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Trade/other name(s): Gilotrif

Why would this drug be used?

This drug is used to treat non-small cell lung cancers that have certain mutations (changes) in the EGFR gene. It is also being studied for use against other types of cancers.

How does this drug work?

Afatinib is a type of targeted therapy known as a kinase inhibitor. Kinases are proteins on or near the surface of a cell that transmit important signals to the cell’s control center. When cancer cells have certain mutations in a gene called EGFR, they make too much of the EGFR protein, which helps the cells grow and divide. Afatinib blocks the EGFR protein so that it can’t signal the cell to grow and divide.

Only a small portion of non-small cell lung cancers have one of the mutations in the EGFR gene that make this drug more likely to work. Your doctor will test your cancer cells to be sure they have one of these mutations before starting you on treatment with this drug.

Before taking this medicine

Tell your doctor…

  • If you are allergic to anything, including medicines, dyes, additives, or foods.
  • If you have any lung or breathing problems. Rarely, this drug can cause serious lung disease (see “Precautions”).
  • If you have any eye or vision problems, or if you wear contact lenses. This drug can cause eye problems or vision changes in some people (see “Precautions”).
  • If you have any type of liver disease (including hepatitis) or kidney disease. This drug is cleared from the body by the liver and kidneys. If these organs aren’t working well, your doctor might need to watch you more closely during treatment. This drug can also affect the liver (see “Precautions”).
  • If you have any heart problems, including congestive heart failure. This drug can damage the heart (see “Precautions”).
  • If you have any other medical conditions such as bleeding problems, gout, or infections. Your doctor may need to monitor you more closely during treatment.
  • 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. Women who could become pregnant need to follow special precautions if taking this drug (see “Precautions” below).
  • If you are breastfeeding. Although no studies have been done, this drug may pass into breast milk and affect the baby. Breastfeeding is not recommended during treatment with this drug.
  • If you think you might want to have children in the future. This drug might 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 or supplements you are taking, including vitamins and herbs. In fact, keeping a written list of these (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

Afatinib can interact with a number of drugs and supplements, so it is important to check with your health care team before taking any new medicines.

Certain drugs and supplements could lower the levels of afatinib in the blood, which might make it less effective. These include:

  • Some anti-seizure drugs, such as carbamazepine (Tegretol), phenobarbital (Solfoton), and phenytoin (Dilantin)
  • Some drugs to treat tuberculosis (TB), such as rifampin (Rifadin, Rimactane; also in Rifamate and Rifater)
  • St. John’s wort (an herbal dietary supplement)

Certain drugs and supplements could cause afatinib to build up in your blood, which might worsen side effects and other problems. These include:

  • Some antibiotics, such as erythromycin, clarithromycin (Biaxin), and similar drugs
  • Some anti-fungal medicines such as ketoconazole (Nizoral) and itraconazole (Sporanox)
  • Some drugs that affect the immune system, such as tacrolimus (Prograf) and cyclosporine
  • Some anti-HIV drugs such as ritonavir (Kaletra), nelfinavir (Viracept), and saquinavir (Invirase)
  • Some drugs used to treat heart or blood pressure problems, such as amiodarone, verapamil, and quinidine

If you need to take any of these drugs, your doctor might have to adjust your dose of afatinib. Do not start or stop taking any of these medicines while on afatinib without talking with the prescribing doctor(s) about all of the medicines you take, including afatinib.

Other medicines or supplements might also affect levels of afatinib in the body, and afatinib could affect the levels of some medicines. This might lead to unwanted side effects or other problems. 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 afatinib with food can affect the levels of the drug in the body, so it should be taken on an empty stomach (see next section).

Check with your doctor, nurse, or pharmacist about whether any specific foods might 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?

Afatinib is taken by mouth as a tablet. The usual starting dose is 40 mg (milligrams), taken once a day. The pill should be taken at the same time each day, at least 1 hour before or at least 2 hours after a meal. Your dose may need to be adjusted or delayed if you have side effects.

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. Keep the medicine in a tightly closed container away from heat and moisture and out of the reach of children and pets.


This drug often causes diarrhea. In some people this might be severe enough to cause loss of body fluid (dehydration), which could lead to kidney damage or even death if not treated. Your doctor will prescribe medicine for you to take if you have diarrhea. Make sure you get the medicine right away, so that you will have it at home when you need it, and be sure to take it exactly as directed. Let your doctor or nurse know if you have diarrhea while taking this drug, especially if it does not go away or if it becomes severe.

Most people who take this drug will have skin problems, such as rash, redness, infections, or hand-foot syndrome (pain, numbness, tingling, redness, swelling, and possibly skin peeling or sores on the hands or feet). A small portion of people could have severe skin problems such as blistering or skin peeling that might require medical care right away or could even be life-threatening. Let your doctor know right away if you notice any of the symptoms above.

A small portion of people might develop severe lung disease during treatment with this drug, which might require them to be in the hospital. Tell your doctor right away if you notice any possible symptoms of lung problems, such as shortness of breath, a new cough, or fever.

Afatinib can damage the liver. Your doctor will 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. Tell your doctor or nurse right away if you have possible symptoms of liver damage, such as yellowing of the eyes or skin (jaundice), dark urine, pain in the upper right part of your belly, easy bleeding or bruising, or feeling very tired.

This drug might cause eye problems in some people. Tell your doctor or nurse right away if you have eye pain, redness, swelling, or tearing, or if you notice sensitivity to light or have any changes in vision while taking this drug.

This drug can cause heart damage in some people. This can lead to congestive heart failure, which can cause symptoms such as a rapid heartbeat, shortness of breath, cough, feeling tired or dizzy, swelling in the hands or feet, or sudden weight gain. Tell your doctor or nurse right away if you develop any of these symptoms.

Women should avoid pregnancy while taking this drug and for at least 2 weeks after stopping it. This drug can cause problems with the fetus if taken at the time of conception or during pregnancy. Check with your doctor about what kinds of birth control can be used with this medicine. Tell your doctor right away if you become pregnant.

Possible side effects

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


  • Diarrhea*
  • Skin rash*
  • Mouth sores
  • Skin infection around the nails
  • Dry skin
  • Loss of appetite
  • Itchy skin

Less common

  • Nosebleeds
  • Weight loss
  • Bladder infection
  • Fever
  • Swelling or cracking of the lips
  • Runny nose
  • Conjunctivitis (pink eye)
  • Abnormal blood tests suggesting drug is affecting the liver (Your doctor will discuss the importance of this finding, if any.)*
  • Low blood potassium level (Your doctor will discuss the importance of this finding, if any.)
  • Severe diarrhea*


  • Vomiting
  • Kidney damage (resulting from severe diarrhea)*
  • Serious skin problems, such as blistering or peeling *
  • Lung damage*
  • Eye problems*
  • Heart damage*
  • Feeling very tired
  • Feeling very short of breath
  • Death due to lung disease, infection, or other causes

*See the “Precautions” section for more detailed information.

Other side effects not listed above 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 2013

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: 07/18/2013
Last Revised: 07/18/2013