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
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
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
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
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
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
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
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 (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
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
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 (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
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
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
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
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.