What to Know About Tarceva (Erlotinib)

A targeted therapy drug approved to treat cancer

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Tarceva (erlotinib) is a targeted cancer drug prescribed to treat advanced-stage non-small cell lung cancer (NSCLC) and advanced pancreatic cancer (in combination with chemotherapy). It is an oral medication that comes in tablet form and is believed to work by targeting epidermal growth factor receptor (EGFR), a protein that promotes cancer cell growth.


EGFR is a protein present on the surface of both healthy cells and cancer cells. It can be overexpressed in NSCLC and pancreatic cancer, causing rapid cell growth that helps the cancer spread.

Tarceva is in a class of medications called tyrosine kinase inhibitors. These medications prevent cancer cells from multiplying by blocking the abnormal tyrosine kinase activity of an abnormal, mutant EGFR protein.

The goal of Tarceva and other targeted therapy drugs is not to cure the cancer; it's intended to prevent the cancer from growing so you can manage the disease like you would a chronic illness such as diabetes.

For Non-Small Cell Lung Cancer Treatment

Lung cancer is one of the most common cancers worldwide, and it can have a poor prognosis.

Approximately 75% of people with lung cancer are diagnosed at an advanced stage of the disease, so surgery is frequently not a treatment option. Instead, chemotherapy has typically been recommended for almost all cases of advanced lung cancer. Targeted therapy is an option for patients with NSCLC who test positive for genetic mutations that are treatable.

For NSCLC with EGFR mutations, Tarceva is a type of targeted therapy that's often recommended as an initial treatment. In studies, patients survived longer with Tarceva compared to chemotherapy (approximately 13 months versus five months, respectively).

For Pancreatic Cancer Treatment

Pancreatic cancer accounts for about 3% of all cancers in the United States, and in 80% of cases, the malignancy is inoperable at the time of diagnosis.

With local treatments ineffective for pancreatic cancer, the chemotherapy drug Gemzar (gemcitabine) is usually the first course of treatment. Increasingly, though, doctors have looked at using a combination of treatments—including Tarceva.

Research shows that Gemzar combined with Tarceva resulted in better outcomes than Gemzar alone. As with NSCLC, the advantage of targeted therapy for pancreatic cancer is that it helps patients manage the disease for longer overall survival. In fact, disease control with Tarceva is estimated to be 85%—versus 33% for patients who undergo chemotherapy without Tarceva.

Off-Label Uses

While approved by the U.S. Food and Drug Administration (FDA) for pancreatic and lung cancer, Tarceva is sometimes prescribed for off-label use for other types of cancers when the tumors show an EGFR mutation. However, there are limited research reports on whether Tarceva is effective in such cases.

Before Taking

It is now common for all patients diagnosed with NSCLC to be tested for genetic mutations (alterations in the gene) with molecular profiling. These mutations are found only in the tumor cells, and not in other cells.

Molecular profiling is done with tissue biopsy sample that's usually collected with a fine needle, a bronchoscope, or surgery.

Your doctor may also order a liquid biopsy, which is a blood test that checks for cancer cells circulating in the blood that can be tested for genetic mutations.

If the EGFR mutation is found in your tumor, your doctor will discuss targeted therapy with you and may recommend Tarceva.


According to the FDA, you should not breastfeed while taking Tarceva. This medication can also cause fetal harm. Talk to your doctors if you're pregnant or if there's the chance you might become pregnant while taking Tarceva.


Tarceva is administered as an oral pill once daily on an empty stomach.

Per the manufacturer, OSI Pharmaceutical, dosing is as follows:

  • For NSCLC: 150 milligrams (mg)
  • For pancreatic cancer: 100 mg

Check your prescription and talk to your doctor to make sure you are taking the right dose for you.

Side Effects

The most common side effects caused by Tarceva include rash and diarrhea.


Tarceva rashes usually appear within two weeks of starting treatment for NSCLC. If you're taking Tarceva in combination with Gemzar, a rash can develop at anytime during treatment.

A Tarceva rash looks similar to acne or dry skin and can appear on the body and face; it most often appears from the waist up. For some, the rash can be itchy or feel like a sunburn.

Interestingly, studies have shown that people who develop a rash when using Tarceva or Tarceva with Gemzar tend to have better outcomes than those who do not develop a rash when using these drugs.

Roughly 10% of people develop a rash that requires a medication change. While your doctor may initially recommend the stronger dose, research shows that even at doses as low as 25 mg, Tarceva can effectively treat some cases of cancer.

Severe blistering skin rashes have occurred during clinical trials. This is an extremely rare side effect that has been compared to Stevens-Johnson syndrome, a potentially fatal condition that is caused by a severe allergic reaction to a medication.

Talk with your doctor before applying any creams or self-care products to treat a Tarceva rash.


Similar to diarrhea from chemotherapy, diarrhea from targeted therapy may result in malnutrition or dehydration, so it is important that you are treated for it. While there are many anti-diarrheal medications, never take any over-the-counter medications without first consulting with your doctor.

Other Side Effects

Other side effects of Tarceva may include:

Warnings and Interactions

While Tarceva usually leads to fewer side effects and complications than chemotherapy drugs, there are some risks associated with its use. Research shows that the following reactions may occur while using this medication.

  • Interstitial lung disease (ILD): This is estimated to occurs in 1.1% of patients.
  • Renal failure: This may result in dehydration.
  • Liver damage: Toxicity may or may not result in liver failure.
  • Gastrointestinal perforations: This may occur in the intestines or bowel.
  • Bullous and exfoliative skin disorders: This manifests as blisters or scaling of the skin.
  • Stroke: The risk of cerebrovascular accident (CVA) is higher in patients with pancreatic cancer.
  • Microangiopathic hemolytic anemia (MAHA): This condition is caused by the destruction of red blood cells, which leads to fatigue, jaundice, and other symptoms. The risk of MAHA is higher in patients with pancreatic cancer.
  • Ocular disorders: This may include corneal perforation, ulceration, or persistent severe keratitis.

For patients taking anticoagulants such as warfarin, there may be a risk for hemorrhage. Your doctor will regularly monitor you as a precaution.

Drug Resistance

While most patients with EGFR mutations respond well to Tarceva, they will also usually develop resistance at some point and the drug will stop working. Tagrisso (osimertinib), another tyrosine kinase inhibitor, may be recommended in place of Tarceva.

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