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tyrosine kinase inhibitors

Tuesday 3 July 2007

TKIs; TKI; tyrosine-kinase inhibitor


Definition: A tyrosine kinase inhibitor (TKI) is a pharmaceutical drug that inhibits tyrosine kinases (TKs ). Tyrosine kinases are enzymes responsible for the activation of many proteins by signal transduction cascades. The proteins are activated by adding a phosphate group to the protein (phosphorylation), a step that TKIs inhibit. TKIs are typically used as anticancer drugs.


- imatinib
- gefitinib
- erlotinib
- sunitinib
- cabozantinib
- osimertinib


- TKIs Rx associated histological transformation of NSCLC to SCLC (risk 3-15%)

See also

- protein kinase inhibitors (PKIs )


- Krause DS, Van Etten RA. Tyrosine kinases as targets for cancer therapy. N Engl J Med 2005;353:172-187.

- Force T, Krause DS, Van Etten RA. Molecular mechanisms of cardiotoxicity of tyrosine kinase inhibition. Nat Rev Cancer. 2007 May;7(5):332-44. PMID: 17457301