 Targeted therapeutic drugs have become mainstream cancer treatments due to their advantages in efficacy and safety compared with traditional chemotherapy drugs. Despite great progress, small molecule targeted anti-cancer drugs still face challenges such as low response rate and drug resistance. A comprehensive review of these drugs according to target classification was conducted, presenting approved drugs and important drug candidates in clinical trials for each target, discussing current challenges, and providing insights and perspectives for the research and development of anti-cancer drugs. This article was authored by Lei Zhong, Yue Shanli, Liang Xiong, and others.