Name: Afatinib

What Is Afatinib?

Afatinib is a cancer medication that interferes with the growth and spread of cancer cells in the body.

Afatinib is used to treat non-small cell lung cancer that has spread to other parts of the body.

Afatinib may also be used for purposes not listed in this medication guide.

Follow all directions on your medicine label and package. Tell each of your healthcare providers about all your medical conditions, allergies, and all medicines you use.

You should not use afatinib if you are allergic to it.

To make sure afatinib is safe for you, tell your doctor if you have:

  • kidney disease;
  • liver disease;
  • heart disease;
  • breathing problems or lung disease other than cancer; or
  • vision problems, a history of very dry eyes, or if you wear contact lenses.

Do not use afatinib if you are pregnant. It could harm the unborn baby. Tell your doctor right away if you become pregnant during treatment. Use effective birth control to avoid pregnancy while you are using this medication and for at least 2 weeks after your treatment ends.

It is not known whether afatinib passes into breast milk or if it could harm a nursing baby. You should not breast-feed while using this medicine.

Afatinib Genetic Information

Non-small cell lung cancer (NSCLC) results from uncontrolled growth of cells in the lungs. Epidermal growth factor receptor (EGFR) is a protein found on the surface of cancer cells that controls the growth of cancer cells.

Some patients have mutations (changes) in this protein that lead cells to grow and divide more rapidly. Having these mutations increases the chance that afatinib will help slow or stop the growth of lung cancer cells. If testing for this mutation in EGFR is not done, afatinib is not likely to be an effective treatment.

Afatinib is FDA approved for the treatment of NSCLC carrying this EGFR mutation. Afatinib is targeted to this specific EGFR protein on cancer cells.


Uses of Afatinib

Afatinib is a prescription medicine used to treat people with advanced (metastatic) non-small cell lung cancer (NSCLC), 

  • that have certain types of abnormal epidermal growth factor receptor (EGFR) genes, and 
  • who have not had previous treatment for cancer that has spread to other parts of the body 

Afatinib is also used to treat advanced squamous cell lung cancer that has progressed after treatment with platinum-based chemotherapy.

This medication may be prescribed for other uses. Ask your doctor or pharmacist for more information.

Afatinib Drug Class

Afatinib is part of the drug class:

  • Protein kinase inhibitors

How should I take afatinib?

Before you start treatment, your doctor may perform tests to make sure afatinib is the best treatment for your type of lung cancer.

Afatinib is usually taken once per day. Follow all directions on your prescription label. Do not take this medicine in larger or smaller amounts or for longer than recommended.

Take afatinib on an empty stomach, at least 1 hour before or 2 hours after a meal.

Afatinib can cause severe diarrhea, which can be life-threatening if it leads to dehydration. You may be given medications to prevent or quickly treat diarrhea.

Your doctor may recommend you have an anti-diarrhea medicine such as loperamide (Imodium) available at all times while you are taking afatinib. Take the anti-diarrhea medicine as directed on the label, or as prescribed by your doctor.

Call your doctor if you are sick with severe diarrhea, or diarrhea lasting longer than 2 days. You may need to stop taking afatinib for a short time.

While using afatinib, you may need frequent blood tests.

Store the tablets in their original container at room temperature away from moisture, heat, and light. Keep the bottle tightly closed when not in use.

Throw away any afatinib tablets not used before the expiration date on the medicine label.

What should I avoid while taking afatinib?

Avoid exposure to sunlight or tanning beds. Afatinib can make you sunburn more easily. Wear protective clothing and use sunscreen (SPF 30 or higher) when you are outdoors.

This medicine can pass into body fluids (urine, feces, vomit). Caregivers should wear rubber gloves while cleaning up a patient's body fluids, handling contaminated trash or laundry or changing diapers. Wash hands before and after removing gloves. Wash soiled clothing and linens separately from other laundry.

Afatinib side effects

Get emergency medical help if you have signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat.

Stop using afatinib and call your doctor at once if you have:

  • severe skin reaction that causes blistering and peeling;

  • pain, redness, numbness, and peeling skin on your hands or feet;

  • blisters or ulcers in your mouth, red or swollen gums, trouble swallowing;

  • eye problems--eye pain or redness, blurred vision, watery eyes, feeling like something is in your eye, increased sensitivity to light;

  • heart problems--pounding heartbeats or fluttering in your chest, shortness of breath (even with mild exertion), swelling in your legs or ankles, rapid weight gain;

  • liver problems--nausea, upper stomach pain, tiredness, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes); or

  • lung problems--fever, chest pain, dry cough, wheezing.

