Afatinib

Name: Afatinib

What is afatinib?

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

Afatinib is used to treat a certain type of non-small cell lung cancer that has spread to other parts of the body. Afatinib is used for this condition only if your tumor has a specific genetic marker for which your doctor will test.

Afatinib is also used to treat squamous non-small cell lung cancer that has spread to other parts of the body after other cancer medicine has been tried without successful treatment.

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

What is the most important information I should know about afatinib?

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.

What should I discuss with my healthcare provider before taking afatinib?

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.

What happens if I overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

What do I need to tell my doctor BEFORE I take Afatinib?

  • If you have an allergy to afatinib or any other part of afatinib.
  • If you are allergic to any drugs like this one, any other drugs, foods, or other substances. Tell your doctor about the allergy and what signs you had, like rash; hives; itching; shortness of breath; wheezing; cough; swelling of face, lips, tongue, or throat; or any other signs.
  • If you are breast-feeding. Do not breast-feed while you take this medicine and for 2 weeks after your last dose.

This medicine may interact with other drugs or health problems.

Tell your doctor and pharmacist about all of your drugs (prescription or OTC, natural products, vitamins) and health problems. You must check to make sure that it is safe for you to take afatinib with all of your drugs and health problems. Do not start, stop, or change the dose of any drug without checking with your doctor.

What are some things I need to know or do while I take Afatinib?

  • Tell all of your health care providers that you take this medicine. This includes your doctors, nurses, pharmacists, and dentists.
  • Have blood work checked as you have been told by the doctor. Talk with the doctor.
  • If you have upset stomach, throwing up, loose stools (diarrhea), or are not hungry, talk with your doctor. There may be ways to lower these side effects.
  • If you get diarrhea, you will need to make sure to avoid getting dehydrated. Drink plenty of fluids and watch for weight loss. Talk with your doctor.
  • You may get sunburned more easily. Avoid sun, sunlamps, and tanning beds. Use sunscreen and wear clothing and eyewear that protects you from the sun.
  • Very bad and sometimes deadly skin rashes have happened with afatinib. Talk to your doctor about any skin changes you may have.
  • This medicine may affect fertility. Fertility problems may lead to not being able to get pregnant or father a child. Talk with the doctor.
  • This medicine may cause harm to the unborn baby if you take it while you are pregnant.
  • Use birth control that you can trust to prevent pregnancy while taking this medicine and for at least 2 weeks after stopping the drug.
  • If you get pregnant while taking afatinib or within 2 weeks after your last dose, call your doctor right away.

If OVERDOSE is suspected

If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

Consumer Information Use and Disclaimer

  • If your symptoms or health problems do not get better or if they become worse, call your doctor.
  • Do not share your drugs with others and do not take anyone else's drugs.
  • Keep a list of all your drugs (prescription, natural products, vitamins, OTC) with you. Give this list to your doctor.
  • Talk with the doctor before starting any new drug, including prescription or OTC, natural products, or vitamins.
  • Some drugs may have another patient information leaflet. Check with your pharmacist. If you have any questions about afatinib, please talk with your doctor, nurse, pharmacist, or other health care provider.
  • If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about afatinib. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not specific medical advice and does not replace information you receive from the healthcare provider. You must talk with the healthcare provider for complete information about the risks and benefits of using afatinib.

Review Date: October 4, 2017

Index Terms

  • Afatinib Dimaleate
  • BIBW 2992

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Tablet, Oral:

Gilotrif: 20 mg

Gilotrif: 30 mg, 40 mg [contains fd&c blue #2 (indigotine)]

Pharmacologic Category

  • Antineoplastic Agent, Epidermal Growth Factor Receptor (EGFR) Inhibitor
  • Antineoplastic Agent, Tyrosine Kinase Inhibitor

Dosing Adjustment for Toxicity

Note: Permanently discontinue for intolerability or severe reaction occurring at a dose of 20 mg daily.

Cardiovascular: Permanently discontinue for symptomatic left ventricular dysfunction.

Dermatologic: Withhold therapy for prolonged (>7 days) or intolerable grade 2 or higher cutaneous reactions. Upon improvement to baseline or ≤ grade 1, resume therapy at 10 mg per day less than previous dose. Discontinue permanently for life-threatening bullous, blistering, or exfoliative skin lesions, as well as for suspected toxic epidermal necrolysis (TEN) or Stevens Johnson syndrome (SJS).

Gastrointestinal:

Diarrhea: Grade 2 or higher diarrhea that persists for ≥2 consecutive days despite antidiarrheal therapy: Interrupt therapy until resolution to ≤ grade 1, then resume at 10 mg per day less than previous dose.

Nausea/vomiting: For intolerable grade 2 or persistent (≥7 days) nausea/vomiting despite antiemetic therapy, the following recommendations have been made: Interrupt therapy for up to 14 days until resolution to ≤ grade 1, then resume at 10 mg per day less than previous dose; if symptoms do not resolve within 14 days, discontinue permanently (Giotrif Canadian product labeling 2016).

