Targeted Therapy Drugs for Colorectal Cancer

As researchers have learned more about the gene and protein changes in cells that cause colorectal cancer, they have developed newer drugs to specifically target these changes. Targeted therapy drugs work differently from standard chemotherapy (chemo) drugs. They sometimes work when standard chemo drugs don’t, and they often have different (and less severe) side effects. They can be used either along with chemo or by themselves if chemo is no longer working.

Drugs that target blood vessel formation (VEGF)

Vascular endothelial growth factor (VEGF) is a protein that helps tumors form new blood vessels (a process known as angiogenesis) to get nutrients they need to grow. Drugs that stop VEGF from working can be used to treat some colon or rectal cancers. These include:

  • Bevacizumab (Avastin)
  • Ramucirumab (Cyramza)
  • Ziv-aflibercept (Zaltrap)

These drugs are given as infusions into your vein (IV) every 2 or 3 weeks, in most cases along with chemotherapy. When combined with chemo, these drugs can often help people with advanced colon or rectal cancers live longer.

Possible side effects of drugs that target VEGF

Common side effects of these drugs include:

  • High blood pressure
  • Extreme tiredness (fatigue)
  • Bleeding
  • Low white blood cell counts (with increased risk of infections)
  • Headaches
  • Mouth sores
  • Loss of appetite
  • Diarrhea

Rare but possibly serious side effects include blood clots, severe bleeding, holes forming in the colon (called perforations), heart problems, kidney problems, and slow wound healing. If a hole forms in the colon it can lead to severe infection and surgery may be needed to fix it.

Another rare but serious side effect of these drugs is an allergic reaction during the infusion, which could cause problems with breathing and low blood pressure.

Drugs that target cells with EGFR changes

Epidermal growth factor receptor (EGFR) is a protein that helps cancer cells grow. There's often a lot of it on the surface of cancer cells. Drugs that target EGFR can be used to treat some advanced colon or rectal cancers. These include:

  • Cetuximab (Erbitux)
  • Panitumumab (Vectibix)

Both of these drugs are given by IV infusion, either once a week or every other week.

These drugs don't work in colorectal cancers that have mutations (defects) in the KRAS, NRAS or BRAF gene. Doctors now commonly test the tumor for these gene changes before treatment, and only use these drugs in people who don't have these mutations. 

Possible side effects of drugs that target EGFR

The most common side effects of these drugs are skin problems such as an acne-like rash on the face and chest during treatment, which can sometimes lead to infections. An antibiotic cream or ointment may be needed to help limit the rash and related infections. The skin problems with panitumumab can be more serious and might lead to the skin peeling off. Other side effects can include:

  • Headache
  • Tiredness
  • Fever
  • Diarrhea

A rare but serious side effect of these drugs is an allergic reaction during the infusion, which could cause problems with breathing and low blood pressure. You may be given medicine before treatment to help prevent this.

Other targeted therapy drugs

Regorafenib (Stivarga) is a type of targeted therapy known as a kinase inhibitor. Kinases are proteins on or near the surface of a cell that carry important signals to the cell’s control center. Regorafenib blocks several kinase proteins that either help tumor cells grow or help form new blood vessels to feed the tumor. Blocking these proteins can help stop the growth of cancer cells.

This drug is used to treat advanced colorectal cancer, typically when other drugs are no longer helpful. It's taken as a pill.

Common side effects include fatigue, loss of appetite, hand-foot syndrome (redness and irritation of the hands and feet), diarrhea, high blood pressure, weight loss, and abdominal pain.

Less common but more serious side effects can include severe bleeding or perforations (holes) in the stomach or intestines.

More information about targeted therapy

To learn more about how targeted drugs are used to treat cancer, see Targeted Cancer Therapy.

To learn about some of the side effects listed here and how to manage them, see Managing Cancer-related Side Effects.

The American Cancer Society medical and editorial content team
Our team is made up of doctors and master's-prepared nurses with deep knowledge of cancer care as well as journalists, editors, and translators with extensive experience in medical writing.

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Last Medical Review: February 21, 2018 Last Revised: February 21, 2018

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