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tyrosine kinase inhibitors
Tuesday 3 July 2007
TKIs; TKI; tyrosine-kinase inhibitor
| WKPD |
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.
Examples
imatinib
gefitinib
erlotinib
sunitinib
cabozantinib
osimertinib
Pathology
TKIs Rx associated histological transformation of NSCLC to SCLC (risk 3-15%)
See also
protein kinase inhibitors (PKIs )
EGFR-TKIs
References
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
