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(a-fa-ti-nib ) ,


(trade name)


Therapeutic: antineoplastics
Pharmacologic: kinase inhibitors
Pregnancy Category: D


First-line treatment of metastatic non-small cell lung cancer (NSCLC) where the tumor has a specific epidermal growth factor receptor (EGFR) deletion or substitution mutation detectable by an FDA-approved test.


Inhibits tyrosine kinases which results in slowed proliferation of specific tumor cell lines

Therapeutic effects

Decreased spread of NSCLC


Absorption: Well abosrbed (92%) following oral administration; absorption is decreased by high fat meal.
Distribution: Unknown
Metabolism and Excretion: Metabolites occur partly as protein-bound products. Excretion is primarily fecal (85%) as parent drug; 4% excreted in urine.
Half-life: 37 hr

Time/action profile (improved progression-free survival)

PO3 mos12 mos20 mos


Contraindicated in: Lactation: Discontinue drug or discontinue breast feeding; Obstetric: May cause fetal harm.
Use Cautiously in: Moderate-severe renal or hepatic impairment (dose adjustment may be necessary);genetic implication Asian ethnicity (may be ↑ susceptible to interstitial lung disease); Obstetric: Patients with child-bearing potential (highly effective contraception should be used during and for at least 2 wks after last dose); Pediatric: Safe and effective use in children has not been established.

Adverse Reactions/Side Effects

Ear, Eye, Nose, Throat

  • keratitis


  • interstitial lung disease (life-threatening)


  • hepatic toxicity (life-threatening)
  • diarrhea (most frequent)
  • ↓ appetite
  • stomatitis


  • cutaneous reactions (including bullous/blistering/exfoliating reactions, acneiform erruptions and palmar-plantar erythrodysesthesia)
  • dry skin
  • pruritus
  • paronychia
  • rash

Fluid and Electrolyte

  • hypokalemia


Drug-Drug interaction

Concurrent use of P-gp inhibitors including amiodarone, cyclosporine, erythromycin, itraconazole, ketoconazole, quinidineritonavir, saquinavir, tacrolimus, or verapamil ↑ blood levels and the risk of toxicity; dosage adjustment may be necessary (ritonavir may be given concurrently or 6 hr after).Concurrent use of P-gp inducers including carbamazepine, phenobarbital, phenytoinrifampicin or rifampin ↓ blood levels and may ↓ effectiveness; dosage adjustment may be necessary.


Oral (Adults) 40 mg/day; concurrent use of P-gp inhibitors—reduce dose by 10 mg/day if necessary; concurrent use of P-gp inducers—increase dose by 10 mg/day if necessary. Dose reductions recommended for various toxicities. Continue until disease progression or occurrence of unacceptable toxicity


Tablets: 20 mg, 30 mg, 40 mg

Nursing implications

Nursing assessment

  • Monitor for diarrhea; occurs frequently. Provide patient with an antidiarrheal agent (loperamide) at the onset of diarrhea and until diarrhea ceases for 12 hrs. If diarrhea is severe and lasts more than 48 hr despite use of antidiarrheal agent (Grade 2 or higher), withhold afatinib until diarrhea resolves to Grade 1 or less, then resume with reduced dose of 10 mg/day.
  • Assess for cutaneous reactions (bullous, blistering, exfoliative lesions; rash, erythema, acneiform rash) periodically during therapy. Discontinue afatinib if life-threatening lesions or prolonged Grade 2 cutaneous lesions lasting ≥7 days, intolerable Grade 2, or Grade 3 cutaneous reactions occur. Withhold afatinib until reaction resolves to Grade 1 or less and resume at 10 mg/day.
  • Monitor for signs and symptoms of interstitial lung disease (lung infiltration, pneumonitis, acute respiratory distress syndrome, allergic alveolitis; genetic implication may occur more commonly in patients of Asian ethnicity. Withhold afatinib if symptoms occur; discontinue if interstitial lung disease is confirmed.
  • Lab Test Considerations: Monitor liver function tests periodically during therapy. If severe decline in liver function occurs, discontinue afatinib. May cause ↑ AST and ALT.
    • May cause hypokalemia.

Potential Nursing Diagnoses

Diarrhea (Side Effects)


  • Oral: Administer once daily on an empty stomach, at least 1 hr before or 2 hrs after meals.

