Tyrosine kinase inhibitor

Tyrosine kinase inhibitors (TKIs) are pharmaceutical drugs that inhibit tyrosine kinases. 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.

Mechanism of action

TKIs act on tyrosine kinases, enzymes that, by transferring a phosphate group to a protein, can modify the function and activity of the latter. There are two types of tyrosine kinases: receptor tyrosine kinases, which are associated with cell membrane receptors, and non-receptor tyrosine kinases, which are located in the cytoplasm. TKIs can act at different levels of the tyrosine kinase pathway, and their action can be selective for one or more tyrosine kinases.

Uses

TKIs are used in the treatment of cancer and inflammation. They have been shown to be effective in treating chronic myeloid leukemia (CML), gastrointestinal stromal tumor (GIST), and several other types of cancer. TKIs are also used in the treatment of rheumatoid arthritis and other inflammatory diseases.

Side effects

The most common side effects of TKIs include nausea, vomiting, diarrhea, and rash. More serious side effects can include liver damage, heart failure, and lung disease.

Examples

Examples of TKIs include imatinib, erlotinib, gefitinib, sunitinib, and lapatinib.

See also

• Protein kinase inhibitor
• Signal transduction
• Phosphorylation

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