Common side effects may include:

  • mild diarrhea for 1 day or less;

  • nausea, vomiting, loss of appetite;

  • mouth sores;

  • acne, dry skin, mild itching or skin rash; or

  • redness, pain, swelling, or other signs of infection around your fingernails or toenails.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Commonly used brand name(s)

In the U.S.

  • Gilotrif

Available Dosage Forms:

  • Tablet

Pharmacologic Class: Tyrosine Kinase Inhibitor

How do I store and/or throw out Afatinib?

  • Store in the original container at room temperature.
  • Protect from light.
  • Store in a dry place. Do not store in a bathroom.
  • Keep all drugs in a safe place. Keep all drugs out of the reach of children and pets.
  • Check with your pharmacist about how to throw out unused drugs.


(a FA ti nib)


Highly selective blocker of the ErbB family, including EGFR (ErbB1), HER2 (ErbB2), and HER4 (ErbB4); covalently and irreversibly binds to the intracellular tyrosine kinase domain, resulting in tumor growth inhibition and tumor regression. Inhibits autophosphorylation and proliferation (in vitro) in cell lines expressing both wild-type EGFR and selected EGFR mutations.


Decreased with high-fat meals


Covalently adducted to proteins and nucleophilic small molecules (minimal enzymatic metabolism) (Wind, 2013)


Feces (85%); urine (4%); primarily as unchanged drug

Time to Peak

2 to 5 hours

Half-Life Elimination

37 hours

Protein Binding


Special Populations Renal Function Impairment

A small pharmacokinetic study demonstrated a 50% increase and a 22% increase in mean AUCinf in patients with severe renal impairment (eGFR 15 to 29 mL/minute/1.73 m2) and moderate renal impairment (eGFR 30 to 59 mL/minute/1.73 m2), respectively, as compared to patients with normal renal function (eGFR 90 mL/minute/1.73 m2 or higher). Cmax was 22% higher in patients with severe renal impairment and was comparable in patients with moderate renal impairment as compared to patients with normal renal function.

Dosing Renal Impairment

Note: The manufacturer recommends using the Modification of Diet in Renal Disease (MDRD) formula to estimate the glomerular filtration rate (eGFR).

Preexisting impairment:

eGFR >30 mL/minute/1.73 m2: No dosage adjustment is necessary.

eGFR 15 to 29 mL/minute/1.73 m2: Reduce dose to 30 mg once daily.

eGFR <15 mL/minute/1.73 m2 and hemodialysis: There are no dosage adjustments provided in the manufacturer’s labeling (has not been studied).

Renal toxicity during treatment: If ≥ grade 2 renal toxicity occurs, withhold therapy. Upon improvement to baseline or ≤ grade 1, resume therapy at 10 mg per day less than previous dose.

Monitoring Parameters

EGFR mutation status; liver and renal function (periodically); monitor for skin toxicity, diarrhea, signs/symptoms of dehydration; monitor for signs/symptoms of interstitial lung disease (eg, acute respiratory distress syndrome, allergic alveolitis, lung infiltration, pneumonitis) and keratitis (eg, acute or worsening eye inflammation, blurred vision, eye pain, lacrimation, light sensitivity, red eye). Consider left ventricular ejection fraction assessment prior to and during therapy in patients with cardiac risk factors or conditions that may impair left ventricular function.

Liver Dose Adjustments

-Mild to Moderate Liver Dysfunction (Child-Pugh A or B): No adjustment recommended
-Severe Liver Dysfunction (Child-Pugh if available): No data available. Closely monitor patients and adjust dose if not tolerated.

Other Comments

Administration advice: Do not take a missed dose within 12 hours of the next dose. Take at least 1 hour before or 2 hours after a meal

Storage requirements: Dispense medication in the original container to protect from exposure to high humidity and light.

Afatinib Pregnancy Warnings

FDA pregnancy category: D Use of afatinib is not recommended unless the benefit outweighs the risk to the developing fetus. If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, the patient should be apprised of the potential hazard to the fetus. Comments: -Advise females of reproductive potential to use highly effective contraception during treatment, and for at least 2 weeks after the last dose of afatinib. -Advise patients to contact their healthcare provider if they become pregnant, or if pregnancy is suspected, while taking afatinib.