. Pharmaceutical companies and research institutions worldwide are highly concerned with AD drug development, especially drugs in clinical phase. Herein, this paper reviewed the current progress in the clinical development of small-molecule anti-AD drugs with different targets and mechanisms, including reducing amyloid-β protein, balancing neurofibrillary tangle, regulating neurotransmission disorder, balancing calcium ion, countering oxidative stress, suppressing neuroinflammation, and regulating glucose metabolism disorder.