Patient/Family Teaching

  • Instruct patient to take afatinib as directed. Take missed dose as soon as remembered unless within 12 hrs of next dose, then omit and take next dose at scheduled time; do not double doses.
  • Caution patient to notify health care professional if signs and symptoms of keratitis (acute or worsening eye inflammation, lacrimation, light sensitivity, blurred vision, eye pain, and/or red eye) occur. Withhold if symptoms occur; if ulcerative keratitis is confirmed, discontinue afatinib. Advise patient that use of contact lenses is also a risk factor.
  • Advise patient to wear sunscreen and protective clothing during therapy to minimize risk of skin disorders.
  • Inform patient that diarrhea occurs in most patients and may cause dehydration and renal impairment. Notify health care professional if diarrhea is severe or persistent, if new or worsening lung symptoms (difficulty breathing, shortness of breath, cough, fever), symptoms of liver problems (yellow skin or whites of eyes, dark brown urine, pain on right side of abdomen, unusual bleeding or bruising, lethargy) or if symptoms of left ventricular dysfunction (shortness of breath, exercise intolerance, cough, fatigue, swelling or ankles or feet, palpitations, sudden weight gain) occur.
  • Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications.
  • Advise female patients to use highly effective contraception during and for at least 2 wks after last dose and to avoid breast feeding. If pregnancy occurs, instruct patient to notify health care professional immediately.

Evaluation/Desired Outcomes

  • Decreased spread of non-small cell lung cancer.
References in periodicals archive ?
For example, this past July, the FDA approved a diagnostic test in conjunction with the approval of Gilotrif (afatinib), which enables physicians to identify EGFR mutation-positive patients eligible for treatment with therapies that will respond well with the genetic mutation.
Withhold GILOTRIF during evaluation of patients with suspected ILD, and discontinueGILOTRIF in patients with confirmed ILD.
Our study forecasts revenues of these 11 brands: -- Alimta (pemetrexed) by Eli Lilly -- Avastin (bevacizumab) by Roche -- Tarceva (erlotinib) by Roche -- Iressa (gefitinib) by AstraZeneca -- Gilotrif (afatinib) by Boehringer Ingelheim -- Xalkori (crizotinib) by Pfizer -- Abraxane (paclitaxel Protein-Bound) by Celgene -- Taxotere (docetaxel) by Sanofi -- Cyramza (ramucirumab) by Eli Lilly -- Zykadia (ceritinib) by Novartis -- Opdivo (nivolumab) by Bristol-Myers Squibb.
How BMS's Opdivo, Astellas'/Roche's Tarceva, AstraZeneca's Iressa, Boehringer Ingelheim's Gilotrif and Vargatef, Pfizer's Xalkori, Novartis' Zykadia, Roche's Avastin and Eli Lilly's Cyramza are perceived by the medical community in terms of efficacy, tolerability, ease of administration, and other product attributes, and how they compare with other current and pipeline treatment options.
Under the pipeline assessment section of these reports, promising drugs in clinical development discussed include Gilotrif (afatinib) and Neratinib whereas promising drugs in early-stage development like Palbociclib, NeuVax (nelipepimut-S), Patritumab, Ganetespib, ARRY-380 (ONT-380) and NVP-BYL719 are also discussed.
The launch of premium-priced novel antibodies and immunotherapies in the first and second lines of therapy, including Boehringer Ingelheim's Gilotrif, Eli Lilly's necitumumab, Bristol-Myers Squibb's Yervoy (ipilimumab) and nivolumab, Pfizer's dacomitinib and Novartis's LDK378 are set to drive the market during the forecast period.
Pipeline Therapies Covered AbbVie veliparib (ABT 888) AstraZeneca olaparib (Lynparza) BioMarin Pharmaceutical talazoparib (BMN 673) Boehringer Ingelheim Gilotrif (afatinib) Eli Lilly abemaciclib (LY 2835219) Galena Biopharma NeuVax (nelipepimut-S) Merck & Co.
Our ongoing research program with Gilotrif and other compounds underscores our commitment to advancing the care of people affected by cancer, particularly lung cancer.
An early interim overall survival analysis of a randomized Phase 3 trial in HER2 positive metastatic breast cancer showed an increased mortality in patients receiving GILOTRIF in combination with vinorelbine compared to trastuzumab and vinorelbine.
Perception of current biomarker-driven therapies: Various therapies compete with each other in the same patient population, such as Genentech/Roche/Astella's Tarceva and Boehringer Ingelheim's Gilotrif for EGFR-mutant NSCLC, and Roche's Kadcyla and GlaxoSmithKline's Tykerb for HER2-positive breast cancer.
Gilotrif (afatinib) is a recently launched EGFR inhibitor with a novel mechanism of action that may delay the onset of resistance, and Zykadia (LDK378) is an ALK inhibitor in the late-stage pipeline that is set to treat Xalkori-resistant patients.