Tarceva (erlotinib)

Reviewed by: HU Medical Review Board | Last reviewed: July 2022

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

It is estimated that approximately 10-20 percent 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 patients who have never smoked (patients may be 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. 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 approximately 30 percent of patients taking erlotinib include rash, diarrhea, poor appetite, fatigue, shortness of breath, cough, nausea and vomiting. Less common side effects experienced in approximately 10-29 percent of patients receiving Tarceva include infection, mouth sores, itching, dry skin, eye irritation, and abdominal pain. Less commonly, 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 an exhaustive list of all potential side effects of erlotinib. Talk to your healthcare provider or pharmacist for further information.1,2


Patients receiving erlotinib should talk to their doctor about any other medications (prescription and over-the-counter), herbal remedies, and any supplements they are taking, as well as any other health conditions. If you are pregnant, plan to become pregnant, or are breastfeeding or plan to breastfeed, talk with your doctor. Erlotinib can cause harm to a developing fetus and should not be taken by women who are pregnant. While receiving erlotinib, females who can become pregnant should use contraceptives during treatment and for a period of time after completing treatment (patients should discuss appropriate birth control methods, and how long they need to use them, with their doctor). Females should not breastfeed during erlotinib treatment and for a period of time following the final dose (patients should discuss breastfeeding considerations with their doctor).2

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