Targeted Therapy

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Types of targeted therapy used today

Today many different types of targeted therapies are used to treat cancer. Looking at examples helps a person understand how these drugs work. A few of the more commonly used targeted therapies are listed here, but this is not a complete list. There are many different targeted therapies in use and new ones are coming out all the time.

There are 2 main types of targeted therapy drugs:

  • Antibody drugs are man-made versions of immune system proteins (called antibodies) that have been designed to attack certain targets on cancer cells. (The body normally makes antibodies to fight harmful invaders like germs.)
  • Small-molecule drugs are not antibodies. Since antibodies are large molecules, this other type of drug is called a “small-molecule” targeted therapy drug.

Some targeted therapy drugs

There are many different targeted therapy drugs. Here are a few examples:

Gleevec® (imatinib mesylate)

This is one of the first targeted therapy drugs ever used to treat cancer. It’s used to treat gastrointestinal (gas-tro-in-TEST-uh-nul) stromal tumor (or GIST, a rare cancer of the gastrointestinal tract) and certain kinds of leukemia. Imatinib is a tyrosine kinase inhibitor that targets abnormal proteins, or enzymes, that form on and inside cancer cells and promote uncontrolled growth. Blocking these enzymes inhibits cancer cell growth.

Iressa® (gefitinib)

Gefitinib is used to treat advanced non-small cell lung cancer. This drug targets the epidermal growth factor receptor (EGFR). These receptors are found on the surface of many normal cells, but certain cancer cells have many more of them. EGFR takes in the signal telling the cell to grow and divide. When gefitinib blocks this signal, it can slow or stop cell growth.

Sutent® (sunitinib)

This drug is used to treat advanced kidney cancer and some gastrointestinal stromal tumors, also called GIST. It’s considered a multi-targeted kinase inhibitor because it’s a type of vascular endothelial (vas-ku-lur en-doe-THEE-lee-uhl) growth factor (VEGF) receptor inhibitor, an angiogenesis inhibitor, and it blocks an enzyme called tyrosine kinase. By doing all of this it slows cancer growth and keeps tumors from making their own blood vessels to help them grow and spread.

Velcade® (bortezomib)

This enzyme inhibitor may be used to treat multiple myeloma that does not respond to other treatments. Bortezomib is a proteasome inhibitor. A proteasome is a complex of enzymes that helps destroy proteins that the cell no longer needs. Some of these proteins help to regulate cell function and growth. Bortezomib stops the proteasome from breaking down these proteins, which in turn causes the cancer cells to die.

Other drugs that may be called targeted therapies

There are other cancer treatments that can be included in the group of drugs called targeted therapies. Some examples of these are:

Monoclonal (ma-nuh-KLO-nuhl) antibodies, such as

Immunomodulating (im-yuh-no-MOD-you-late-ing) drugs, such as

Cytokines (sy-toe-kines) such as

The prostate cancer vaccine, Provenge® (sipuleucel-T)

The targeted therapies listed above are often grouped as immunotherapies, or treatments that work with your immune system to fight cancer. But some of them act more like targeted therapy drugs. For example, bevacizumab acts as an angiogenesis inhibitor, and cetuximab and trastuzumab work like enzyme inhibitors. You can learn more about these drugs in our document called Immunotherapy.


Last Medical Review: 07/12/2013
Last Revised: 07/12/2013