Small-molecule kinase inhibitors: an analysis of FDA-approved drugs

Peng Wu, Thomas Eiland Nielsen, Mads Hartvig Clausen

Research output: Contribution to journalJournal articleResearchpeer-review


Small-molecule kinase inhibitors (SMKIs), 28 of which are approved by the US Food and Drug Administration (FDA), have been actively pursued as promising targeted therapeutics. Here, we assess the key structural and physicochemical properties, target selectivity and mechanism of function, and therapeutic indications of these approved inhibitors. Our analysis showed that >30% of approved SMKIs have a molecule weight (MW) exceeding 500 and all have a total ring count of between three and five. The assumption that type II inhibitors tend to be more selective than type I inhibitors has been proved to be unreliable. Although previous SMKI research was concentrated on tyrosine kinase inhibitors for cancer treatment, recent progress indicates diversification of SMKI research in terms of new targets, mechanistic types, and therapeutic indications.
Original languageEnglish
JournalDrug Discovery Today
Issue number1
Pages (from-to)5–10
Number of pages6
Publication statusPublished - 2016


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