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Targeted therapy is a type of medication that blocks the growth of cancer cells by interfering with specific targeted molecules involved in tumor growth and progression, rather than by simply interfering with rapidly dividing cells (eg. with traditional chemotherapy). Because scientists often call these molecules "molecular targets," targeted cancer therapies are sometimes called "molecularly targeted drugs," "molecularly targeted therapies," or other similar names. Targeted cancer therapies may be more effective than current treatments, including chemotherapy and radiotherapy, and less harmful to normal cells.

Many oncologists believe that targeted therapies are the chemotherapy of the future. As solid tumor cancer continues to be viewed as a chronic condition, methods for long-term treatment, with less side-effects, continue to be investigated.

How targeted cancer therapies work

Targeted cancer therapies interfere with cancer cell division (proliferation) and spread in different ways. Many of these therapies focus on proteins that are involved in cell signaling pathways, which form a complex communication system that governs basic cellular functions and activities, such as cell division, cell movement, how a cell responds to specific external stimuli, and even cell death. By blocking signals that tell cancer cells to grow and divide uncontrollably, targeted cancer therapies can help stop cancer progression and may induce cancer cell death through a process known as apoptosis. Other targeted therapies can cause cancer cell death directly, by specifically inducing apoptosis, or indirectly, by stimulating the immune system to recognize and destroy cancer cells and/or by delivering toxic substances to them.

The development of targeted therapies, therefore, requires the identification of good targets - that is, targets that are known to play a key role in cancer cell growth and survival.

Types of targeted therapies

The main categories of targeted therapy are small molecules and monoclonal antibodies. Small-molecule drugs are typically able to diffuse into cells and can act on targets that are found inside the cell. Most monoclonal antibodies usually cannot penetrate the cell`s plasma membrane and are directed against targets that are outside cells or on the cell surface.

The first molecular target for targeted cancer therapy was the cellular receptor for the female sex hormone estrogen, which many breast cancers require for growth. Drugs called selective estrogen receptor modulators (SERMs), including tamoxifen and toremifene (Fareston) have been approved by the FDA for the treatment of ER-positive breast cancer.

Examples of some other FDA approved targeted therapies

  • Imatinib mesylate (Gleevec) to treat gastrointestinal stromal tumor (a rare cancer of the gastrointestinal tract) and certain kinds of leukemia.
  • Dasatinib (Sprycel) to treat some patients with chronic myeloid leukemia (CML) and acute lymphoblastic leukemia (ALL).
  • Nilotinib (Tasigna) to treat some patients with CML.
  • Trastuzumab (Herceptin) for the treatment of certain types of breast cancer.
  • Gefitinib (Iressa) to treat patients with advanced non-small cell lung cancer.
  • Erlotinib (Tarceva) to treat metastatic non-small cell lung cancer and pancreatic cancer that cannot be removed by surgery or has metastasized.
  • Cetuximab (Erbitux) for treating some patients with squamous cell carcinoma of the head and neck or colorectal cancer.
  • Lapatinib (Tykerb) for the treatment of certain types of advanced or metastatic breast cancer.
  • Panitumumab (Vectibix) to treat some patients with metastatic colon cancer.
  • Temsirolimus (Torisel) to treat patients with advanced renal cell carcinoma.
  • Bortezomib (Velcade) to treat some patients with multiple myeloma.
  • Bevacizumab (Avastin) for the treatment of glioblastoma, and for some patients with non-small cell lung cancer, metastatic breast cancer, and metastatic colorectal cancer.
  • Sorafenib (Nexavar) for the treatment of advanced renal cell carcinoma and some cases of hepatocellular carcinoma.
  • Sunitinib (Sutent) for the treatment of patients with metastatic renal cell carcinoma or gastrointestinal stromal tumor that is not responding to imatinib.
  • Rituximab (Rituxan) to treat certain types of B-cell non-Hodgkin lymphoma.
  • Alemtuzumab (Campath) to treat patients with B-cell chronic lymphocytic leukemia.
  • Gemtuzumab ozogamicin (Mylotarg) to treat some patients with acute myeloid leukemia (AML).
  • Tositumomab and 131I-tositumomab (Bexxar) to treat certain types of B-cell non-Hodgkin lymphoma.
  • Ibritumomab tiuxetan (Zevalin) to treat some patients with B-cell non-Hodgkin lymphoma.

Impact of targeted therapies on cancer treatment

Targeted cancer therapies give doctors a better way to tailor cancer treatment, especially when a target is present in some but not all tumors of a particular type. Eventually, treatments may be individualized based on the unique set of molecular targets produced by the patient?s tumor. Targeted cancer therapies also hold the promise of being more selective for cancer cells than normal cells, thus harming fewer normal cells, reducing side effects, and improving quality of life.

Nevertheless, targeted therapies have some limitations. Chief among these is the potential for cells to develop resistance to them.

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