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Tyrosine Kinase Inhibitors (TKIs)


Generic NameBrand Name
dasatinibSprycel, Gleevec, Tasigna, Nexavar, Sutent
imatinibSprycel, Gleevec, Tasigna, Nexavar, Sutent
nilotinibSprycel, Gleevec, Tasigna, Nexavar, Sutent
sorafenibSprycel, Gleevec, Tasigna, Nexavar, Sutent
sunitinibSprycel, Gleevec, Tasigna, Nexavar, Sutent

A tyrosine kinase inhibitor (say "TY-ruh-seen KY-nays in-HIH-bih-ter") is used in cancer treatment as targeted therapy.

How It Works

Tyrosine kinase inhibitors (TKIs) are medicines that block signals that tell a cell to grow and divide. This can slow or stop cancer cells from growing. In some cases it can cause the cells to die.

Why It Is Used

Tyrosine kinase inhibitors (TKIs) are medicines used to treat cancers such as chronic myelogenous leukemia (CML) and some kinds of acute lymphoblastic leukemia (ALL).

How Well It Works

Tyrosine kinase inhibitors are effective medicines for the treatment of some cancers, such as chronic myelogenous leukemia (CML).

Side Effects

Side effects of tyrosine kinase inhibitors are generally mild and can include:

But some TKIs, such as sunitinib, may cause serious liver problems, including liver failure.

Taking dasatinib may increase your risk for pulmonary arterial hypertension (PAH), a rare but serious heart problem.

Tyrosine kinase inhibitors may cause depression in some people. If you have symptoms of depression or thoughts of suicide while you are taking it, talk to your doctor right away.

See Drug Reference for a full list of side effects. (Drug Reference is not available in all systems.)

What To Think About

Each of the TKIs have specific ways they need to be taken, so talk with your doctor about how to take your medicine.

If imatinib or dasatinib does not work for you, your doctor may treat you with nilotinib.

Tyrosine kinase inhibitors should be used only under the supervision of a medical oncologist or hematologist. He or she will monitor your blood counts regularly.

You may not be able to become pregnant or father a child after taking this drug. Talk about this with your doctor before starting treatment.

Tyrosine kinase inhibitors can cause birth defects. Do not use this drug if you are pregnant or wish to become pregnant or to father a child while you are taking it. Do not breast-feed while you are taking this drug.

These medicines can interact with many other drugs. Be sure that your doctor knows all the prescription and over-the-counter drugs you are taking.

If your tyrosine kinase inhibitor becomes less effective over time, your doctor may increase your dose, prescribe it along with another drug, or try other drugs to treat your cancer.

Do not take tyrosine kinase inhibitors with grapefruit juice. Grapefruit juice can make these medicines useless.

Complete the new medication information form (PDF)Click here to view a form.(What is a PDF document?) to help you understand this medication.


ByHealthwise Staff
Primary Medical ReviewerE. Gregory Thompson, MD - Internal Medicine
Specialist Medical ReviewerMatthew I. Kim, MD - Endocrinology
Last RevisedNovember 8, 2011

eMedicineHealth Medical Reference from Healthwise

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