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Afatinib

Generic name: afatinib
Brand name: Gilotrif
Dosage form: oral tablet
Drug class: Multikinase inhibitors

Medically reviewed by N. France, BPharm. Last updated on Apr 12, 2022.

What is afatinib?

Afatinib is a cancer drug used to treat non-small cell lung cancer (NSCLC) that is EGFR (epidermal growth factor receptor)-positive, which means that it is caused by an abnormal EGFR gene or genes.

The EGFR protein is found on the surface of cells and helps them to grow, but when the gene for EGFR is defective or abnormal cells can grow out of control causing cancer.

Afatinib belongs to a class of drugs called kinase inhibitors. It is an EGFR tyrosine kinase inhibitor that works by irreversibly blocking EGFR.

Afatinib helps to stop or slow the spread of cancer and may help people with EGFR-positive NSCLC live longer. It was approved by the US Food and Drug Administration in 2013.

What is Afatinib used for?

Afatinib is a prescription medicine that is used to treat people with NSCLC that:

  • has certain (non-resistant) abnormal EGFR gene(s). Your healthcare provider will perform a test to make sure that afatinib is right for you.
  • has spread to other parts of the body (metastatic), and
  • has not been previously treated for metastatic lung cancer

It is not known if afatinib is safe and effective in treating people with lung cancer that has resistant abnormal EGFR genes.

or

is used to treat people with squamous cell lung cancer that:

  • has spread to other parts of the body, and
  • has been previously treated with chemotherapy that contains platinum.

It is not known if afatinib is safe and effective in children.

What should I tell my doctor before taking afatinib?

Before you take afatinib, tell your healthcare provider about all of your medical conditions, including if you:

  • have kidney or liver problems
  • have lung or breathing problems other than lung cancer
  • have a history of an ulcer, a tear (perforation) in your stomach or intestine, or diverticular disease (inflammation) in parts of your large intestine. See “What are the side effects of afatinib?” below
  • have a history of severe dry eye or any other eye problems. Tell your healthcare provider if you wear contact lenses.
  • have heart problems

How should I take afatinib?

  • Take afatinib exactly as your healthcare provider tells you to take it.
  • Your healthcare provider will tell you how many afatinib tablets to take and when to take them. Do not change your dose or stop afatinib unless your healthcare provider tells you to.
  • Take afatinib on an empty stomach at least 1 hour before a meal or 2 hours after a meal.

What happens if I miss a dose?

If you miss a dose of afatinib, take it as soon as you remember. If it is within 12 hours of your next dose, skip the dose and just take your next dose at your regular time. Do not take 2 doses of afatinib at the same time.

What happens if I overdose?

If you take too much afatinib, call your healthcare provider or go to the nearest hospital emergency room right away.

What should I avoid while taking afatinib?

Limit your time in the sun. afatinib can make your skin sensitive to sunlight. You could get or have worsening rash or acne. You could get a severe sunburn. Use sunscreen and wear a hat and clothes that cover your skin if you have to be in sunlight during treatment with afatinib.

Dosing information

  • The recommended dose of afatinib is 40 mg orally once daily.
  • In patients with severe renal impairment the recommended dose of afatinib is 30 mg orally once daily
  • Take afatinib at least 1 hour before or 2 hours after a meal
  • See full prescribing information for further dosing information

What are the side effects of afatinib?

Afatinib may cause serious side effects, including:

