Tyrosine Kinase Inhibitors (TKIs)

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Tyrosine Kinase Inhibitors (TKIs)


Generic NameBrand Name

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 chronic myelogenous leukemia (CML).

Side Effects

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

  • Decreased white blood cell counts, which may lead to increased infections.
  • Decreased platelet counts, which may lead to bleeding in the digestive tract, causing tarry stools.
  • Nausea or vomiting. You may be able to decrease these side effects by taking your medicine with a meal and a full glass of water.
  • Diarrhea.
  • Heartburn.
  • Headache.
  • Muscle cramps.
  • Fluid retention and swelling, especially around the eyes.
  • Rash.

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) (What is a PDF document?) to help you understand this medication.


By Healthwise Staff
Primary Medical Reviewer Kathleen Romito, MD - Family Medicine
Primary Medical Reviewer Anne C. Poinier, MD - Internal Medicine
Specialist Medical Reviewer Brian Leber, MDCM, FRCPC - Hematology
Last Revised February 9, 2011

This information does not replace the advice of a doctor. Healthwise, Incorporated disclaims any warranty or liability for your use of this information.