Ocular: Interrupt therapy for suspected keratitis; consider discontinuation if diagnosis of ulcerative keratitis is confirmed. Permanently discontinue for persistent ulcerative keratitis.

Pulmonary: Interrupt therapy for suspected interstitial lung disease (ILD); permanently discontinue if diagnosis is confirmed.

Other toxicity: Grade 3 or higher adverse reactions: Withhold therapy for ≥ grade 3 adverse reactions. Upon improvement to baseline or ≤ grade 1, resume therapy at 10 mg per day less than previous dose.

Drug Interactions

Aminolevulinic Acid (Systemic): Photosensitizing Agents may enhance the photosensitizing effect of Aminolevulinic Acid (Systemic). Avoid combination

Aminolevulinic Acid (Topical): Photosensitizing Agents may enhance the photosensitizing effect of Aminolevulinic Acid (Topical). Monitor therapy

CarBAMazepine: May decrease the serum concentration of Afatinib. Management: Per US labeling: if requiring chronic use of carbamazepine, increase afatinib dose by 10 mg as tolerated; reduce to original afatinib dose 2-3 days after stopping carbamazepine. Per Canadian labeling: avoid combination if possible. Consider therapy modification

Lumacaftor: May decrease the serum concentration of P-glycoprotein/ABCB1 Substrates. Lumacaftor may increase the serum concentration of P-glycoprotein/ABCB1 Substrates. Monitor therapy

Nelfinavir: May increase the serum concentration of Afatinib. Management: Per US labeling: reduce afatinib by 10 mg if not tolerated. Per Canadian labeling: avoid combination if possible; if used, administer nelfinavir simultaneously with or after the dose of afatinib. Consider therapy modification

P-glycoprotein/ABCB1 Inducers: May decrease the serum concentration of Afatinib. Management: Per US labeling: if requiring chronic use of P-gp inducers, increase afatinib dose by 10mg as tolerated; reduce to original afatinib dose 2-3 days after stopping P-gp inducers. Per Canadian labeling: avoid combination if possible. Consider therapy modification

P-glycoprotein/ABCB1 Inhibitors: May increase the serum concentration of Afatinib. Management: Per US labeling: reduce afatinib by 10mg if not tolerated. Per Canadian labeling: avoid combination if possible; if used, administer the P-gp inhibitor simultaneously with or after the dose of afatinib. Consider therapy modification

PHENobarbital: May decrease the serum concentration of Afatinib. Management: Per US labeling: if requiring chronic use of phenobarbital, increase afatinib dose by 10 mg as tolerated; reduce to original afatinib dose 2-3 days after stopping phenobarbital. Per Canadian labeling: avoid combination if possible. Consider therapy modification

Porfimer: Photosensitizing Agents may enhance the photosensitizing effect of Porfimer. Monitor therapy

Primidone: May decrease the serum concentration of Afatinib. Management: Per US labeling: if requiring chronic use of primidone, increase afatinib dose by 10 mg as tolerated; reduce to original afatinib dose 2-3 days after stopping primidonel. Per Canadian labeling: avoid combination if possible. Consider therapy modification

Saquinavir: May increase the serum concentration of Afatinib. Management: Per US labeling: reduce afatinib by 10 mg if not tolerated. Per Canadian labeling: avoid combination if possible; if used, administer saquinavir simultaneously with or after the dose of afatinib. Consider therapy modification

Tacrolimus (Systemic): May increase the serum concentration of Afatinib. Management: Per US labeling: reduce afatinib by 10 mg if not tolerated. Per Canadian labeling: avoid combination if possible; if used, administer tacrolimus simultaneously with or after the dose of afatinib. Consider therapy modification

Verteporfin: Photosensitizing Agents may enhance the photosensitizing effect of Verteporfin. Monitor therapy

Adverse Effects

All grades included unless otherwise noted

>10%

Diarrhea (75-96%)

Rash/dermatitis acneiform (90%)

Stomatitis (71%)

Paronychia (58%)

Dry skin (31%)

Decreased appetite (29%)

Pruritus (21%)

Epistaxis (17%)

Weight decreased (17%)

Diarrhea, grades 3 or 4 (11-15%)

Cystitis (13%)

Cheilitis (12%)

Pyrexia (12%)

Rhinorrhea (11%)

Conjunctivitis (11%)

Increased ALT (11%)

Hypokalemia (11%)

1-10%

Increased AST (8%)

Interstitial lung disease (1.5%)

<1%

Keratitis (0.8%)

Postmarketing Reports

Nausea/vomiting

Pancreatitis

Toxic epidermal necrolysis/Stevens Johnson syndrome

Administration

Oral Administration

Take PO on empty stomach, at least 1 hr before or 2 hr after a meal

In Summary

Commonly reported side effects of afatinib include: diarrhea, abnormal hepatic function tests, acneiform eruption, skin rash, and erythema. Other side effects include: palmar-plantar erythrodysesthesia, and renal insufficiency. See below for a comprehensive list of adverse effects.

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