Targeted Therapy for Non-Small Cell Lung Cancer

Targeted therapy uses drugs to target specific changes in cancer cells that help them grow, divide, and spread. Targeted therapy drugs are designed to be more precise. They fight cancer cells while causing less harm to other cells in the body.  

Most lung cancer targeted therapies are taken by mouth as a pill. A few targeted drugs are given by IV (through a vein), sometimes in combination with chemotherapy. 

These are the latest targeted therapies available to treat non-small cell lung cancer. New treatments become available all the time, so this may not be a complete list. 

Please note: The side effects listed here do not represent a comprehensive list. It's important to discuss all potential side effects of a drug with your healthcare team. Be sure to tell your healthcare team about any side effects you do have.

All Available Treatments

Intravenous =
Pill =

Treatment Type

ALK Inhibitors

Drug Names
Alecensa® (alectinib) (Pill)
Alunbrig® (brigatinib) (Pill)
Lorbrena® (lorlatinib) (Pill)
Xalkori (ALK Inhibitors)® (crizotinib) (Pill)
Zykadia® (ceritinib) (Pill)
Potential Severe Side Effects (All drugs)
Heart problems Kidney problems Liver problems Lung problems
Potential Severe Side Effects (Lobrena)
Low blood counts
Potential Side Effects (All drugs)
Eye problems Constipation Diarrhea Fatigue/weakness Weight/appetite changes Nausea/vomiting Neuropathy Swelling
Potential Side Effects (Lorbrena)
Emotional or cognitive changes
Potential Side Effects (Alecensa)
Cough Skin/nail changes
Important Things to Know
  • These drugs are for ALK+ metastatic NSCLC.
  • Alecensa and Xalkori are given as a twice-daily pill.
  • Alunbrig, Lorbrena, and Zykadia are given as a once-daily pill.       

Treatment Type

BRAF Inhibitors

Drug Names
Mekinist® (trametinib) (Pill)
Tafinlar® (dabrafenib) (Pill)
Rare But Serious Potential Side Effects
Adverse drug reaction Eye problems Heart problems Blood sugar changes Kidney problems Liver problems Lung problems
Potential Side Effects
Diarrhea Fatigue/weakness Fever Nausea/vomiting Skin/nail changes Sun sensitivity
Important Things to Know
  • These drugs are for BRAF+ NSCLC. They are given in combination with each other.
  • Tafinlar is given as a twice-daily pill.
  • Mekinist is given as a once-daily pill.

Treatment Type

EGFR Inhibitors

Drug Names
Gilotrif® (afatinib) (Pill)
Iressa® (gefitinib) (Pill)
Portrazza® (necitumumab) (IV)
Tagrisso® (osimertinib) (Pill)
Tarceva® (erlotinib) (Pill)
Vizimpro® (dacomitinib) (Pill)
Rare But Serious Potential Side Effects
Eye problems Heart problems Liver problems Lung problems
Potential Side Effects
Diarrhea Fatigue/weakness Weight/appetite changes Mouth sores Skin/nail changes
Important Things to Know

Mouth sores are a potential side effect that can be painful and affect your oral intake. Speak to your provider about proactive management and an oral care regimen.

For EGFR+ metastatic NSCLC 

  • Depending on the exact EGFR mutation, can be used as first treatment: Gilotrif, Iressa, Tagrisso, Tarceva, and Vizimpro.
  • Can be used when other EGFR drugs have stopped working: Tagrisso.
  • All of these drugs are given as a once-daily pill.

For EGFR+ earlier-stage NSCLC 

  • Depending on the exact EGFR mutation, can be used as treatment after surgery: Tagrisso.

For advanced squamous cell NSCLC: Portrazza

  • Given by IV (in the vein) in combination with chemotherapy.

Treatment Type

Bispecific Antibody

Drug Name
Rybrevant™ (amivantamab) (IV)
Rare But Serious Potential Side Effects
Heart problems Blood sugar changes Liver problems Lung problems
Potential Side Effects
Breathing problems Constipation Fatigue/weakness Adverse drug reaction Nausea/vomiting Skin/nail changes Swelling
Important Things to Know
  • This drug is used for EGFR+ metastatic NSCLC. Depending on the exact EGFR mutation, it can be used as first treatment.
  • Rybrevant is given by IV (in the vein) every 2-4 weeks.                 

Treatment Type

HER2 Inhibitors

Drug Name
Enhertu (fam-trastuzumab deruxtecan-nxki) (IV)
Potential Severe Side Effects
Embryo-Fetal Toxicity Interstitial Lung Disease (ILD) including pneumonitis Neutropenia
Potential Side Effects
Abdominal Pain Bleeding Constipation Diarrhea Fatigue/weakness Hair thinning/loss Headache Infections Low blood counts Musculoskeletal pain Nausea/vomiting Weight/appetite changes
Important Things to Know
  • These drugs treat NSCLC tumors which have activating HER2 (ERBB2) mutations and have received a prior systemic therapy.
  • Enhertu is given by IV (in the vein) every 3 weeks.

