Afatinib

Name: Afatinib

Side Effects of Afatinib

The most common side effects include: 

  • diarrhea
  • rash
  • mouth sores
  • nail infection
  • dry skin
  • acne
  • decreased appetite
  • itching

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

Serious side effects may occur. See "Drug Precautions" section.

These are not all of the possible side effects of afatinib. For more information, ask your doctor or pharmacist.

Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Afatinib Usage

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

 

Afatinib Dosage

Take afatinib exactly as prescribed by your doctor. Follow the directions on your prescription label carefully.

The recommended dose of afatinib to treat advanced (metastatic) non-small cell lung cancer (NSCLC) is 40 mg orally once daily.

The dose will be reduced with severe renal dysfunction.

Afatinib Overdose

If you take too much afatinib, call your healthcare provider or local Poison Control Center, or seek emergency medical attention right away.

If afatinib is administered by a healthcare provider in a medical setting, it is unlikely that an overdose will occur. However, if overdose is suspected, seek emergency medical attention.

Other Requirements

  • 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  • Safely throw away (discard) any afatinib that is out of date or no longer needed.

 

Afatinib dosing information

Usual Adult Dose for Non-Small Cell Lung Cancer:

40 mg orally once a day

Duration of therapy: Until disease progression or no longer tolerated by patient.

Comments: Administer at least 1 hour before or 2 hours after a meal

afatinib Side Effects

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur:

More common
  • Bloody or cloudy urine
  • burning, dry, or itching eyes
  • diarrhea
  • difficult, burning, or painful urination
  • discharge or excessive tearing
  • fever
  • frequent urge to urinate
  • redness, pain, or swelling of the eye, eyelid, or inner lining of the eyelid
  • redness, swelling, or pain of the skin
  • scaling of the skin on the hands and feet
  • tingling of the hands and feet
  • ulceration of the skin
Less common
  • Cough
  • difficult breathing

Get emergency help immediately if any of the following symptoms of overdose occur:

Symptoms of overdose
  • Abdominal or stomach pain
  • dizziness
  • headache
  • lack or loss of strength
  • nausea
  • vomiting

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common
  • Blemishes on the skin
  • canker sores
  • chapped, red, or swollen lips
  • decreased appetite
  • decreased weight
  • dry skin
  • itching skin or rash
  • loosening of the fingernails
  • nosebleeds
  • pimples
  • redness or soreness around the fingernails
  • runny nose
  • scaling, redness, burning, pain, or other signs of inflammation of the lips
  • sores, ulcers, or white spots on the lips or tongue or inside the mouth

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

What are some side effects that I need to call my doctor about right away?

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

  • Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
  • Signs of kidney problems like unable to pass urine, change in how much urine is passed, blood in the urine, or a big weight gain.
  • Shortness of breath, a big weight gain, or swelling in the arms or legs.
  • Feeling tired or weak.
  • A heartbeat that does not feel normal.
  • Change in eyesight, eye pain, or very bad eye irritation.
  • If bright lights bother your eyes.
  • Pain when passing urine.
  • Redness or irritation of the palms of hands or soles of feet.
  • It is common to have loose stools (diarrhea) when taking this medicine. Some cases of loose stools may cause fluid loss and kidney problems that can sometimes be deadly. Call your doctor right away if you have loose stools that do not go away or if you have very loose stools. Do not try to treat loose stools without first checking with your doctor.
  • Very bad and sometimes deadly liver problems have happened with afatinib. Call your doctor right away if you have signs of liver problems like dark urine, feeling tired, not hungry, upset stomach or stomach pain, light-colored stools, throwing up, or yellow skin or eyes.
  • Very bad and sometimes deadly lung problems have happened with this medicine. The chance may be raised in people who are of Asian descent. Call your doctor right away if you have new or worsening lung or breathing problems like trouble breathing, shortness of breath, cough, or fever.
  • A very bad skin reaction (Stevens-Johnson syndrome/toxic epidermal necrolysis) may happen. It can cause very bad health problems that may not go away, and sometimes death. Get medical help right away if you have signs like red, swollen, blistered, or peeling skin (with or without fever); red or irritated eyes; or sores in your mouth, throat, nose, or eyes.

