How Do Antineoplastic EGFR Inhibitors Work?

Antineoplastic epidermal growth factor receptor (EGFR) inhibitors are a class of drugs used to treat hormone receptor-positive breast cancer (breast cancer that depends on hormones such as estrogen to grow), medullary thyroid cancer, advanced head and neck cancer, metastatic colorectal cancer, non-small cell lung cancer, and pancreatic cancer.

EGFR inhibitors are anti-cancer medications that block the activity of a protein called EGFR. EGFR is found on the surface of some normal cells and is involved in cell growth, also found at high levels on some types of cancer cells, which causes these cells to grow and divide. Blocking EGFR helps in preventing unregulated cell division, thus preventing the growth, and spread of cancer cells.

EGFR inhibitors can be classified into the following:

• Tyrosine kinase inhibitors: targets the intracellular domain in EGFR and stops the activity of the EGFR.
• Monoclonal antibodies: targets the extracellular ligand-binding domain of EGFR and prevents cell division.

EGFR inhibitors are administered via intravenous (into a vein) and oral routes.

EGFR inhibitors work in the following ways:

• They belong to a class of medications called “tyrosine kinase inhibitors” that work by slowing down or stopping the growth of cancer cells.
• They work by blocking the action of an abnormal protein that signals cancer cells to multiply. This helps slow or stop the spread of cancer cells.
• They block the activity of a protein called "EGFR" and thus prevent unregulated cell division.

Antineoplastic EGFR inhibitors are used to treat conditions such as:

• Breast cancer
• Non-small cell lung cancer
• Medullary thyroid cancer
• Metastatic colorectal cancer
• Advanced squamous cell carcinoma of head and neck
• Pancreatic cancer
• Malignant gliomas

Some of the common side effects include:

• Nausea
• Vomiting
• Constipation
• Diarrhea
• Abdominal pain
• Headache
• Tiredness/weakness
• Taste changes
• Mouth sores
• Stomach upset
• Dry skin/mild rash
• Loss of appetite
• Heartburn
• Gas
• Bone/muscle pain
• Pain, redness, swelling, hardness, or itching at the injection site

Other rare side effects include:

• Dizziness 
• Blurred vision
• Fatigue 
• Weight loss
• Hair loss
• Chest pain
• Anemia (low red blood cell count)
• Insomnia (trouble falling and/or staying asleep)
• Shortness of breath
• Chills, sore throat, fever, or cough
• Rash/hives/itching
• Yellowing of the skin or eyes
• Swelling of the face, throat, tongue, lips, eyes, hands, feet, ankles, or lower legs
• Thrombocytopenia (low blood platelet count)
• Hypocalcemia (low blood calcium level)
• Hypokalemia (low blood potassium level)
• Hypophosphatemia (low blood phosphate level)
• Increased creatinine (a waste product formed by the normal breakdown of muscle cells)
• Hypoglycemia (low blood sugar level)
• Numbness, burning, or tingling of the hands or feet
• Changes in the appearance of the hair and nails
• Decreased urination
• Depression
• Anxiety
• Paronychia (skin infection around the fingernails or toenails)

Information contained herein is not intended to cover all possible side effects, precautions, warnings, drug interactions, allergic reactions, or adverse effects. Check with your doctor or pharmacist to make sure these drugs do not cause any harm when you take them along with other medicines. Never stop taking your medication and never change your dose or frequency without consulting your doctor.

Generic and brand names of antineoplastic EGFR inhibitors include:

• Afatinib
• Amivantamab
• Amivantamab-vmjw
• Caprelsa
• Cetuximab
• Dacomitinib
• Erbitux
• Erlotinib
• Exkivity
• Gefitinib
• Gilotrif
• Iressa
• Lapatinib
• Mobocertinib
• Necitumumab
• Neratinib
• Nerlynx
• Osimertinib
• Panitumumab
• Portrazza
• Rybrevant
• Tagrisso
• Tarceva
• Tykerb
• Vandetanib
• Vectibix
• Vizimpro