An update of new small-molecule anticancer drugs approved from 2015 to 2020.

A high incidence of cancer has given rise to the development of more anti-tumor drugs. From 2015 to 2020, fifty-six new small-molecule anticancer drugs, divided into ten categories according to their anti-tumor target activities, have been approved. These include TKIs (30 drugs), MAPK inhibitors (3 drugs), CDK inhibitors (3 drugs), PARP inhibitors (3 drugs), PI3K inhibitors (3 drugs), SMO receptor antagonists (2 drugs), AR antagonists (2 drugs), SSTR inhibitors (2 drugs), IDH inhibitors (2 drugs) and others (6 drugs). Among them, PTK inhibitors (30/56) have led to a paradigm shift in cancer treatment with less toxicity and more potency. Each of their structures, approval statuses, applications, SAR analyses, and original research synthesis routes have been summarized, giving us a more comprehensive map for further efforts to design more specific targeted agents for reducing cancer in the future. We believe this review will help further research of potential antitumor agents in clinical usage.