How does erlotinib work (mechanism of action)?

Erlotinib works by blocking the epidermal growth factor receptor (EGFR), a protein on cells that encourages cancer cell growth. EGFR is found on the surface of normal cells and cancer cells. EGFR normally helps cells to divide and multiply, but some cancer cells have too much EGFR which leads to uncontrolled growth. When EGFR is blocked by erlotinib, cancer growth may shrink or stop for a period of time.

Erlotinib may prolong how long you can live without your cancer worsening and may also help to increase the amount of time you live overall.

Erlotinib (brand name: Tarceva) is approved by the FDA for the treatment of:

• Non-small cell lung cancer (NSCLC) with EGRF protein mutations (exon 19 deletions or exon 21 substitution mutations) in patients who have had at least one prior chemotherapy regimen. If you have a cancer with EGFR receptors you are considered “EGFR positive”. Your doctor may order tests to check for these receptors before you receive treatment.
• Advanced stage pancreatic cancer that has spread to other parts of the body, in combination with gemcitabine, in patients who have not previously received chemotherapy.

What enzyme does erlotinib block?

Erlotinib is an inhibitor of the tyrosine kinase inhibitor enzyme. EGFR inhibitors can be classified as either tyrosine kinase inhibitors (TKI) or monoclonal antibodies.

Erlotinib is considered a targeted drug therapy as opposed to being a traditional chemotherapy. Targeted drug therapies are more specific in the way they target cancer cells. Targeted drugs like erlotinib can block signals that make cancer cells grow. It is given as an oral tablet.

Related: Can Tarceva (erlotinib) cure lung cancer?

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Which other medicines are EGFR inhibitors?

EGFR inhibitors are a large class of medicines used to treat various types of cancers such as breast cancer, non-small cell lung cancer (NSCLC), pancreatic cancer, squamous cell cancer of the head and neck, medullary thyroid cancer and colorectal cancer.

Medications in the EGFR class include:

• afatinib (Gilotrif)
• cetuximab (Erbitux)
• dacomitinib (Vizimpro)
• erlotinib (Tarceva)
• gefitinib (Iressa)
• lapatinib (Tykerb)
• mobocertinib (Exkivity)
• necitumumab (Portrazza)
• neratinib (Nerlynx)
• osimertinib (Tagrisso)
• panitumumab (Vectibix)
• vandetanib (Caprelsa)

What other EGFR inhibitors are used to treat non-small cell lung cancer (NSCLC)?

EGFR inhibitors that are specifically used to treat non-small cell lung cancer (NSCLC) with EGFR mutations include:

• afatinib (Gilotrif)
• dacomitinib (Vizimpro)
• erlotinib (Tarceva)
• gefitinib (Iressa)
• mobocertinib (Exkivity)
• necitumumab (Portrazza)
• osimertinib (Tagrisso)

This is not all the information you need to know about erlotinib for safe and effective use and does not take the place of your doctor’s directions. Review the full product information and discuss this information and any questions you have with your doctor or other health care provider.