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Erlotinib

    Brands

    DEA Class; Rx

    Common Brand Names; Tarceva

    • Antineoplastics, Tyrosine Kinase Inhibitor; 
    • Antineoplastics, EGFR Inhibitor

    Oral epidermal growth factor receptor-tyrosine kinase inhibitor (EGFR-TKI)
    Used for the treatment of metastatic non-small cell lung cancer (NSCLC) with exon 19 deletions or exon 21 (L858R) substitution mutations as monotherapy, and for the treatment of locally advanced, unresectable, or metastatic pancreatic cancer with gemcitabine
    Periodically monitor liver function, renal function, and electrolytes during treatment

    Indicated for patients with metastatic non-small cell lung cancer (NSCLC) whose tumors have epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 (L858R) substitution mutations as detected by an FDA-approved test receiving first-line, maintenance, or ≥second-line treatment after progression following at least 1 prior chemotherapy regimen

    Indicated for first-line treatment in patients with locally advanced, unresectable, or metastatic pancreatic cancer

    —

    • Rash (75-76%)
    • Anorexia (52-69%)
    • Diarrhea (54-55%)
    • Fatigue (52-79%)
    • Nausea (33-40%)
    • Infection (39%)
    • Vomiting (23-25%)
    • Dyspnea (24%)
    • Stomatitis (17-19%)
    • Cough (16%)
    • Pruritus (13%)
    • Conjunctivitis (12%)
    • Dry skin (12%)
    • Keratoconjunctivitis sicca (12%)
    • Abdominal pain (11%)
    • Elevated LFT’s (grade 2)
    • Acne
    • Paronychia
    • Weight loss
    • Pneumonitis pulmonary infiltrate
    • Pulmonary fibrosis

    Risk of potentially fatal interstitial lung disease (ILD); withhold therapy for acute onset of new or progressive unexplained pulmonary symptoms, such as dyspnea, cough and fever; discontinue therapy if ILD diagnosed

    Potentially fatal GI perforations

    Severe bullous, blistering, or exfoliating skin conditions

    Ocular disorders include decreased tear production, abnormal eyelash growth, corneal perforation/ulceration, keratoconjunctivitis sicca, keratitis

    Diarrhea

    Smoking reduces erlotinib plasma concentration; advise patient to quit smoking

    Monitor renal function and electrolytes, particularly in patients at risk of dehydration; withhold therapy for severe renal toxicity

    Hepatotoxicity with or without hepatic impairment including hepatic failure and hepatorenal syndrome; monitor periodic liver testing; withhold or discontinue therapy for severe or worsening liver tests

    Coadministration with CYP3A4 inhibitors/inducers

    CYP1A2 inducers may decrease plasma concentration

    Risk of myocardial infarction (MI)/ischemia is increased in patients with pancreatic cancer

    Risk of cerebrovascular accident is increased in patients with pancreatic cancer

    Risk of microangiopathic hemolytic anemia (MAHA) is increased in patients with pancreatic cancer

    No evidence drug has any benefit after disease progression

    Monitor if on warfarin or other coumarin-derived anticoagulants for changes in PT/INR

    Based on animal data and its mechanism of action, erlotinib can cause fetal harm when administered to a pregnant woman

    No data exist on the presence of erlotinib in human milk, or the effects of erlotinib on the breastfed infant or on milk production

    Adults

    NSCLC: 150 mg PO daily.
    Pancreatic Cancer: 100 mg PO daily.

    Geriatric

    NSCLC: 150 mg PO daily.
    Pancreatic Cancer: 100 mg PO daily.

    Adolescents

    Safety and efficacy have not been established.

    Children

    Safety and efficacy have not been established.

    Erlotinib 

    tablet

    • 25mg
    • 100mg
    • 150mg