Tyrosine kinase inhibitor

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Tyrosine Kinase Inhibitor

Tyrosine kinase inhibitors (TKIs) are a type of pharmacological inhibitor that specifically block the action of tyrosine kinase. Pronounced as "tie-ROW-seen KY-nase in-HIB-it-or", the term originates from the Greek words "tyros" meaning cheese (where the amino acid was first discovered), "kinase" from "kinesis" meaning movement, and "inhibitor" from the Latin "inhibere" meaning to restrain.

Function

Tyrosine kinase inhibitors function by blocking the phosphorylation of tyrosine residues in proteins, thereby inhibiting the activation of signal transduction pathways that are crucial for the proliferation and survival of certain types of cancer cells.

Types

There are two main types of tyrosine kinase inhibitors: small molecule TKIs and monoclonal antibody TKIs. Small molecule TKIs, such as imatinib, gefitinib, and erlotinib, are able to penetrate the cell membrane and inhibit the activity of intracellular tyrosine kinases. Monoclonal antibody TKIs, on the other hand, are large proteins that cannot penetrate the cell membrane and therefore inhibit the activity of extracellular tyrosine kinases.

Use in Medicine

Tyrosine kinase inhibitors are used in the treatment of various types of cancers, including chronic myeloid leukemia (CML), non-small cell lung cancer (NSCLC), and breast cancer. They work by targeting and inhibiting specific tyrosine kinases that are overactive in certain cancer cells.

Side Effects

Like all medications, tyrosine kinase inhibitors can cause side effects. These may include nausea, vomiting, diarrhea, and skin rash. More serious side effects can include heart failure, liver toxicity, and lung toxicity.

Future Research

Future research on tyrosine kinase inhibitors is focused on developing new inhibitors that are more selective and have fewer side effects, as well as on finding new uses for these drugs in the treatment of other diseases.

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