There are many treatment options available for people with advanced non-small cell lung cancer (NSCLC). Targeted therapies are a relatively new type of NSCLC treatment that focuses on identifying cancer cells with specific gene mutations (changes) or receptors, then targeting and destroying only those cells.

Targeted therapies have been used to treat lung cancer for more than 20 years. As researchers continue to discover more targets on cancer cells, more targeted therapies are developed. Continue reading to learn more about targeted therapy for NSCLC.

1. Targeted Drugs Are Mostly Used for Advanced NSCLC

At this time, targeted therapies are often reserved for people with advanced NSCLC. NSCLC is typically considered to be advanced when it has spread to other tissues — near the lungs (locally advanced) or in other parts of the body (metastatic NSCLC). They can be used alone or in combination with other NSCLC treatments, including surgery, chemotherapy, immunotherapy, or radiation therapy.

Researchers are currently studying whether targeted therapy drugs may also be effective for people with early-stage NSCLC. For example, targeted therapies may help decrease the risk of recurrent (returning) NSCLC after surgical treatment for people with stage 1 or 2 NSCLC.

Most often, targeted therapies are used for advanced NSCLC, when cancer has spread. Studies are looking into whether targeted drugs may help people with earlier stages of NSCLC, too.

2. Targeted Drugs Zero in Specifically on Cancer Cells

In general, targeted therapies work by inhibiting the effect of gene mutations that cause cancer cells to grow out of control. The mutated genes contain instructions for how to make abnormal proteins that encourage cancer cell growth. Many targeted therapy drugs zero in on these proteins, blocking their effect and preventing rapid cancer cell growth. In contrast to conventional chemotherapy, targeted therapies are less likely to damage other normal cells, which reduces the risk of unwanted side effects.

3. Many Gene Mutations and Proteins Can Be Targeted

Different types of targeted therapies are designed to block the abnormal proteins that result from specific gene mutations.

Common Targets

The most common genetic mutation in NSCLC is in the KRAS gene. Between 20 percent and 25 percent of people with NSCLC have this mutation. Epidermal growth factor receptor (EGFR) mutations are the second most common. EGFR mutations occur in about 10 percent to 20 percent of people with NSCLC. Several other targeted therapies are available for people with specific genetic mutations.

VEGF Inhibitors

Vascular endothelial growth factor (VEGF) inhibitors help block the formation of new blood vessels. Some tumors can release the VEGF protein to encourage angiogenesis, the formation of new blood vessels. Angiogenesis encourages tumor growth by providing a continuous supply of blood, oxygen, and nutrients to cancer cells. Blocking angiogenesis can help slow tumor growth. Bevacizumab (Avastin) and ramucirumab (Cyramza) both target the VEGF protein.

HER2 Inhibitors

HER2-directed therapies can help slow cancer cell growth in people who have mutations in the HER2 gene. Some HER2 inhibitors are antibody-drug conjugates. These targeted therapies use laboratory-made antibodies to target the HER2 protein and bring a chemotherapy drug directly to the tumor cells. Fam-trastuzumab deruxtecan-nxki (Enhertu) and zenocutuzumab-zbco (Bizengri) are examples of NSCLC treatments that target HER2.

Targeted Therapies by Class

In the following table, you’ll find examples of specific drugs for each class of targeted therapy approved by the U.S. Food and Drug Administration (FDA) for NSCLC. Drugs from each class of targeted cancer therapy work similarly by targeting the same mutation or protein. However, some drugs can target several mutations or proteins.

More targeted therapies for NSCLC are being studied and may become available in the future.

4. Some Targeted Therapies Are Also Immunotherapies

Immunotherapies are treatments that use your immune system to fight cancer. Some targeted therapies use laboratory-made versions of antibodies (immune proteins) called monoclonal antibodies to zero in on a specific target.

Types of immunotherapy for NSCLC include:

• PD-1/PD-L1 inhibitors — These include cemiplimab (Libtayo), nivolumab (Opdivo), and pembrolizumab (Keytruda).
• CTLA-4 inhibitors — These include ipilimumab (Yervoy) and tremelimumab (Imjudo).

5. Most Targeted Therapies Are Taken by Mouth

Most of the targeted therapy drugs currently available are pills that are given orally (by mouth). This may allow you to take targeted therapy at home. The way you take a targeted drug depends on the type of drug. It’s important to follow your cancer care team’s instructions exactly.

Some targeted therapies are given as an injection into a vein. In general, monoclonal antibody drugs are usually given as an injection instead of as a pill.

6. Targeted Therapies May Have Fewer Side Effects

Other types of lung cancer treatments, like chemotherapy and radiation therapy, can affect healthy cells in addition to cancer cells.

Chemotherapy drugs work by killing all cells that are quickly growing and dividing. Since cancer cells generally grow much faster than healthy cells, chemotherapy drugs are more likely to kill these cells. However, chemotherapy can also affect healthy cells that grow quickly, such as those in the skin, bone marrow, and digestive tract.

Radiation therapy uses high-energy particles to slow or stop cancer cell growth. This type of treatment can cause side effects if the healthy tissue nearby is affected.

Targeted therapy drugs are designed to zero in on a protein or gene that’s only found in cancer cells. Because of this, the effect on normal cells may be more limited compared to other treatments.

Targeted therapy drugs are designed to zero in on a protein or gene that’s only found in cancer cells. Because of this, they may cause fewer side effects.

The side effects of targeted drugs vary depending on which drug you’re taking, your dose, and other factors. Common side effects of targeted therapy drugs may include:

• Rash and other skin problems
• Nail changes
• Inflammation
• Diarrhea or constipation
• Blood test changes
• Fatigue (tiredness that does not improve with rest)

7. Targeted Therapy Is a Type of Personalized Medicine

Targeted therapy drugs offer personalized treatment options based on the genetic factors unique to your cancer. Between 40 percent and 50 percent of people with NSCLC may be candidates for targeted therapies.

Your oncologist can find out which targeted therapies are more likely to work for your cancer with molecular testing of cancer cells. Also known as biomarker testing, these tests look for the genetic changes that help cancer cells grow. Next-generation sequencing tests can check for several biomarkers at once. Talk to your cancer care team to learn more about molecular testing for NSCLC.

8. Targeted Therapies May Help People With NSCLC Live Longer

Targeted therapies have changed the landscape of NSCLC treatment by offering a personalized approach to treatment. Studies have found that this individualized approach can improve prognosis (outcomes) for some people. For example, a 2023 study found that people with advanced NSCLC who received targeted therapies lived significantly longer compared to those who didn’t.

Researchers continue to develop new targeted therapies as they learn more about how NSCLC grows. The research field is growing so quickly that new targeted therapies may be available to you since you’ve been diagnosed. Stay in touch with your oncology team to learn if there are any new targeted therapies or clinical trials that may benefit you.

Ask your oncologist whether there are any new targeted therapies or clinical trials that might help treat your NSCLC.

Talk With Others Who Understand

On MyLungCancerTeam, the social network for people with lung cancer and their loved ones, more than 15,000 people from around the world come together to ask questions, offer support and advice, and connect with others who understand life with lung cancer.

Have you used any targeted treatments for NSCLC? What were your experiences? Share in the comments below or by posting on your Activities page.