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Erlotinib

(er-lot-tin-nib)

Trade/other name(s): Tarceva, OSI-774

Why would this drug be used?

This drug is used to treat pancreatic cancer and non-small cell lung cancer, and is being studied for use in other conditions as well.

How does this drug work?

Erlotinib is a type of targeted therapy known as a tyrosine kinase inhibitor. Its target is a tyrosine kinase protein called epidermal growth factor receptor (EGFR), which is located on the surface of certain cells in the body. Some cancers have higher than normal numbers of these receptors on their surfaces. Erlotinib blocks the receptor so that it can’t signal the cell to divide and grow.

Before taking this medicine

Tell your doctor…

  • If you are allergic to anything, including medicines, dyes, additives, or foods.
  • If you have any type of liver disease (including hepatitis). This drug is cleared from the body mainly by the liver. Reduced liver function may result in more drug staying in the body, which could lead to unwanted side effects. Your doctor may need to adjust your dose accordingly.
  • If you have ever had peptic ulcers, diverticulosis, or diverticulitis. People who have these conditions have an increased risk of developing perforations (holes) in the digestive tract while taking this drug.
  • If you smoke. Smoking may make erlotinib less effective.
  • If you have any other medical conditions such as kidney disease, heart disease, congestive heart failure, lung disease, diabetes, gout, or infections. These conditions may require that your medicine dose, regimen, or timing be changed.
  • If you are taking any blood-thinning medicines (see “Interactions with other drugs” below).
  • If you are pregnant, trying to get pregnant, or if there is any chance of pregnancy. This drug can cause problems with the fetus if taken at the time of conception or during pregnancy. If you’re sexually active and are taking this drug, you should use some kind of birth control during treatment and for at least 2 weeks afterward. Check with your doctor about what kinds of birth control can be used with this medicine. In pregnant women, treatment with this drug should be started or continued only if the potential benefit to the mother outweighs the risk to the fetus.
  • If you are breastfeeding. It is not known whether this drug passes into breast milk. If it does, it may affect the baby. Breastfeeding is not recommended during treatment with this drug.
  • If you think you might want to have children in the future. It is not known whether or not this drug can affect fertility. Talk with your doctor about the possible risk with this drug and the options that may preserve your ability to have children.
  • About any other prescription or over-the-counter medicines you are taking, including vitamins and herbs. In fact, keeping a written list of each of these medicines (including the doses of each and when you take them) with you in case of emergency may help prevent complications if you get sick.

Interactions with other drugs

The following drugs can cause erlotinib to build up in the body, raising the risk of serious side effects:

  • The antidepressants nefazodone (Serzone) and fluvoxamine (Luvox)
  • The antibiotics erythromycin (EES), clarithromycin (Biaxin), telithromycin (Ketek), and similar drugs
  • The antibiotic ciprofloxacin (Cipro)
  • Anti-fungal antibiotics such as ketoconazole (Nizoral), itraconazole (Sporanox), voriconazole (Vfend)
  • HIV drugs such as indinavir, ritonavir, fosamprenavir, nelfinavir, atazanavir, and others

Do not start or stop taking these medicines while on erlotinib without talking with the prescribing doctor(s) about all of the medicines you take, including erlotinib.

These drugs and supplements can lower the levels of erlotinib in the blood and make it less effective:

  • The anti-seizure drugs carbamazepine (Tegretol), phenobarbital (Luminal), and phenytoin (Dilantin)
  • The TB drugs rifampin (Rifadin, Rimactane; also in Rifamate and Rifater), and rifabutin (Mycobutin)
  • The steroid drug dexamethasone (Decadron)
  • St. John’s wort (an herbal dietary supplement)

If you need to take any of these drugs, your doctor may need to adjust your dose of erlotinib.

Smoking tobacco reduces the amount of erlotinib in your body. Be sure your doctor knows if you smoke. Tell the doctor right away if you stop smoking or start back smoking during treatment. Your dose may need to be adjusted.

Drugs commonly used to treat heartburn, reflux, or ulcers reduce acid levels in the stomach, which may affect the amount of erlotinib your body can absorb. Tell your doctor if you are taking:

  • An H2 blocker such as cimetidine (Tagamet), ranitidine (Zantac), famotidine (Pepcid), or nizatidine (Axid)
  • A proton pump inhibitor such as omeprazole (Prilosec), esomeprazole (Nexium), pantoprazole (Protonix), rabeprazole (Aciphex), or lansoprazole (Prevacid)

Antacids (Maalox, Mylanta, Tums, etc.) may affect the body’s ability to absorb erlotinib. If you are taking antacids, they should be taken at least 2 hours before or after you take erlotinib.

Any drugs or supplements that interfere with blood clotting can raise the risk of serious or even fatal bleeding during treatment with erlotinib. These include:

  • Vitamin E
  • Non-steroidal anti-inflammatory drugs (NSAIDs) such as aspirin, ibuprofen (Advil, Motrin), naproxen (Aleve, Naprosyn), and many others
  • Warfarin (Coumadin)
  • Ticlopidine (Ticlid), clopidogrel (Plavix), dabigatran (Pradaxa), rivaroxaban (Xarelto), or other blood thinners, including any type of heparin injections

Note that many cold, flu, fever, and headache remedies contain aspirin or ibuprofen. Ask your pharmacist if you aren’t sure what's in the medicines you take. If you take warfarin, your doctor will watch your clotting times closely while you are taking erlotinib.

There may be more drugs that interact with erlotinib. Check with your doctor, nurse, or pharmacist about any other medicines, herbs, and supplements you are taking, and whether alcohol can cause problems with this medicine.

Interactions with foods

Taking this drug with food can raise the levels of the drug in the body, so it should be taken on an empty stomach (see next section).