  • diarrhea. Diarrhea is common with afatinib and may sometimes be severe. Severe diarrhea can cause loss of too much body fluid (dehydration) and kidney problems that can sometimes lead to death. During your treatment with afatinib, your healthcare provider should prescribe medicines to treat diarrhea. Take this medicine exactly as your healthcare provider tells you to. Tell your healthcare provider if you have diarrhea. Get medical attention right away if your diarrhea does not go away or becomes severe.
  • skin reactions. Afatinib can cause redness, rash, and acne. It is important to get treatment for skin reactions as soon as you notice them. Take medicines to help skin reactions exactly as your healthcare provider tells you to. Get medical attention right away if you develop severe skin reactions such as peeling or blistering of the skin, or blisters in your mouth.
  • lung or breathing problems. Afatinib may cause inflammation of the lung that may lead to death. Symptoms may be similar to those symptoms from lung cancer. Tell your healthcare provider right away if you have any new or worsening lung problems, or any combination of the following symptoms: trouble breathing or shortness of breath, cough, or fever.
  • liver problems. Afatinib can cause liver problems that can sometimes lead to death. Tell your healthcare provider right away if you have any symptoms of a liver problem which may include:
    • yellowing of your skin or the white part of your eyes (jaundice)
    • dark or brown (tea colored) urine
    • pain on the upper right side of your stomach area (abdomen)
    • bleeding or bruising more easily than normal
    • feeling very tired
      Your healthcare provider will do blood tests to check your liver function during your treatment with afatinib.
  • tear (perforation) in your stomach or intestine. Tears in your stomach or intestine can happen with afatinib and can sometimes lead to death. Your risk of developing a tear in your stomach or intestine may be increased if you:
    • take certain medicines with afatinib including: corticosteroids, nonsteroidal anti-inflammatory drugs (NSAIDS), and certain other medicines.
    • have a history of stomach or intestinal ulcers, or if you have had diverticular disease (inflammation in parts of the large intestine).
      Get medical help right away if you develop severe stomach-area (abdomen) pain during treatment with afatinib.
  • eye problems. Tell your healthcare provider right away if you have symptoms of eye problems which may include:
    • eye pain, swelling, redness, or tearing
    • blurred vision
    • sensitivity to light
    • other changes in your vision
  • heart problems. Tell your healthcare provider right away if you have symptoms of a heart problem which may include:
    • new or worsening shortness of breath while at
    • rest or with activity
    • cough
    • tiredness
    • swelling of your ankles, feet, or legs
    • feeling that your heart is pounding or
    • racing (palpitations)
    • sudden weight gain

Your healthcare provider may change your dose, temporarily stop or permanently stop treatment with afatinib if you have certain side effects.

The most common side effects of afatinib include:

  • diarrhea
  • rash
  • acne
  • mouth sores
  • nail inflammation
  • dry skin
  • decreased appetite
  • nausea
  • vomiting
  • itching

Afatinib may cause decreased fertility in females and males. This may affect your ability to have a child. Talk to your healthcare provider if this is a concern for you.

Tell your healthcare provider if you have any side effect that bothers you or that does not go away.

These are not all of the possible side effects of afatinib. For more information, ask your healthcare provider or pharmacist. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA1088.

Interactions

Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements. Afatinib may affect the way other medicines work, and other medicines may affect the way afatinib works. Taking certain medicines with afatinib may increase your risk of developing a tear (perforation) in your stomach or intestine. See “What are the side effects of afatinib?” above.

Know the medicines you take. Keep a list of them to show your healthcare provider or pharmacist when you get a new medicine.

Pregnancy and breastfeeding

Tell your doctor if you are pregnant or plan to become pregnant. Afatinib can harm your unborn baby.

Females who are able to become pregnant should use effective birth control during treatment with afatinib. and for at least 2 weeks after your last dose of afatinib. Talk to your healthcare provider about birth control methods that may be right for you.

Tell your healthcare provider right away if you become pregnant or think you are pregnant during treatment with afatinib.

Tell your doctor if you are breastfeeding or plan to breastfeed. It is not known if afatinib passes into your breast milk. Do not breastfeed during treatment with afatinib and for 2 weeks after your last dose of afatinib. Talk to your healthcare provider about the best way to feed your baby if you take afatinib.

Storage

  • Store afatinib at room temperature between 68°F to 77°F (20°C to 25°C).
  • Keep afatinib in the original container and keep the container tightly closed.
  • Keep afatinib away from moisture and light.
  • Safely throw away (discard) any afatinib that is out of date or no longer needed.

Keep afatinib and all medicines out of the reach of children.

What are the ingredients in afatinib?

Active ingredient: afatinib

Inactive ingredients:

Tablet Core: lactose monohydrate, microcrystalline cellulose, crospovidone, colloidal silicon dioxide, magnesium stearate.

Tablet Coating: hypromellose, polyethylene glycol, titanium dioxide, talc, polysorbate 80, FD&C Blue No. 2 (40 mg and 30 mg tablets only).

Afatinib is distributed under the brandname Gilotrif by Boehringer Ingelheim Pharmaceuticals, Inc. Ridgefield, CT 06877 USA.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.