Tarceva (Erlotinib) - Oral

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What Is Tarceva?

Tarceva (erlotinib) is a prescription oral medication used to treat lung cancer that has spread to other areas of the body (metastatic). It can also be used in combination with a chemotherapy called Gemzar (gemcitabine) to treat metastatic pancreatic cancer. Tarceva belongs to a class of medications called kinase inhibitors and works by targeting specific epidermal growth factor receptor (EGFR) pathways.

Tarceva is available in tablet form.

Drug Facts

  • Generic Name: Erlotinib
  • Brand Name(s): Tarceva
  • Drug Availability: Prescription
  • Therapeutic Classification: Antineoplastic agent
  • Available Generically: Yes
  • Controlled Substance: N/A
  • Administration Route: Oral
  • Active Ingredient: Erlotinib
  • Dosage Form(s): Tablet

What Is Tarceva Used For?

The Food and Drug Administration (FDA) has approved Tarceva to treat metastatic non-small cell lung cancer (NSCLC) with an EGFR exon 19 deletion or exon 21 substitution mutation. It can be used as the first therapy given, also known as first-line treatment, or after prior chemotherapy hasn’t worked.

Tarceva can also be given as a first-line treatment along with Gemzar to treat metastatic pancreatic cancer.

How to Take Tarceva

Take Tarceva on an empty stomach once a day. An empty stomach usually means one hour before eating or two hours after eating. Avoid eating grapefruit or drinking grapefruit juice while taking Tarceva. Grapefruit can increase the chance of side effects.

Storage

Store Tarceva in its original packaging and keep it at room temperature.

What Are the Side Effects of Tarceva?

This is not a complete list of side effects, and others may occur. A medical professional can advise you on side effects. If you experience other effects, contact your pharmacist or a medical professional. You may report side effects to the FDA at www.fda.gov/medwatch or 1-800-FDA-1088.

Tarceva is associated with some mild and severe side effects.

Common Side Effects

The most common side effects associated with taking Tarceva include:

  • Rash
  • Diarrhea (can usually be treated with anti-diarrhea medicine). Speak to your healthcare team.
  • Decreased appetite
  • Fatigue
  • Shortness of breath
  • Cough
  • Nausea
  • Vomiting

Severe Side Effects

Contact your healthcare provider right away if you have serious side effects. If you think your side effects are life-threatening or you are experiencing a medical emergency, call 911.

Serious side effects and their symptoms can include:

  • Interstitial lung disease: Worsening cough, shortness of breath, or fever that any other cause can’t explain
  • Renal failure: Dehydration, decreased kidney function found through blood work
  • Liver dysfunction: Elevated liver enzymes seen in blood work, abdominal pain
  • Gastrointestinal issues: Severe diarrhea, severe abdominal pain
  • Severe rash: Blistering skin lesions, peeling of the skin 
  • Eye disorders: Abnormal eyelash growth, decreased tears, severely dry eyes
  • Increased risk of bleeding: Easy bleeding when taken in combination with a blood thinner called warfarin

Long-Term Side Effects

Severe side effects that go untreated can potentially lead to long-term effects.

Report Side Effects

Tarceva may cause other side effects. Call your healthcare provider if you have any unusual problems while taking this medication.
If you experience a serious side effect, you or your provider may send a report to the Food and Drug Administration's (FDA) MedWatch Adverse Event Reporting Program or by phone (1-800-332-1088).

Dosage: How Much Tarceva Should I Take?

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The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

For oral dosage form (tablets):

For lung cancer:

  • Adults—150 milligrams (mg) once a day. Your doctor may adjust your dose as needed.
  • Children—Use and dose must be determined by your doctor.

For pancreas cancer:

  • Adults—100 milligrams (mg) once a day, taken with gemcitabine. Your doctor may adjust your dose as needed.
  • Children—Use and dose must be determined by your doctor.

Modifications

Discuss any occurrence of severe side effects with your medical oncology provider. They may need to adjust your dose of Tarceva or discontinue its use. Cigarette smoking can interfere with how Tarceva is absorbed in the body. If you smoke, your provider may increase the dose of Tarceva.

Missed Dose

If you miss a dose of Tarceva, you can take it when you remember as long as it is within 12 hours of the missed dose. Do not double up or take extra to make up for a completely missed dose.

Overdose: What Happens If I Take Too Much Tarceva?

Notify your healthcare team if you take too much Tarceva and quickly manage any symptoms that you experience.

What Happens If I Overdose On Tarceva?

If you think you or someone else may have overdosed on Tarceva (erlotinib), call a healthcare provider or the Poison Control Center (1-800-222-1222).

If someone collapses or isn't breathing after taking erlotinib, call 911 immediately.

Precautions

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It is very important that your doctor check your progress at regular visits to make sure this medicine is working properly. Blood and urine tests may be needed to check for unwanted effects.

Using this medicine while you are pregnant can harm your unborn baby. Use an effective form of birth control to keep from getting pregnant. You should continue to use birth control during treatment and for 1 month after your last dose. If you think you have become pregnant while using the medicine, tell your doctor right away.

