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Tyrosine Kinase Inhibitors (TKIs) for Cancer


Generic NameBrand Name
bosutinibBosulif, Xalkori, Sprycel, Tarceva, Gleevec, Tykerb, Tasigna, Nexavar, Sutent
crizotinibBosulif, Xalkori, Sprycel, Tarceva, Gleevec, Tykerb, Tasigna, Nexavar, Sutent
dasatinibBosulif, Xalkori, Sprycel, Tarceva, Gleevec, Tykerb, Tasigna, Nexavar, Sutent
erlotinibBosulif, Xalkori, Sprycel, Tarceva, Gleevec, Tykerb, Tasigna, Nexavar, Sutent
imatinibBosulif, Xalkori, Sprycel, Tarceva, Gleevec, Tykerb, Tasigna, Nexavar, Sutent
lapatinibBosulif, Xalkori, Sprycel, Tarceva, Gleevec, Tykerb, Tasigna, Nexavar, Sutent
nilotinibBosulif, Xalkori, Sprycel, Tarceva, Gleevec, Tykerb, Tasigna, Nexavar, Sutent
sorafenibBosulif, Xalkori, Sprycel, Tarceva, Gleevec, Tykerb, Tasigna, Nexavar, Sutent
sunitinibBosulif, Xalkori, Sprycel, Tarceva, Gleevec, Tykerb, 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 many different cancers, such as leukemia and non-small cell lung cancer.

How Well It Works

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

Side Effects

All medicines have side effects. But many people don't feel the side effects, or they are able to deal with them. Ask your pharmacist about the side effects of each medicine you take. Side effects are also listed in the information that comes with your medicine.

Here are some important things to think about:

  • Usually the benefits of the medicine are more important than any minor side effects.
  • Side effects may go away after you take the medicine for a while.
  • If side effects still bother you and you wonder if you should keep taking the medicine, call your doctor. He or she may be able to lower your dose or change your medicine. Do not suddenly quit taking your medicine unless your doctor tells you to.

Callor other emergency services right away if you have:

  • Trouble breathing.
  • Swelling of your face, lips, tongue, or throat.

Call your doctor right away if you have:

  • Hives.
  • Shortness of breath or a new cough.
  • Signs of an infection, such as a fever or chills.
  • Tarry stools.
  • Skin problems, including rash and infections.
  • Eye pain or irritation.
  • Severe or ongoing nausea, vomiting, or diarrhea.
  • Depression or thoughts of suicide.

In rare cases, erlotinib can cause a serious lung problem called interstitial lung disease. Immediately report to your oncologist any shortness of breath or cough.

Taking dasatinib may cause pleural effusion. Dasatinib can also increase your risk for pulmonary arterial hypertension (PAH), a rare but serious heart problem.

Common side effects of these medicines include:

  • Nausea or vomiting. You may be able to reduce 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.

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

What To Think About

These medicines may cause serious blood, heart, lung, or liver problems, so your doctor will watch you closely and monitor your blood counts. You may also have tests to check your liver, heart, and lungs.

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

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

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

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

Skin rashes are often a problem for people taking these medicines. Try using a moisturizer several times a day. Seeing a dermatologist may help.

Taking medicine

Medicine is one of the many tools your doctor has to treat a health problem. Taking medicine as your doctor suggests will improve your health and may prevent future problems. If you don't take your medicines properly, you may be putting your health (and perhaps your life) at risk.

There are many reasons why people have trouble taking their medicine. But in most cases, there is something you can do. For suggestions on how to work around common problems, see the topic Taking Medicines as Prescribed.

Advice for women

Do not use this medicine if you are pregnant, breast-feeding, or planning to get pregnant. If you need to use this medicine, talk to your doctor about how you can prevent pregnancy.


Follow-up care is a key part of your treatment and safety. Be sure to make and go to all appointments, and call your doctor if you are having problems. It's also a good idea to know your test results and keep a list of the medicines you take.

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 ReviewerBrian Leber, MDCM, FRCPC - Hematology
Last RevisedDecember 14, 2012

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