Pharmacologic class: Epidermal growth factor receptor (EGFR) inhibitor
Therapeutic class: Antineoplastic
Pregnancy risk category D
Unclear. Drug inhibits intracellular phosphorylation of tyrosine kinase associated with EGFR, which is expressed on cell surface of both normal cells and cancer cells.
Tablets: 25 mg, 100 mg, 150 mg
Indications and dosages
➣ Locally advanced or metastatic non-small-cell lung cancer after failure of at least one chemotherapy regimen; maintenance treatment in patients whose disease hasn't progressed after four cycles of platinumbased first-line chemotherapy
Adults: 150 mg P.O. at least 1 hour before or 2 hours after food ingestion, continued until disease progresses or unacceptable toxicity occurs
➣ First-line treatment of locally advanced, unresectable, or metastatic pancreatic cancer (given with gemcitabine)
Adults: 100 mg P.O. daily at least 1 hour before or 2 hours after food ingestion, continued until disease progresses or unacceptable toxicity occurs
• Severe diarrhea
• Pretreatment with CYP3A4 inducers
• Concurrent use of potent CYP3A4 inhibitors (such as ketoconazole)
• Acute onset of new or progressing pulmonary symptoms
• Colorectal and renal cell cancer
• Malignant glioma
Use cautiously in:
• hepatic impairment, diarrhea
• pulmonary symptoms, suspected interstitial lung disease (such as pneumonitis, interstitial pneumonia, obliterative bronchiolitis, pulmonary fibrosis, adult respiratory distress syndrome, or lung filtration)
• concomitant use of anti-angiogenic agents, corticosteroids, nonsteroidal anti-inflammatory drugs, or taxane-based chemotherapy; prior history of peptic ulceration or diverticular disease
• concurrent warfarin therapy
• pregnant or breastfeeding patients
• children (safety and efficacy not established).
• Give at least 1 hour before or 2 hours after food ingestion.
☞ Interrupt therapy if patient develops acute onset of new or progressing pulmonary symptoms pending diagnostic evaluation. If interstitial lung disease develops, discontinue drug and administer appropriate interventions.
☞ Be aware that some cases of hepatorenal syndrome, acute renal failure, and renal insufficiency may be secondary to baseline hepatic impairment while others may be associated with severe dehydration. Interrupt therapy and take appropriate measures to intensively rehydrate patient, as needed.
☞ Discontinue drug if total bilirubin level is above three times upper limit of normal (ULN) or transaminase levels are above five times ULN versus pretreatment values; signs and symptoms of GI perforation occur; severe bullous, blistering, or exfoliating conditions develop; or acute or worsening ocular disorders such as eye pain occur.
EENT: conjunctivitis, keratoconjunctivitis sicca corneal perforation and ulceration
GI: nausea, vomiting, diarrhea, abdominal pain, anorexia, stomatitis GI perforation
GU: renal insufficiency, acute renal failure
Hepatic: hepatorenal syndrome, hepatic failure
Respiratory: dyspnea, cough, interstitial lung disease
Skin: rash, pruritus, dry skin, Stevens-Johnson syndrome, toxic epidermal necrolysis-like reactions
Drug-drug. CYP3A4 inhibitors (such as clarithromycin, indinavir, itraconazole, ketoconazole, ritonavir, saquinavir, telithromycin): increased erlotinib blood level
CYP3A4 inducers (such as carbamazepine, phenobarbital, phenytoin, rifampin): decreased erlotinib blood level
Warfarin, other coumarin anticoagulants: elevated INR, increased bleeding risk
Drug-diagnostic tests. Alanine aminotransferase, aspartate aminotransferase, bilirubin: increased
International Normalized Ratio: increased
Liver function tests: abnormal
Drug-food. Any food: increased erlotinib bioavailability
Drug-herb. Coenzyme Q10: decreased chemotherapy efficacy
St. John's wort: decreased erlotinib blood level
Drug-behaviors. Smoking: decreased erlotinib plasma concentration
☞ Perform periodic serum electrolyte measurements and renal and liver function testing.
• Advise patient not to smoke while taking drug.
• Monitor INR and prothrombin time regularly in patients receiving warfarin, other coumarin anticoagulants, or nonsteroidal anti-inflammatory drugs.
☞ Monitor for signs and symptoms of respiratory disorders and GI perforation.
