Advances of small molecule targeting of kinases.
Level 5 - mechanism / opinion, no new human data
Narrative review with no systematic search methodology or original experimental data.
PubMed 28732278 · doi:10.1016/j.cbpa.2017.06.015
What was done
This narrative review summarizes the landscape of small-molecule protein kinase inhibitors (PKIs) approved for clinical use since 1995, outlining the scope of kinase targets, cancer indications, challenges, and emerging strategies based on published literature and regulatory data.
What was found
Almost three dozen PKIs have gained approval since 1995, mostly for cancer. Out of over 100 cancer types cataloged by the NCI, approved PKIs cover only 14. Furthermore, out of more than 500 protein kinases encoded by the human genome, only 22 are targeted by approved PKIs.
Why it matters
The paper outlines the extent to which the human kinome remains untargeted by approved therapeutics, highlighting substantial room for future drug development.
Limits
This is a brief narrative review without a systematic search protocol, meta-analysis, or primary clinical trial data, and it reports only high-level descriptive counts.
Cited by
- supports There are over 100 distinct types of cancer.