Targeted Therapy for Lung Cancer

May 5, 2025

This page was reviewed under our medical and editorial policy by Jyoti Malhotra, M.D., M.P.H., associate professor, Department of Medical Oncology & Therapeutics Research, City of Hope^® Orange County Lennar Foundation Cancer Center; and Arya Amini, M.D., associate professor, Department of Radiation Oncology, City of Hope Cancer Center Duarte 

Targeted therapy may be an effective treatment option for some lung cancer patients. It's most often used to treat advanced non-small cell lung cancer (NSCLC), sometimes in combination with other treatments.

Targeted therapy involves a range of cancer treatments designed to attack tumors on a cellular level to kill cancer cells or slow their growth. To determine if targeted therapy is a lung cancer treatment option, patients undergo certain tests that look for specific cellular or genetic changes that may respond to it.

What Is Targeted Therapy for Lung Cancer?

Unlike conventional chemotherapy, which may affect cells throughout the body, targeted therapies are engineered to find and attack cancer cells only. Most targeted therapies are taken in the form of a pill. They precisely target certain elements within a tumor — for example, the proteins or enzymes that control how the tumor grows — to slow down tumor growth or kill cancer cells.

Most targeted therapies are designed to do one of the following:

• Alter the proteins in a cancer cell so it dies
• Deliver treatments to the cancer cell to kill it
• Block certain chemical signals to slow down or prevent a tumor from growing
• Prevent new blood vessels from developing, to slow the growth of a tumor

Targeted therapy is sometimes considered part of a precision medicine or personalized medicine approach to cancer care, because it's an individually targeted type of treatment.

Molecular and Biomarker Testing

Advanced lung cancer patients usually undergo molecular and biomarker testing (sometimes just referred to as biomarker testing) to determine whether their cancer may respond to targeted therapy.

Molecular and biomarker testing involves taking a tissue sample and examining it to look for specific proteins, gene changes or other molecular signs that a tumor may be targeted using a type of targeted therapy. Testing may require a conventional biopsy that removes a solid tissue sample. But it's sometimes possible to use a liquid biopsy, which takes a sample of a bodily fluid such as blood.

Types of Lung Cancer Targeted Therapy

ALK Inhibitors

ALK inhibitors target a mutation in the ALK gene that causes the production of an abnormal protein that may lead to lung cancer. The ALK gene alteration is more common among younger people, those who do not smoke heavily or at all and those with NSCLC adenocarcinoma. Current ALK inhibitors include:

• Lorlatinib (Lorbrena^®)
• Alectinib (Alecensa^®)
• Brigatinib (Alunbrig^®)
• Ceritinib (Zykadia^®)
• Crizotinib (Xalkori^®)
• Alectinib (Alecensa^®)

Angiogenesis Inhibitors

Angiogenesis refers to the process of a tumor creating new blood vessels so it may continue to grow. Angiogenesis inhibitors work to stop or slow down this process on a cellular level by targeting the vascular endothelial growth factor (VEGF) protein.

Current angiogenesis inhibitors for lung cancer include:

• Bevacizumab (Avastin^®)
• Ramucirumab (Cyramza^®)

BRAF Inhibitors

BRAF inhibitors target a mutation in the BRAF gene. This mutation may produce a specific protein which encourages the growth of lung cancer. Sometimes, BRAF inhibitors are recommended in combination with another type of targeted therapy that targets changes in the MEK gene. Some common BRAF inhibitor treatments are:

• Dabrafenib (Tafinlar®) with MEK inhibitor trametinib (Mekinist®)
• Encorafenib (Braftovi®) with MEK inhibitor binimetinib (Mektovi®)
• Vemurafenib (Zelboraf®)

EGFR Inhibitors

The epidermal growth factor receptor (EGFR) protein is found on the surface of cells. In certain advanced lung cancers, a cell produces too much EGFR, leading to a quick-growing tumor. EGFR inhibitors target the EGFR mutation to try to slow down a tumor’s growth. These include:

• Afatinib (Gilotrif^®), erlotinib (Tarceva^®), dacomitinib (Vizimpro^®), gefitinib (Iressa^®) and osimertinib (Tagresso^®), most often taken alone
• Lazertinib (Lazcluze^®), often taken with amivantamab (Rybrevant^®)
• Osimertinib or amivantamab, often combined with chemotherapy
• Erlotinib, often combined with an angiogenesis inhibitor

HER2 Inhibitors

HER2 inhibitors are intravenous medications that target changes in the HER2 gene that may cause lung cancer. They are most often recommended for people with metastatic lung cancer who have already undergone other treatments.

• Fam-trastuzumab deruxtecan-nxki (Enhertu^®) and ado-trastuzumab emtansine (Kadcyla^®): These lab-made antibodies are given intravenously and help the medication target and attach to the HER2 protein.
• Zenocutuzumab-zbco (Bizengri^®): This drug targets tumors that have an NRG1 fusion, which is a rare genetic alteration.

KRAS Inhibitors

A mutation in the KRAS gene, leading to the production of too much of a certain protein, is found in around one out of eight cases of NSCLC. KRAS inhibitors target this mutation to slow down or stop a tumor’s growth. They include:

• Sotorasib (Lumakras^®)
• Adagrasib (Krazati^®)

MET Inhibitors

MET inhibitors target a genetic mutation in the MET gene that drives the growth of cancer cells. There are several types of MET inhibitors, including:

• Capmatinib (Tabrecta^®)
• Tepotinib (Tepmetko^®)
• Crizotinib (Xalkori^®)

RET Inhibitors

RET inhibitors target a change in the RET gene that causes the production of a protein that encourages tumor growth. Current RET inhibitors include:

• Selpercatinib (Retevmo^®)
• Pralsetinib (Gayreto^®)
• Cabozantinib (Cometriq^® or Cabometyx^®), which is recommended in a smaller number of cases

ROS1 Inhibitors

Changes in the ROS1 gene are similar to those found in the ALK gene, and are found in less than 2% of all NSCLC cases. ROS1 inhibitors target this genetic mutation:

• Entrectinib (Rozlytrek^®), crizotinib (Xalkori^®) and ceritinib (Zykadia^®) are most commonly recommended
• Lorlatinib (Lorbrena^®) and repotrectinib (Augtyro^®) may also be recommended

TRK Inhibitors

TRK inhibitors target a change in the TRK gene that may cause the growth of tumors. Current TRK inhibitors include:

• Larotrectinib (Vitrakyi^®)
• Entrectinib (Rozlytrek^®)

Side Effects of Lung Cancer Targeted Therapy

Patients with lung cancer may experience some side effects related to targeted therapy. Although the exact side effects may vary depending on the type of targeted therapy, the most common issues patients experience include:

• Nausea, diarrhea or vomiting
• Sore muscles or swelling in the extremities
• Fatigue or tiredness
• Changes to blood count or other blood test values
• Changes to the skin or nails
• Nerve damage

Talk to the care team to evaluate which types of side effects the patient may expect on lung cancer targeted therapy.