It is important that you talk to your doctor right away if you have severe or continuing diarrhea, nausea, loss of appetite, or vomiting.

Call your doctor right away if you have unexplained shortness of breath, cough, and fever that comes on suddenly. These could be symptoms of a serious lung condition.

Check with your doctor right away if you have bloody or black, tarry stools, severe stomach pain, or vomiting of blood or material that looks like coffee grounds. These could be symptoms of a serious stomach or bowel problem.

Tell your doctor right away if you have dark urine or pale stools, yellow skin or eyes, nausea or vomiting, or upper stomach pain. These could be symptoms of a liver problem.

Kidney problems may occur while you are using this medicine. Tell your doctor right away if you have decreased urine output, dizziness, headache, irritability, rapid weight gain, seizures, swelling of the face, ankles, or hands, or unusual tiredness or weakness.

Serious skin reactions can occur with this medicine. Check with your doctor right away if you have blistering, peeling, or loosening of the skin, red skin lesions, severe acne or skin rash, sores or ulcers on the skin, or fever or chills while you are using this medicine.

You may use alcohol-free emollient creams, sunscreen, or sun blocking lotions to prevent dry skin and other serious skin reactions.

Check with your doctor right away if blurred vision or any vision change, eye pain, or eye irritation occurs during or after treatment. Your doctor may want you to have your eyes checked by an ophthalmologist (eye doctor).

Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines and herbal (eg, St. John's wort) or vitamin supplements.

What Are Reasons I Shouldn’t Take Tarceva?

People who are pregnant or breastfeeding should not take Tarceva.

What Other Medications Interact With Tarceva?

There are multiple medications and drug classes that can have interactions with Tarceva, including:

  • CYP3A4 inhibitors (e.g., clarithromycin, ketoconazole, and grapefruit): Your healthcare provider may recommend decreasing your dose of Tarceva if you take any of the medications in this class. 
  • CYP34A inducers (e.g., phenytoin, rifampin, phenobarbital, and St. Johns’ wort)
  • CYP1A2 inducers (e.g., rifampin, phenytoin, and cigarette smoking): You may need to increase your Tarceva dose if you use one of these medications or smoke cigarettes.
  • Proton pump inhibitors (e.g., Prilosec (omeprazole) and Protonix (pantoprazole): Do not take these with Tarceva if at all possible. 
  • H2 receptor antagonists and antacids (e.g., Tagamet (cimetidine), famotidine, ranitidine, and calcium carbonate): Do not take Tarceva 10 hours before and less than two hours after these medications. 

What Medications Are Similar?

There are other medications that target the EGFR pathway in lung cancer.

These medications include:

  • Gilotrif (afatinib)
  • Iressa (gefitinib)
  • Tagrisso (osimertinib)
  • Vizimpro (dacomitinib)

These are drugs that are also prescribed for the same condition. It is not a list of drugs recommended to take with Tarceva.

Frequently Asked Questions

  • What is Tarceva used for?

    Tarceva is a medication used to treat metastatic non-small cell lung cancer with an EGFR mutation. It is also used to treat metastatic pancreatic cancer in combination with a chemotherapy called Gemzar.

  • What drugs should not be taken with Tarceva?

    There are a number of medications that you should not take with Tarceva. Some of these include proton pump inhibitors such as omeprazole or pantoprazole, and other medications including rifampin, St. John’s wort, phenytoin, and phenobarbital.

  • What are the side effects of Tarceva?

    Side effects associated with Tarceva include diarrhea, skin rash, fatigue, nausea, vomiting, and loss of appetite. Report any other side effects that become severe to your healthcare team.

  • How do I safely stop taking Tarceva?

    Keep taking Tarceva as directed by your oncologist. Your doctor may recommend discontinuing use if Tarceva causes severe side effects or is no longer effective in treating the cancer.

How Can I Stay Healthy While Taking Tarceva?

Be sure to follow the directions and take Tarceva on an empty stomach. Take care of any side effects as they develop to prevent them from worsening.

Stay hydrated and take care of your skin by using alcohol-free moisturizing lotion regularly. Skin reactions can occur or worsen on sun-exposed areas, so use sunscreen or avoid being out in the sun. I

f you experience side effects and don’t know what to do, reach out to your oncology healthcare team.

Medical Disclaimer

Verywell Health's drug information is meant for education purposes only and not intended as a replacement for medical advice, diagnosis, or treatment from a healthcare professional. Consult your doctor before taking any new medication(s). IBM Watson Micromedex provides some of the drug content, as indicated on the page.

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2 Sources
Verywell Health uses only high-quality sources, including peer-reviewed studies, to support the facts within our articles. Read our editorial process to learn more about how we fact-check and keep our content accurate, reliable, and trustworthy.
  1. Food and Drug Administration. Tarceva (erlotinib) label. Updated October 2016.

  2. American Cancer Society. Targeted drug therapy for non-small cell lung cancer. Updated June 1, 2021.