Treatment Type

KRAS Inhibitors

Drug Names
Lumakras™ (sotorasib) (Pill)
Krazati® (adagrasib) (Pill)
Rare But Serious Potential Side Effects (Lumakras)
Nervous system changes Heart problems Kidney problems Liver problems Lung problems
Rare But Serious Potential Side Effects (Krazati)
Heart problems Gastrointestinal problems Liver problems Lung problems
Potential Side Effects (Lumakras)
Cough Diarrhea Fatigue/weakness Nausea/vomiting
Potential Side Effects (Krazati)
Abdominal Pain Bleeding Bone pain Cough Diarrhea Fatigue/weakness Fever Kidney problems Muscle pain Nausea/vomiting Shortness of breath Swelling Urinary, kidney, or bladder changes Weight/appetite changes
Important Things to Know

Lumakras

  • This drug is used for KRAS C12C+ metastatic NSCLC.
  • Lumakras is given as a once-daily pill.                 

Krazati

  • Adagrasib is a RAS GTPase family inhibitor for adult patients with KRAS G12C-mutated locally advanced or metastatic non-small cell lung cancer who have received at least one prior systemic therapy.
  • The recommended adagrasib tablet dose is 600 mg orally twice daily until disease progression or unacceptable toxicity.

Treatment Type

MET Inhibitors

Drug Names
Tabrecta™ (capmatinib) (Pill)
Tepmetko™ (tepotinib) (Pill)
Rare But Serious Potential Side Effects
Liver problems Lung problems
Potential Side Effects
Fatigue/weakness Nausea/vomiting Swelling
Important Things to Know
  • These drugs are used for MET+ metastatic NSCLC.
  • Tabrecta is given as a twice-daily pill.
  • Tepmetko is given as a once-daily pill.                 

Treatment Type

NTRK Inhibitors

Drug Names
Rozlytrek (NTRK Inhibitors)™ (entrectinib) (Pill)
Vitrakvi® (larotrectinib) (Pill)
Potential Severe Side Effects (All Drugs)
Nervous system changes Liver problems
Potential Severe Side Effects (Rozlytrek)
Eye problems Heart problems Kidney problems
Potential Side Effects (All drugs)
Constipation Diarrhea Dizziness Fatigue/weakness Nausea/vomiting
Potential Side Effects (Rozlytrek)
Neuropathy Swelling Taste changes Shortness of breath
Potential Side Effects (Vitrakvi)
Low blood counts
Important Things to Know
  • These drugs are used for NTRK+ metastatic solid tumors, including NSCLC.
  • Rozlytrek is given as a once-daily pill.
  • Vitrakvi is given as a twice-daily pill.
  • Regular blood tests are needed to check liver function.
  • Let your doctor know if you have dizziness, unclear speech, problems walking, or are feeling tingling, burning or numbness (most often occurs in the first 3 months).                

Treatment Type

RET Inhibitors

Drug Names
Gavreto™ (pralsetinib) (Pill)
Retevmo™ (selpercatinib) (Pill)
Potential Severe Side Effects
Bleeding Liver problems Lung problems
Potential Side Effects
Constipation Diarrhea Mouth/throat changes Fatigue/weakness Heart problems Blood pressure changes Swelling
Important Things to Know
  • These drugs are used for metastatic NSCLC.
  • Gavreto is given as a once-daily pill.
  • Retevmo is given as a twice-daily pill.

Treatment Type

ROS1 Inhibitors

Drug Names
Augtyro™ (repotrectinib) (Pill)
Rozlytrek (ROS1 Inhibitors)™ (entrectinib) (Pill)
Xalkori (ROS1 Inhibitors)® (crizotinib) (Pill)
Rare But Serious Potential Side Effects (Rozlytrek)
Nervous system changes Eye problems Heart problems Kidney problems Lung problems Liver problems
Rare But Serious Potential Side Effects (Xalkori)
Lung problems
Rare But Serious Potential Side Effects (Augtyro)
Liver Cancer Lung Cancer Nervous system changes
Potential Side Effects (All drugs)
Eye problems Constipation Diarrhea Fatigue/weakness Weight/appetite changes Nausea/vomiting Taste changes Swelling
Potential Side Effects (Rozlytrek)
Neuropathy Dizziness Shortness of breath
Potential Side Effects (Augtyro)
Abnormal lab tests Dizziness
Important Things to Know
  • These drugs are used for ROS1+ metastatic NSCLC.
  • Xalkori is given as a twice-daily pill.
  • Rozlytrek is given as a once-daily pill.                

Treatment Type

VEGF or Angiogenesis Inhibitors

Drug Names
Avastin® (bevacizumab) (IV)
Mvasi® (bevacizumab-awwb) (IV)
Zirabev™ (bevacizumab-bvzr) (IV)
Cyramza® (ramucirumab) (IV)
Rare But Serious Potential Side Effects
Bleeding Blood clots Heart problems
Potential Side Effects (All drugs)
Blood pressure changes Skin/nail changes Diarrhea Weight/appetite changes Low blood counts Fatigue/weakness Runny nose Infections
Potential Side Effects (Avastin)
Nosebleeds
Important Things to Know
  • Avastin is given for non-squamous advanced NSCLC.
  • Cyramza is given for EGFR+ metastatic NSCLC in combination with Tarceva.
  • These drugs are given by IV (in the vein) every 3 weeks, often in combination with chemo.
  • A stroke is a rare but serious potential side effect.