Contraindications

US labeling: There are no contraindications listed in the manufacturer’s labeling.

Canadian labeling: Hypersensitivity to afatinib or any component of the formulation.

Dosing Adult

Non-small cell lung cancer (NSCLC), metastatic, with EGFR exon 19 deletions or exon 21 (L858R) substitution mutations: Oral: 40 mg once daily until disease progression or unacceptable toxicity

NSCLC, metastatic squamous: Oral: 40 mg once daily until disease progression or unacceptable toxicity

Missed doses: Do not take a missed dose within 12 hours of next dose

Dosage adjustment for concomitant therapy:

P-gp inhibitors: If concomitant therapy is not tolerated, reduce afatinib daily dose by 10 mg. Upon discontinuation of the P-gp inhibitor, resume previous dose as tolerated.

P-gp inducers: Increase afatinib daily dose by 10 mg as tolerated if on chronic concomitant therapy with a P-gp inducer. Resume previous dose 2 to 3 days after discontinuation of P-gp inducer.

Dosing Geriatric

Refer to adult dosing.

Adverse Reactions

>10%:

Dermatologic: Acneiform eruption (≤70% to 90%; grade 3: ≤16%), skin rash (≤70% to 90%; grade 3: ≤16%), paronychia (11% to 58%), xeroderma (31%), pruritus (10% to 21%), cheilitis (12%)

Endocrine & metabolic: Decreased serum potassium (11% to 30%), weight loss (17%), hypokalemia (11%)

Gastrointestinal: Diarrhea (75% to 96%; grade 3: 15%; grades 3/4: 11% to 16%), stomatitis (30% to 71%), decreased appetite (25% to 29%), nausea (21% to 25%), vomiting (13% to 23%)

Genitourinary: Cystitis (13%)

Hematologic & oncologic: Abnormal lymphocytes (decreased: 38%; grades 3/4: 9%), decreased white blood cell count (12%; grades 3/4: 1%)

Hepatic: Increased serum ALT (10% to 54%; grades 3/4: 1% to 2%), increased serum alkaline phosphatase (34% to 51%; grades 3/4: 2% to 3%), increased serum AST (7% to 46%; grades 3/4: 1% to 3%), abnormal hepatic function tests (6% to 18%; grades 3/4: ≤4%), increased serum bilirubin (3% to 16%; grades 3/4: ≤1%)

Ophthalmic: Conjunctivitis (11%)

Renal: Decreased creatinine clearance (49%; grades 3/4: 2%)

Respiratory: Epistaxis (17%), rhinorrhea (11%)

Miscellaneous: Fever (12%)

1% to 10%:

Central nervous system: Fatigue (<2%)

Dermatologic: Palmar-plantar erythrodysesthesia (2% to 7%)

Ophthalmic: Keratitis (≤2%; grade 3: <1%)

Renal: Renal insufficiency (6%; grade 3: >1%)

Respiratory: Interstitial pulmonary disease (2%; grades 3/4: ≤1%), dyspnea (<2%)

Frequency not defined:

Endocrine & metabolic: Dehydration

Infection: Sepsis

Renal: Acute renal failure

Respiratory: Pneumonia

Miscellaneous: Physical health deterioration

<1% (Limited to important or life-threatening): Pancreatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis

Pregnancy Considerations

Based on animal reproduction studies and on the mechanism of action, afatinib may cause fetal harm if used during pregnancy. Women of reproductive potential should use highly-effective contraception during therapy and for at least 2 weeks after treatment has been discontinued.

Renal Dose Adjustments

-Mild Renal Dysfunction (CrCl 60 to 89 mL/min): No adjustment recommended.
-Moderate Renal Dysfunction (CrCl 30 to 59 mL/min): Closely monitor patients and adjust dose if not tolerated.
-Severe Renal Dysfunction (CrCl less than 30 mL/min): No data available. Closely monitor patients and adjust dose if not tolerated.

Dialysis

Data not available

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