Classes
DEA Class; Rx
Common Brand Names; Tarceva
- Antineoplastics, Tyrosine Kinase Inhibitor;
- Antineoplastics, EGFR Inhibitor
Description
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
Indications
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
Adverse Effects
- 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
Warnings
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
Pregnancy and Lactation
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
Maximum Dosage
NSCLC: 150 mg PO daily.
Pancreatic Cancer: 100 mg PO daily.
NSCLC: 150 mg PO daily.
Pancreatic Cancer: 100 mg PO daily.
Safety and efficacy have not been established.
Safety and efficacy have not been established.
How supplied
Erlotinib
tablet
- 25mg
- 100mg
- 150mg
