Malignant tumors have become a significant public health problem that severely threatens human health. Drug-targeting therapy is essential for tumor therapy, along with surgery and radiotherapy. Of the 378 novel drugs approved over the past five years, those for oncological therapy remains at the top (25%). These drugs are used to treat patients with various cancers by acting on corresponding targets, such as EGFR, JAK, BTK, IDH, and FLT3. This review examines anti-tumor agents approved between 2016 and 2020, classifying them according to indication (such as lung cancer, leukemia, breast cancer, and myeloma). These drugs are reviewed according to their route of administration, first-in-class designation, approval dates, and expedited review categories. Furthermore, this paper summarizes the targets and modes of action of the approved anti-tumor drugs while systematically discussing their synthetic routes for medicinal chemistry or industrial use, which will benefit next-generation drug discovery.

恶性肿瘤已成为严重威胁人类健康的重大公共卫生问题。药物靶向治疗对于肿瘤治疗以及手术和放疗都是必不可少的。在过去五年批准的 378 种新药中，用于肿瘤治疗的药物仍然位居榜首（25%）。这些药物通过作用于相应的靶标，如EGFR、JAK、BTK、IDH和FLT3，用于治疗各种癌症患者。本综述审查了 2016 年至 2020 年间批准的抗肿瘤药物，根据适应症（如肺癌、白血病、乳腺癌和骨髓瘤）对它们进行分类。这些药物根据其给药途径、一流名称、批准日期和快速审查类别进行审查。此外，