Kinase Inhibitors in Clinical Development – 2021

First cancer targeting tyrosine kinase inhibitor imatinib was approved to enter the market by the US Food and Drug Administration (FDA) in 2001, since then an increasing number of small-molecule targeted drugs have been developed and approved for the treatment of cancer. By the end of June 2021, worldwide 96 small-molecule targeted antitumor drugs have been approved by the US FDA and the National Medical Products Administration (NMPA) of China, which majorly includes 73 kinase Inhibitors, beside other including Epigenetic Inhibitors, inhibitors of BCL-2, hedgehog pathway, proteasome, and PARP.

Beside Cancer, nearly 14 other disease targeting small molecule Kinase Inhibitors were also approved worldwide during the same time period, thus making total tally to 87 approved kinase Inhibitors.

Despite great progress, small-molecule targeted anti-cancer drugs still face many challenges, such as a low response rate and drug resistance. This article carefully summarizes the approved cancer kinases inhibitors.