Afatinib

Afatinib is a prescription medication used to treat the symptoms of non-small cell lung cancer. 

• Afatinib is available under the following different brand names: Gilotrif

Common side effects of Afatinib include:

• Mild diarrhea for 1 day or less,
• Nausea,
• Vomiting,
• Loss of appetite,
• Mouth sores,
• Acne,
• Itching,
• Dry skin, and
• Redness, pain, swelling, or other signs of infection around the fingernails or toenails

Serious side effects of Afatinib include:

• Hives,
• Difficulty breathing,
• Swelling of the face, lips, tongue, or throat,
• New or worsening cough,
• Fever,
• Severe or ongoing diarrhea (lasting 2 days or longer),
• Severe skin reaction that causes blistering and peeling,
• Pain, redness, numbness, and peeling skin on the hands or feet,
• Blisters or ulcers in your mouth,
• Red or swollen gums,
• Trouble swallowing,
• Eye pain or redness,
• Blurred vision,
• Watery eyes,
• Feeling like something is in the eye,
• Increased sensitivity to light,
• Stomach pain (upper right side),
• Easy bruising,
• Unusual bleeding,
• Tiredness,
• Dark urine,
• Clay-colored stools,
• Yellowing of the skin or eyes (jaundice),
• Pounding heartbeats,
• Fluttering in your chest,
• Shortness of breath,
• Swelling in the legs and ankles, and
• Rapid weight gain

Rare side effects of Afatinib include:

• None

Seek medical care or call 911 at once if you have the following serious side effects:

• Severe headache, confusion, slurred speech, arm or leg weakness, trouble walking, loss of coordination, feeling unsteady, very stiff muscles, high fever, profuse sweating, or tremors;
• Serious eye symptoms such as sudden vision loss, blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights;
• Serious heart symptoms such as fast, irregular, or pounding heartbeats; fluttering in the chest; shortness of breath; sudden dizziness, lightheartedness, or passing out.

This is not a complete list of side effects and other serious side effects or health problems that may occur as a result of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

Adult dosage

Tablet

• 20 mg
• 30 mg
• 40 mg

Non-small cell lung cancer

Adult dosage

• Metastatic non-small cell lung cancer
  • 40 mg orally once a day until disease progression or is no longer tolerated by the patient
• Metastatic squamous non-small cell lung cancer
  • 40 mg orally once a day until disease progression or is no longer tolerated by the patient

Dosage considerations – should be given as follows: 

• See “Dosages”

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider, or pharmacist first.

• Afatinib has severe interactions with no other drugs.
• Afatinib has serious interactions with at least 60 other drugs.
• Afatinib has moderate interactions with at least 21 other drugs.
• Afatinib has minor interactions with no other drugs.

This information does not contain all possible interactions or adverse effects. Visit the RxList drug interaction checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist about all your products. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Check with your health care professional or doctor for additional medical advice, or if you have health questions or concerns.

Contraindications

• None

Effects of drug abuse

• None

Short-term effects

• See “what are side effects associated with using Afatinib?”

Long-term effects

• See “what are side effects associated with using Afatinib?”

Cautions

• May cause diarrhea that results in dehydration with or without renal impairment; some reported cases were fatal; withhold therapy for severe and prolonged diarrhea not responsive to antidiarrheal agents (see dosage modifications)
• Post marketing cases consistent with toxic epidermal necrolysis (ten), including bullous and exfoliative skin disorders, and stevens-johnson syndrome (SJS) reported; discontinue if life-threatening bullous, blistering, or exfoliating lesions occur; withhold therapy for severe and prolonged cutaneous reactions (see dosage modifications)
• May increase the risk for sunburn/phototoxicity; may worsen rash or acne; caution patients to limit sun exposure and wear sunscreen and protective clothing
• Interstitial lung disease (ILD) or ILD-like adverse reactions reported (.g, lung infiltration, pneumonitis, acute respiratory distress syndrome, alveolitis allergy) occurred in 1%, of these, 0.4% were fatal; discontinue therapy if ILD diagnosed (see dosage modifications)
• Hepatotoxicity reported; monitor with periodic liver testing; withhold or discontinue therapy for severe or worsening liver tests
• Keratitis, characterized as acute or worsening eye inflammation, lacrimation, light sensitivity, blurred vision, eye pain, and/or red eye occurred in 0.8%; withhold or discontinue therapy for confirmed ulcerative keratitis
• Gastrointestinal perforation, including fatal cases, reported; patients receiving concomitant corticosteroids, nonsteroidal anti-inflammatory drugs (NSAIDs) or anti-angiogenic agents, or patients with increasing age or who have an underlying history of gastrointestinal ulceration, underlying diverticular disease or bowel metastases may be at increased risk of perforation; permanently discontinue therapy in patients who develop gastrointestinal perforation
• Based on its mechanism of action, imatinib can cause fetal harm; advise pregnant women and females of reproductive potential of the potential risk to the fetus and to use effective contraception (see pregnancy)
• Drug interactions overview
  • See also dosage modifications
  • Coadministration of p-gp inhibitors (. g, ritonavir, cyclosporine a, ketoconazole, itraconazole, erythromycin, verapamil, quinidine, tacrolimus, nelfinavir, saquinavir, and amiodarone) with afatinib can increase exposure to afatinib
  • Coadministration of p-gp inducers (. g, rifampicin, carbamazepine, phenytoin, phenobarbital, and St. John’s wort) with afatinib can decrease exposure to afatinib

Pregnancy and Lactation

• Based on findings from animal studies and mechanism of action, therapy can cause fetal harm when administered to a pregnant woman; there is no available data on use in pregnant women; administration to pregnant rabbits during organogenesis at exposures approximately 0.2 times the exposure in humans at the recommended dose of 40 mg daily resulted in embryotoxicity and, in rabbits showing maternal toxicity, increased abortions at late gestational stages; advise pregnant women of the potential risk to a fetus
• Contraception
  • Advise females of reproductive potential to use effective contraception during treatment and for at least 2 weeks after the last dose of afatinib
  • Based on results from an animal fertility study, afatinib may reduce fertility in females and males of reproductive potential
  • Unknown if the effects on fertility are reversible
• Lactation
  • There are no data on the presence of afatinib in human milk or effects on breastfed infants or milk production; presence is shown in the milk of lactating rats; because of the potential for serious adverse reactions in nursing infants, advise a lactating woman not to breastfeed during treatment and for 2 weeks after the final dose