Avoid grapefruit or grapefruit juice during treatment. Grapefruit is known to affect the level of erlotinib in your blood. Check with your doctor, nurse, or pharmacist about whether other foods may be a problem.

Tell all the doctors, dentists, nurses, and pharmacists you visit that you are taking this drug.

How is this drug taken or given?

Erlotinib is in pill form, and is taken by mouth, once each day. The dose depends on a number of factors, including the type of cancer being treated. Take the dose as directed, at least 1 hour before or 2 hours after eating. It should be taken at about the same time each day. If you miss a dose, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double your daily prescribed dose. Let your doctor know if you miss a dose.

Take this drug exactly as directed by your doctor. If you do not understand the instructions, ask your doctor or nurse to explain them to you.

Store this drug in a tightly closed container away from heat and moisture and out of the reach of children and pets.

Precautions

It is common to develop a rash on the face, neck, and trunk during the first 2 weeks of treatment. The rash will likely go away once treatment is stopped. Tell your doctor if the rash bothers you or if it starts to get worse, especially if you notice any blistering. Avoid sunlight; cover up and wear sunscreen while receiving this drug. You can also try using moisturizing creams that don’t contain alcohol. Avoid acne treatments that dry the skin. Your doctor may need to stop the drug for a time or change your dose if the problem is severe.

Call your doctor if you have diarrhea. If left unchecked, this could lead to dehydration and chemical imbalances. Your doctor will likely prescribe medicine to help prevent or control this side effect. It is very important that you take this medicine as prescribed. Make sure you get the medicine right away, so that you will have it at home when you need it. Tell your doctor if the medicine doesn't stop the diarrhea.

Call your doctor if you have ongoing nausea, vomiting, or poor appetite.

Erlotinib can increase liver enzyme levels in your blood. Your doctor will likely check your liver function with blood tests on a regular basis. The drug may need to be stopped or the dose reduced if the changes are severe. If you have liver metastasis or other liver problems before starting treatment, the doctor may need to monitor you more carefully.

In rare cases, patients have developed severe lung disease during treatment. Tell your doctor right away if you notice any possible symptoms of lung problems, such as shortness of breath or cough.

Erlotinib may damage the outer parts (corneas) of your eyes. It may also lower your production of tears, cause inflammation of the eye, and make your eyelashes to grow longer. Tell your doctor right away if you notice any eye pain, redness, or irritation.

Call your doctor if you start or stop smoking tobacco. This medicine works better if you don’t smoke. Your dose may need to be adjusted.

Rarely, erlotinib can cause holes (perforations) in the digestive tract, which can be life-threatening. People who have had peptic ulcers, diverticulosis, or diverticulitis are at higher risk, as are people taking steroids, aspirin-like drugs, or certain other drugs used to treat cancer. It is important to tell your doctor or nurse right away if you develop severe stomach (abdominal) pain, and have nausea, constipation, or any other symptom with it.

This drug may rarely cause a fast-spreading rash and blistering or peeling of the skin (usually on the hands), sometimes along with swelling or sores in the mouth. This condition, known as Stevens-Johnson syndrome, can be severe or even life-threatening. Tell your doctor or nurse right away if you notice any new rashes, blistering or peeling of the skin, or mouth sores or swelling.

In rare cases, people taking erlotinib have had heart attacks or strokes. Because of the small number of cases involved, it is not known whether this was due to the drug. Still, it is important to tell your doctor if you have ever had blood clots or heart problems. Get help right away if you have chest or arm pain, or if you have trouble breathing, speaking, or moving.

Your doctor will likely test your blood throughout your treatment, looking for possible effects of the drug on blood counts or on blood chemistry levels. Based on the test results, you may be given medicines to help treat any effects. Your doctor may also need to reduce or delay your next dose of this drug, or even stop it altogether. Keep all your appointments for lab tests and doctor visits.

Avoid pregnancy while taking this drug and for at least 2 weeks afterward. Check with your doctor about this, and let your doctor know if you become pregnant or suspect pregnancy during treatment.

Possible side effects

You will probably not have most of the following side effects, but if you have any talk to your doctor or nurse. They can help you understand the side effects and cope with them.

Common

  • Skin rash on face, neck, and trunk*
  • Diarrhea*
  • Feeling tired
  • Poor appetite*
  • Nausea*

Less common

  • Shortness of breath
  • Cough
  • Fever
  • Vomiting*
  • Mouth sores
  • Infection
  • Back pain
  • Chest pain
  • Muscle or joint pain
  • Abnormal blood tests suggesting the drug is affecting the liver (Your doctor will discuss the importance of this finding, if any.)*
  • Itching
  • Dry skin
  • Eyelash and eyebrow changes
  • Eye problems such as redness, pain, inflammation of the eyes, and decreased tear production
  • Loose, brittle, or infected nails
  • Abnormal blood tests which suggest that the drug is affecting the liver (your doctor will discuss the importance of this finding, if any.)*

Rare

  • Abdominal pain
  • Damage to the lungs*
  • Hole (perforation) in the digestive tract*
  • Blistering or peeling of the skin, mouth sores*
  • Death due to lung damage, liver failure, kidney failure, heart attack, bleeding, or stroke

*See “Precautions” section for more detailed information.

There are some other side effects not listed above that can also occur in some patients. Tell your doctor or nurse if you develop these or any other problems.

FDA approval

Yes – first approved in 2004.

Disclaimer: This information does not cover all possible uses, actions, precautions, side effects, or interactions. It is not intended as medical advice, and should not be relied upon as a substitute for talking with your doctor, who is familiar with your medical needs.

Last Medical Review: 06/18/2014
Last Revised: 06/18/2014