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. Tarceva is an EGFR inhibitor and is also classified as a tyrosine kinase inhibitor (TKI). It is designed to block the activating sites (tyrosine 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, Tarceva may shrink the cancer or slow the cancer’s progression.1,2

Tarceva is used to treat the following types of patients with NSCLC:

  • As an initial treatment for those whose cancer is metastatic (spread to distant parts of the body) with EGFR exon 19 deletions or exon 21 (L858R) substitution mutations
  • As a maintenance treatment for patients with advanced stage NSCLC whose cancer has not spread or grown after prior treatment with certain types of chemotherapy
  • As a second or third-line treatment for advanced stage NSCLC in patients whose cancer has spread or grown after at least one chemotherapy treatment 2

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

Taking Tarceva

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 Tarceva is determined by several factors, including the patient’s general health, the type of cancer, and ongoing response to treatment.2

Side Effects of Tarceva

Tarceva 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 Tarceva 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, Tarceva can cause severe side effects, including serious issues with lungs, liver, kidneys,  or gastrointestinal tract. Patients taking Tarceva 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 Tarceva 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 Tarceva 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 Tarceva, as it may be hazardous to the fetus. It is not recommended for men or women to conceive a child while taking Tarceva, and patients are advised to use barrier methods of contraception (i.e. condoms). It is not known whether Tarceva passes into breast milk, and patients should not breastfeed while taking Tarceva.2

Written by: Emily Downward | Last reviewed: October 2018.
View References
  1. Tarceva product website, Astellas Pharma. Accessed online on 9/28/16 at http://www.tarceva.com/.
  2. Chemocare. Accessed online on 9/28/16 at http://chemocare.com/chemotherapy/drug-info/Tarceva.aspx.
  3. National Cancer Institute. Accessed online on 8/1/16 at http://www.cancer.gov/.
  4. My Cancer Genome. Accessed online on 8/11/16 at https://www.mycancergenome.org/.