☞ Advise patient to seek immediate medical attention for severe or persistent diarrhea, nausea, vomiting, anorexia, severe rash, eye pain, eye irritation, or onset or worsening of unexplained shortness of breath or cough.
• Advise patient not to smoke while taking drug.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, foods, and herbs mentioned above.
Pharmacologic: enzyme inhibitors
Time/action profile (blood levels)
|Oral||unknown||4 hr||24 hr|
Adverse Reactions/Side Effects
Central nervous system
- cerebrovascular accident (pancreatic cancer patients) (life-threatening)
- myocardial infarction/ischemia (pancreatic cancer patients) (life-threatening)
Ear, Eye, Nose, Throat
- corneal perforation
- corneal ulceration
- interstitial lung disease (life-threatening)
- dyspnea (most frequent)
- gi perforation (life-threatening)
- diarrhea (most frequent)
- abdominal pain
- ↑ liver enzymes
- bullous and exfoliative skin disorders (life-threatening)
- rash (most frequent)
- dry skin
- renal failure (life-threatening)
- microangiopathic hemolytic anemia with thrombocytopenia (pancreatic cancer patients)
Drug-Drug interactionStrong inhibitors of CYP3A4, including atazanavir, clarithromycin, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin, or voriconazole ↑ levels and the risk of toxicity; consider dose reduction.Strong inducers of CYP3A4, including rifampin, rifabutin, rifapentine, phenytoin, carbamazepine, or phenobarbital ↓ levels and may ↓ response; alternative therapy or ↑ dose should be considered.Ciprofloxacin may ↑ levels and the risk of toxicity.Smoking may ↓ levels and may ↓ response; may consider ↑ dose if smoking continues.May ↓ midazolam levels.May ↑ risk of bleeding with warfarin.↓ levels with proton pump inhibitors and H2 blockers ; avoid concurrent use.St. John's wort may ↓ levels and may ↓ response; alternative therapy or ↑ dose should be considered.
- Assess respiratory status prior to and periodically during therapy. If dyspnea, cough, or fever occur, discontinue erlotinib, assess for interstitial lung disease, and institute treatment as needed.
- Assess for diarrhea. Usually responds to loperamide but may require dose reduction or discontinuation of therapy if patient becomes dehydrated.
- Assess skin throughout therapy. If bullous, blistering, and exfoliative skin conditions, including Stevens-Johnson syndrome/toxic epidermal necrolysis, occur, interrupt or discontinue treatment. Skin rash may require treatment with corticosteroids or anti-infectives with anti-inflammatory properties; acne treatments may aggravate dry skin and erythema.
- Assess eyes periodically during therapy. If acute or worsening eye disorders or pain occur, interrupt or discontinue therapy.
- Assess for GI pain. Patients receiving concomitant antiangiogenic agents, corticosteroids, NSAIDs, and/or taxane-based chemotherapy, or who have prior history of peptic ulceration or diverticular disease, are at increased risk for GI perforation. Permanently discontinue erlotinib in patients who develop gastrointestinal perforation.
- Lab Test Considerations: Monitor liver function tests (AST, ALT, bilirubin, alkaline phosphatase) periodically during therapy. Dose reduction or discontinuation of therapy should be considered if severe changes in liver function (total bilirubin ≥3 times upper limit of normal and/or transaminases ≥5 times upper limit of normal) occur.
- Monitor renal function and electrolytes in patients at risk for dehydration. Withhold therapy if dehydration occurs.
- Monitor INR regularly in patients taking warfarin. May cause ↑ INR.
Potential Nursing DiagnosesIneffective breathing pattern (Side Effects)
- Oral: Administer at least 1 hr before or 2 hr after food.
- Instruct patient to take erlotinib as directed.
- Advise patient to notify health care professional if severe or persistent diarrhea, nausea, anorexia, vomiting, onset or worsening of skin rash, unexplained dyspnea or cough, or eye irritation occur.
- Advise patient to wear sunscreen and protective clothing to decrease skin reactions.
- Caution patient to use highly effective contraceptive during and for at least 2 wk after completion of therapy. Advise female patients to notify health care professional if pregnancy is planned or suspected or if breast feeding.
- Instruct patient to discontinue smoking during therapy; smoking decreases blood levels of erlotinib.
- Decrease in spread of non–small-cell lung or pancreatic cancer with increased survival.
Patient discussion about Tarceva
Q. Does anyone know anything about the drug Tarceva (from Genentech)?