Small molecule kinase inhibitor drugs (1995-2021): Medical indication, pharmacology and synthesis

Cecilia Ayala Aguilera, Alvaro Lorente Macias, Dan Baillache, Stephen Croke, Asier Unciti-Broceta*

*Corresponding author for this work

Research output: Contribution to journalReview articlepeer-review

Abstract / Description of output

The central role of dysregulated kinase activity in the etiology of progressive disorders, including cancer, has fostered incremental efforts on drug discovery programs over the last 40 years. As a result, kinase inhibitors are today one of the most important classes of drugs. The FDA approved 72 small molecule kinase inhibitor drugs until Aug 2021, and additional inhibitors were approved
by other regulatory agencies during that time. To complement the published literature on clinical kinase inhibitors, we have prepared a review that recaps this large dataset into an accessible format for the medicinal chemistry community. Along with the therapeutic and pharmacological properties of each kinase inhibitor approved across the world until 2020, we provide the synthesis
routes originally used during the discovery phase, many of which were only available in patent applications. In the last section, we also provide an update on kinase inhibitor drugs approved in
Original languageEnglish
Pages (from-to)1047-1131
Number of pages85
JournalJournal of Medicinal Chemistry
Issue number2
Early online date8 Oct 2021
Publication statusE-pub ahead of print - 8 Oct 2021


Dive into the research topics of 'Small molecule kinase inhibitor drugs (1995-2021): Medical indication, pharmacology and synthesis'. Together they form a unique fingerprint.

Cite this