(redirected from Gilotrif)


(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.
Drug Guide, © 2015 Farlex and Partners
References in periodicals archive ?
The TKIs for lung cancer include drugs such as afatinib (Gilotrif), crizotinib (Xalkori), erlotinib (Tarceva) and gefitinib (Iressa).
The company said the US FDA approval extends the indications for use of its therascreen EGFR RGQ PCR Kit as a companion diagnostic to guide the use of Boehringer Ingelheim's targeted therapy GILOTRIF (afatinib) for first-line treatment of metastatic non-small cell lung cancer (NSCLC) with non-resistant epidermal growth factor receptor (EGFR) mutations.
Browse Non-Small Cell Lung Cancer (NSCLC) Therapeutics Market by Drug Classes (Angiogenesis Inhibitors - Avastin, Cyramza; Epidermal Growth Factor Receptor Blockers - Tarceva, Gilotrif, Iressa; Folate Antimetabolites - Alimta; Kinase Inhibitors - Xalkori, Zykadia; Microtubule Stabilizers - Abraxane, Docetaxel; and PD-1/ PD-L1 Inhibitors - Opdivo, Keytruda), and Clinical Pipeline Analysis of Phase 1, 2 and 3 Drugs (Avelumab, MPDL3280A, MEDI4736, Abemaciclib) and Forecast 2017-2021 at
Specifically, oral afatinib (Gilotrif) is approved for the first-line treatment for patients who have metastatic NSCLC with EGFR exon 19 deletions or exon 21 (L858R) substitution mutations as detected by an FDA-approved test.
Further, the FDA approved Gilotrif (afatinib) as a new oral treatment option for patients with squamous cell lung cancer, providing a new second-line treatment option for patients with the second largest sub-type of non-small cell lung cancer (NSCLC), representing about 20-30% of cases.
The seven new antineoplastic agents are adotrastuzumab emtansine (Kadcyla) for HER2-positive breast cancer; afatinib (Gilotrif) for non-small cell lung cancer; dabrafenib (Tafinlar) for unresectable or metastatic melanoma; ibrutinib (Imbruvica) for mantle cell lymphoma or chronic lymphocytic leukemia; obinutuzumab (Gazyva) for chronic lymphocytic leukemia; pomalidomide (Pomalyst) for multiple myeloma; and trametinib (Mekinist) for unresectable or metastatic melanoma.
The therascreen EGFR RGQ PCR kit is now approved as a companion diagnostic to guide the use of three FDA-approved therapies, including also GILOTRIF (Afatinib) from Boehringer Ingelheim and Iressa (Gefitinib) from AstraZeneca.
M2 EQUITYBITES-January 17, 2018-Boehringer announces expanded indication for Gilotrif for NSCLC patients whose tumors have certain EGFR mutations
The global non-small cell lung cancer therapeutics market report estimates the market size (Revenue USD million - 2013 to 2020) for key market segments based on the drug classes (angiogenesis inhibitors - Avastin, Cyramza; epidermal growth factor receptor blockers - Tarceva, Gilotrif, Iressa; Folate antimetabolites - Alimta; kinase inhibitors - Xalkori, Zykadia; microtubule stabilizers - Abraxane, Docetaxel; and PD-1/ PD-L1 inhibitors - Opdivo, Keytruda), clinical pipeline analysis of phase 1, 2 and 3 drugs (Avelumab, MPDL3280A, MEDI4736, Abemaciclib, etc.), and forecasts growth trends (CAGR% - 2016 to 2020).
In the current market, patients with non-squamous histology can be treated with more efficacious therapies such as Alimta (pemetrexed), while patients harboring activating mutations in EGFR or ALK can be prescribed targeted therapies such as Tarceva, Iressa, Xalkori and Gilotrif. Opdivo (nivolumab) - a mAb immune checkpoint inhibitor targeted towards Programmed cell Death (PD) 1 - is a recent market entrant, gaining approval for treating advanced or metastatic squamous NSCLC patients in Japan in 2015 and in Australia in 2016.