Afatinib

What is Afatinib?

• Afatinib (Gilotrif) is a kinase inhibitor used to treat people with non-small cell lung cancer (NSCLC).

What are the uses of this medicine?

This medicine is used to treat people with non-small cell lung cancer (NSCLC) that:

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

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.

Limitations of Use:

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

How does this medicine work?

• Afatinib (a fa' ti nib) is a small molecule tyrosine kinase receptor inhibitor with potent activity against epidermal growth factor receptor 2 (EGFR2 or ErbB1) and human epidermal growth factor receptor 2 (HER2 or ErbB2).
• These tyrosine kinase receptors are often mutated and over expressed in tumor tissue and cause unregulated cell growth and proliferation.
• Inhibition of the unregulated receptor can lead to reversal of progression of the cancer, although clinical responses are sometimes limited by the development of tumor resistance caused by further mutations in the receptor gene.
• In several large controlled trials, afatinib was shown to improve progression-free survival in patients with non-small cell lung cancer (NSCLC) with mutated EGFR2.
• Afatinib has also shown promise in therapy of some cases of advanced breast cancer.

Who Should Not Use this medicine ?

Limitations of Use:

• Safety and efficacy of Gilotrif were not established in patients whose tumors have resistant EGFR mutations

What drug interactions can this medicine cause?

• Co-administration of P-gp inhibitors can increase afatinib exposure. Reduce Gilotrif by 10 mg per day if not tolerated.
• Co-administration of chronic P-gp inducers orally can decrease afatinib exposure. Increase Gilotrif by 10 mg per day as tolerated.

Is this medicine FDA approved?

• FDA approved this drug in the year of 2013.

How should this medicine be used?

• Select patients for first-line treatment of metastatic NSCLC with Gilotrif based on the presence of non-resistant EGFR mutations in tumor specimens.

Recommended Dosage:

• The recommended dosage of Gilotrif is 40 mg orally once daily until disease progression or no longer tolerated by the patient.

Dosage Modification for Pre-Existing Severe Renal Impairment

• The recommended dosage of Gilotrif in patients with pre-existing severe renal impairment (estimated glomerular filtration rate [eGFR*] 15 to 29 mL/min /1.73 m2) is 30 mg orally once daily.

• Reduce Gilotrif daily dose by 10 mg if not tolerated for patients who require therapy with a P-glycoprotein (P-gp) inhibitor.
• Increase Gilotrif daily dose by 10 mg as tolerated for patients who require chronic therapy with a P-gp inducer.

Administration

• Take Gilotrif exactly as your doctor tells you to take it.
• Your doctor will tell you how many Gilotrif tablets to take and when to take them. Do not change your dose or stop Gilotrif unless your doctor tells you to.
• Take Gilotrif on an empty stomach at least 1 hour before a meal or 2 hours after a meal.
• If you miss a dose of Gilotrif, 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 Gilotrif at the same time.
• If you take too much Gilotrif, call your doctor or go to the nearest hospital emergency room right away.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form: As Tablets: 40 mg, 30 mg, and 20 mg

This medicine is available in fallowing brand namesː

• Gilotrif

What side effects can this medication cause?

The most common side effects of this medicine include:

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

Gilotrif may cause serious side effects, including:

• diarrhea
• skin reactions
• lung or breathing problems
• liver problems
• tear (perforation) in your stomach or intestine
• eye problems
• heart problems

What special precautions should I follow?

• Diarrhea may result in dehydration and renal failure. Withhold Gilotrif for severe and prolonged diarrhea not responsive to anti-diarrheal agents.
• Severe bullous, blistering, and exfoliating lesions occurred in 0.2% of patients. Discontinue for life-threatening cutaneous reactions. Withhold Gilotrif for severe and prolonged cutaneous reactions.
• Interstitial lung disease or ILD-like adverse reactions (e.g., lung infiltration, pneumonitis, acute respiratory distress syndrome, or alveolitis allergic) occurs in 1.6% of patients. Withhold Gilotrif for acute onset or worsening of pulmonary symptoms. Discontinue Gilotrif if ILD is diagnosed.
• Fatal hepatic impairment occurs in 0.2% of patients. Monitor with periodic liver testing. Withhold or discontinue Gilotrif for severe or worsening liver tests.
• Gastrointestinal perforation, including fatal cases, has occurred with Gilotrif. Permanently discontinue Gilotrif in patients who develop gastrointestinal perforation.
• Keratitis, characterized as acute or worsening eye inflammation, lacrimation, light sensitivity, blurred vision, eye pain, and/or red eye occurred in 0.7% of patients treated with Gilotrif. Withhold Gilotrif for keratitis evaluation. Withhold or discontinue Gilotrif for confirmed ulcerative keratitis.
• Gilotrif Can cause fetal harm when administered to a pregnant woman. Advise pregnant women and females of reproductive potential of the potential risk to the fetus and to use effective contraception.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• nausea
• vomiting
• asthenia
• dizziness
• headache
• abdominal pain
• elevated amylase

• Management of overdosage may include supportive care.

Can this medicine be used in pregnancy?

• Based on findings from animal studies and its mechanism of action, Gilotrif can cause fetal harm when administered to a pregnant woman.
• There are no available data on the use of Gilotrif in pregnant women.

Can this medicine be used in children?

• Safety and effectiveness of Gilotrif in pediatric patients have not been established.

What are the active and inactive ingredients in this medicine?

• 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).

Who manufactures and distributes this medicine?

Distributed by: Boehringer Ingelheim Pharmaceuticals, Inc. Ridgefield

Licensed from: Boehringer Ingelheim International GmbH

• Gilotrif is a registered trademark of and used under license from Boehringer Ingelheim International GmbH.

What should I know about storage and disposal of this medication?

• Store at 25°C (77°F); excursions permitted to 15°-30°C (59°-86°F).
• Dispense medication in the original container to protect from exposure to high humidity and light.

• Dailymed label info on Afatinib
• FDA Afatinib

Afatinib Resources
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