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Tarceva (erlotinib)

Tarceva® is a targeted therapy that is used to treat some non-small cell lung cancers (NSCLC) that have a certain EGFR (epidermal growth factor receptor) mutation, specifically the exon 19 deletions or exon 21 (L858R) substitution mutations. EGFR mutation is determined by biomarker tests (molecular testing) conducted on a biopsy sample of the tumor. Erlotinib is an EGFR inhibitor and is also classified as a kinase inhibitor. It is designed to block the activating sites (kinases) of several proteins within the cancer cell. These proteins can stimulate cancer growth when the tumor has an EGFR mutation. By blocking the action of the proteins, erlotinib may shrink the cancer or slow the cancer’s progression.1,2

Erlotinib is used to treat NSCLC that is positive for EGFR mutation (exon 19 deletions or exon 21 (L858R) substitution) and is metastatic (spread to distant parts of the body) in patients undergoing first-line treatment, maintenance treatment, or treatment that is second line or beyond in patients where the cancer has become worse after receiving at least one previous chemotherapy treatment regimen.

About EGFR Mutations

An estimated 10% of patients with non-small cell lung cancer (NSCLC) in the United States have a tumor mutation associated with EGFR. EGFR mutations are most often found in tumors in female patients who have never smoked (patients are considered “never smokers” if they have smoked less than 100 cigarettes in their lifetime). The tumors are likely to be adenocarcinoma. However, EGFR mutations are not exclusive to this type of NSCLC or non-smokers – mutations have also been found in smokers and in other tumor types.3,4

Receiving erlotinib

Tarceva is a tablet that is taken by mouth on an empty stomach. It should be taken at least 1 hour before a meal or 2 hours after a meal and may be taken with a glass of water. The dosage of erlotinib is determined by several factors, including the patient’s general health, the type of cancer, and ongoing response to treatment. Patients should take their medication as prescribed by their doctor. Patients should talk to their doctor if they have any questions, or if they have questions regarding their erlotinib regimen.2

Side effects of erlotinib

Erlotinib may cause side effects, and in some cases, these side effects can be severe. Any side effects should be reported to a health care professional. Side effects experienced in greater than 30% of patients taking erlotinib include rash, diarrhea, poor appetite, fatigue, shortness of breath, cough, nausea and vomiting. Less common side effects experienced in 10-29% of patients receiving Tarceva include infection, mouth sores, itching, dry skin, eye irritation, and abdominal pain. Rarely, erlotinib can cause severe side effects, including serious issues with lungs, liver, kidneys,  or gastrointestinal tract. Patients taking erlotinib should seek medical care immediately if they experience any of the following symptoms: serious or ongoing diarrhea, nausea, loss of appetite, vomiting, new or worsening shortness of breath or cough, eye irritation, or new or worsening rash, blistering, or peeling of the skin. This is not a complete list of side effects.1,2


Patients receiving erlotinib should talk to their doctor about other medications, herbal remedies, and any supplements they are taking, as well as any other health conditions. Patients should talk to their doctor before receiving immunizations or vaccinations while taking erlotinib to make sure they are appropriate. Patients who are pregnant or may become pregnant during treatment should discuss their condition with their doctor prior to starting erlotinib, as it may be hazardous to the fetus. Females who can become pregnant should utilize effective birth control (patients should discuss appropriate birth control methods with their doctor) throughout erlotinib treatment and for one month following the final dose of erlotinib. It is not known whether erlotinib passes into breast milk, and patients should not breastfeed during erlotinib treatment and for two weeks following the last dose of erlotinib.2

Written by: Emily Downward | Last reviewed: January 2020.
  1. Tarceva product website, Astellas Pharma. Accessed online on 9/28/16 at
  2. Chemocare. Accessed online on 9/28/16 at
  3. National Cancer Institute. Accessed online on 8/1/16 at
  4. My Cancer Genome. Accessed online on 8/11/16 at