Targeted Therapy

Reviewed by: HU Medical Review Board | Last reviewed: September 2023

Many lung cancer treatments that kill cancer cells also affect healthy cells. This can cause side effects. But some lung cancer drugs only target specific features of cancer cells, so they help reduce damage to healthy cells. These are called targeted therapies.1

Targeted therapies are not the best treatment for everyone. They work only if you have the specific genetic changes that the treatment targets. And your response to the treatment may not last over time. Talk to your doctor about whether targeted therapies are right for you.2

How does targeted therapy work?

Targeted therapies block specific proteins that help tumors grow and spread. They often have a lower risk of side effects than chemotherapy. Chemotherapies kill many different types of cells that grow and divide quickly. This can affect normal healthy cells, leading to side effects.1

Targeted therapies are tailored to specific genetic factors in cancer cells. Your doctor can identify changes in the DNA of your cancer cells. Targeted therapies then “target” your specific changes. This type of treatment attempts to minimize the impact of healthy cells.1

Targeted therapy treats cancer by:2

  • Stopping uncontrolled division of cancer cells
  • Preventing tumors from forming new blood vessels
  • Delivering cell-destroying drugs to cancer cells
  • Causing cancer cell death

Examples of targeted therapy

The FDA has approved many targeted therapies for lung cancers. Many therapies target proteins that are important for cells to grow and divide. Changes to these proteins can lead to uncontrolled tumor growth. So, blocking these targets can reduce cancer cell growth.3

Epidermal growth factor receptor (EGFR) inhibitors

Lung cancers with EGFR mutations are called EGFR-positive lung cancers. About 10 to 15 percent of people with lung cancer are EGFR-positive. People with EGFR-positive lung cancer tend to have no smoking history.4,5

Those with EGFR-positive cancer may be treated with EGFR inhibitors, including:4,5

  • Gilotrif® (afatinib)
  • Iressa® (gefitinib)
  • Portrazza® (necitumumab)
  • Tagrisso® (osimertinib)
  • Tarceva® (erlotinib)
  • Vizimpro® (dacomitinib)
  • Rybrevant® (amivantamab)
  • Exkivity® (mobocertinib)

Anaplastic lymphoma kinase (ALK) inhibitors

Another possibility is that someone's ALK gene rearranges and combines with another gene. When this happens, the cancer is known as ALK-positive. About 4 percent of people with lung cancer are ALK-positive. People with ALK-positive lung cancer tend to have no smoking history.4,6

Those with ALK-positive cancer may be treated with ALK inhibitors, including:4,6

  • Alecensa® (alectinib)
  • Xalkori® (crizotinib)
  • Zykadia® (ceritinib)
  • Alunbrig® (brigatinib)
  • Lorbrena® (lorlatinib)

BRAF/MEK inhibitors

Mutations in the BRAF gene can cause a protein called MEK to be overactive. The BRAF V600E mutation is the most common. About 1 to 2 percent of people with non-small cell lung cancer have BRAF V600E. It is most common in people with a history of smoking.4,7

Those with BRAF V600E lung cancer may be treated with a combination of:4,7

  • Tafinlar® (dabrafenib) – a BRAF inhibitor
  • Mekinist® (trametinib) – an MEK inhibitor

ROS1 inhibitors

In some people, the ROS1 gene rearranges and combines with part of another gene. This is called being ROS1-positive. About 1 to 2 percent of people with lung cancer are ROS1-positive.4,8

Those with ROS1-positive cancer may be treated with ROS1 inhibitors, including:4,8

  • Xalkori® (crizotinib)
  • Lorbrena® (lorlatinib)
  • Rozlytrek® (entrectinib)
  • Zykadia® (ceritinib)

Neurotrophic tyrosine receptor kinase (NTRK) inhibitors

The NTRK gene can fuse with another gene to produce altered TRK proteins. NTRK fusion-positive lung cancer is very rare.

People with NTRK fusion-positive cancer may be treated with NTRK inhibitors, including:4,9

  • Rozlytrek® (entrectinib)
  • Vitrakvi® (Larotrectinib)

Mesenchymal epithelial transition (MET) inhibitors

Changes in the MET gene can prevent cells from breaking down the MET protein. About 5 percent of people with lung cancer have MET changes.4,10

Those with MET changes may be treated with MET inhibitors, including:4,10

  • Tabrecta® (capmatinib)
  • Tepmetko® (tepotinib)

Rearranged during transfection (RET) inhibitors

Changes in the RET gene can cause it to rearrange and fuse with other genes. About 1 to 2 percent of people with lung cancer have RET rearrangements.4,11

Those with RET rearrangements may be treated with RET inhibitors, including:4,11

  • Retevmo® (selpercatinib)
  • Gavreto® (pralsetinib)

KRAS inhibitors

About 20 to 25 percent of people with lung cancer have a mutation on the KRAS gene. KRAS G12C is the most common KRAS mutation.12-14

People with the KRAS G12C mutation may be treated with a KRAS inhibitor, including:12-14

  • Lumakras® (sotorasib)
  • Krazati® (adagrasib)

Angiogenesis inhibitors

Angiogenesis is the development of new blood vessels. Tumors must form new blood vessels to grow beyond a certain size. Angiogenesis inhibitors that may treat certain forms of non-small cell lung cancer include:15

  • Avastin® (bevacizumab)
  • Cyramza® (ramucirumab)

What are the possible side effects?

Targeted therapies usually cause fewer side effects than chemotherapy. However, side effects are possible. They depend on the targeted therapy you are taking. Some common side effects of targeted therapies include:2

  • Skin problems
  • Problems with blood clotting and wound healing
  • High blood pressure
  • Diarrhea
  • Liver problems

These are not all the possible side effects of targeted therapy. Talk to your doctor about what to expect during treatment. Call your doctor if you experience any changes that concern you while taking targeted therapies.

Other things to know

Take targeted therapies only as your doctor prescribes. Some are taken as pills, while others are injected. How often and how long you take targeted therapies will depend on the type of targeted therapy.2

During treatment, your doctor will perform physical exams and medical tests. This can help them know whether the treatment is working. Your response to targeted therapy treatment may not stay the same over time. This is because cancers can become resistant to these treatments. If this happens, your doctor may suggest new treatments.2

Before beginning a targeted therapy, tell your doctor about all your health conditions and any other drugs, vitamins, or supplements you are taking. This includes over-the-counter drugs.

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