Drug Detail:Erlotinib (Erlotinib)
Drug Class: EGFR inhibitors
Usual Adult Dose for Non-Small Cell Lung Cancer
150 mg orally once a day on an empty stomach (at least 1 hour before or 2 hours after food)
- Duration of therapy: Until disease progression or unacceptable toxicity
Use: 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 receiving first-line, maintenance, or second or greater line treatment after progression following at least one prior chemotherapy regimen
Usual Adult Dose for Pancreatic Cancer
100 mg orally once a day on an empty stomach (at least 1 hour before or 2 hours after food)
- Duration of therapy: Until disease progression or unacceptable toxicity
Use: For first-line treatment of patients with locally advanced, unresectable or metastatic pancreatic cancer, in combination with gemcitabine
Renal Dose Adjustments
Dose adjustment(s) may be required; however, no specific guidelines have been suggested. Caution recommended.
Liver Dose Adjustments
Therapy should be interrupted or discontinued if:
- Total serum bilirubin doubles and/or serum transaminases triple in patients with baseline hepatic impairment
- Total serum bilirubin is greater than 3 times the upper limit of normal (3 x ULN) and/or serum transaminases are greater than 5 x ULN in patients with normal pretreatment values.
Dose Adjustments
Discontinue therapy for:
- Interstitial Lung Disease (ILD)
- Severe hepatic toxicity that does not improve significantly or resolve within 3 weeks
- GI perforation
- Severe bullous, blistering, or exfoliating skin conditions
- Corneal perforation or severe ulceration
Interrupt therapy:
- During diagnostic evaluation for ILD
- In patients with preexisting hepatic impairment or biliary obstruction for doubling of bilirubin or tripling of transaminases values over baseline; consider discontinuing therapy
- In patients without preexisting hepatic impairment for total bilirubin levels greater than 3 x ULN or transaminases greater than 5 x ULN; consider discontinuing therapy
- For severe (CTCAE grade 3 to 4) renal toxicity; consider discontinuing therapy
- For persistent severe diarrhea not responsive to medical management (e.g., loperamide)
- For severe rash not responsive to medical management
- For Grade 3 or 4 keratitis or Grade 2 keratitis lasting more than 2 weeks
- For acute/worsening ocular disorders such as eye pain; consider discontinuing therapy
If severe reactions occur with concomitant use of strong CYP450 3A4 inhibitors (e.g., atazanavir, clarithromycin, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin, troleandomycin, voriconazole), or grapefruit or grapefruit juice, or when using concomitantly with an inhibitor of both CYP450 3A4 and CYP450 1A2 (e.g., ciprofloxacin): Reduce dose by 50 mg decrements and avoid concomitant use if possible
Concomitant use with CYP450 3A4 inducers (e.g., rifampin, rifabutin, rifapentine, phenytoin, carbamazepine, phenobarbital, St. John's Wort: Increase dose by 50 mg increments every 2 weeks to a maximum dose of 450 mg as tolerated; avoid concomitant use if possible
Concurrent cigarette smoking: Increase the dose by 50 mg every 2 weeks to a maximum dose of 300 mg. Upon cessation of smoking, immediately reduce dose to the recommended dose (150 mg or 100 mg daily)
Proton pump inhibitors: Avoid concomitant use if possible; separation of doses may not eliminate the interaction since proton pump inhibitors affect the pH of the upper GI tract for an extended period
H2-receptor antagonists: Erlotinib must be taken 10 hours after the H2-receptor antagonist and at least 2 hours before the next dose of the H2-receptor antagonist
Antacids: The antacid dose and the dose of erlotinib should be separated by several hours, if an antacid is necessary; the effect of antacids on erlotinib pharmacokinetics has not been evaluated
Precautions
Safety and efficacy have not been established in patients younger than 18 years.
Consult WARNINGS section for additional precautions.
Dialysis
Data not available
Other Comments
Administration advice:
- Take this drug at least 1 hour before or 2 hours after food.
- Avoid taking this drug with antacids, histamine-2 antagonists, and proton pump inhibitors.
Monitoring:
- Dermatologic: Bullous and exfoliative skin conditions
- GI: Diarrhea, GI perforation
- Hepatic: Liver function tests
- Metabolic: Dehydration, serum electrolytes (e.g., potassium)
- Ophthalmologic: Acute or worsening ocular disorders (e.g., corneal perforation, ulceration)
- Renal: Renal function
- Respiratory: Interstitial lung disease
Frequently asked questions
- How does erlotinib work (mechanism of action)?
- Can Tarceva (erlotinib) cure lung cancer?