Dosing & Uses
Dosage Forms & Strengths
Non-Small Cell Lung Cancer
150 mg PO qDay 1 hr before or 2 hrs after meals
Continue until disease progression
- First-line treatment of metastatic 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 (ie, cobas EGFR Mutation Test)
- Maintenance treatment of locally advanced or metastatic NSCLC in patients whose disease has not progressed after 4 cycles of platinum-based first-line chemotherapy
- Treatment of locally advanced or metastatic NSCLC after failure of at least 1 prior chemotherapy regimen
NSCLC limitations of use
- Not recommended for use in combination with platinum-based chemotherapy
- Safety and efficacy has not been evaluated as first-line treatment in patients with metastatic NSCLC whose tumors have EGFR mutations other than exon 19 deletions or exon 21 (L858R) substitution
100 mg/day PO with gemcitabine
Malignant Gliomas (Orphan)
Orphan sponsor: Genentech, Inc; 1 DNA Way; South San Francisco, CA 94080-4990
Decrease dose by 50 mg decrements
- Strong CYP3A4 inhibitors: Reduce by 50 mg decrements if severe reactions occur when coadministered with strong CYP3A4 inhibitors (eg, atazanavir, clarithromycin, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin, troleandomycin, voriconazole, or grapefruit or grapefruit juice)
- CYP3A4 and CYP1A2 inhibitors: Avoid concomitant use if possible when coadministered with an inhibitor of both CYP3A4 and CYP1A2 (eg, ciprofloxacin)
- When restarting therapy following withholding treatment for a dose-limiting toxicity that has resolved to baseline or grade ≤1
Increase dose by 50 mg increments
- CYP3A4 inducers: Increase by 50 mg increments at 2 week intervals as tolerated to a maximum of 450 mg for concomitant use with CYP3A4 inducers (eg, rifampin, rifabutin, rifapentine, phenytoin, carbamazepine, phenobarbital, St. John’s Wort); if possible, avoid concomitant use
- Concurrent cigarette smoking: Increase by 50 mg increments at 2 week intervals to a maximum of 300 mg; immediately reduce dose to recommended dose (ie, 100 mg or 150 mg daily) upon smoking cessation
Drugs affecting gastric pH
- Proton pump inhibitors: Avoid coadministration if possible
- H2-antagonists: Take erlotinib 10 hr after or at least 2 hr before H2-anagonist
- Antacids: Separate erlotinib and antacid doses by several hours
Discontinue erlotinib for
- Interstitial lung disease (ILD) Severe hepatic toxicity that is unimproved or does not resolve
- GI perforation
- Severe bullous, blistering, or exfoliating skin conditions
- Corneal perforation or severe ulceration
- During diagnostic evaluation for ILD
- Severe renal toxicity (grades 3-4)
- Total bilirubin levels >3 xULN or transaminases >5 xULN in patients without pre-existing hepatic impairment
- In patients with pre-existing hepatic impairment for bilirubin 2 xULN or transaminases 3 xULN
- Persistent severe diarrhea or rash unresponsive to medical management
- Keratitis (grades 3-4, or grade 2 for >2 wk)
- Acute/worsening ocular disorders
Safety and efficacy not established
Serious - Use Alternative
Significant - Monitor Closely
Dry skin (12%)
Keratoconjunctivitis sicca (12%)
Abdominal pain (11%)
Elevated LFT's (grade 2)
Pneumonitis pulmonary infiltrate
Interstitial lung disease-like events
Musculoskeletal and connective tissue disorders: Myopathy, including rhabdomyolysis, in combination with statin therapy
Eye disorders: Ocular inflammation including uveitis
Risk of potentially fatal interstitial lung disease
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
Smoking reduces erlotinib plasma concentration; advise patient to quit smoking
Hepatic or renal impairment
Coadministration with CYP3A4 inhibitors/inducers
CYP1A2 inducers may decrease plasma concentration
Cases of fatal hepatotoxicity reported
No evidence drug has any benefit after disease progression
Monitor if on warfarin or other coumarin-derived anticoagulants for changes in PT/INR
Pregnancy & Lactation
Pregnancy Category: D
Lactation: excretion in milk unknown/not recommended
A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA:Information not available.
Mechanism of Action
EGF receptor tyrosine kinase inhibitor; TKI inhibition possibly blocks angiogenesis and cellular proliferation
Bioavailability: 60% (increased by food to almost 100%)
Peak Plasma Time: 4 hr
Half-life: 36 hr
Clearance: 24% higher in smokers
Protein Bound: 93%
Metabolism: primarily by CYP3A4; to a lesser extent by CYP1A2, and the extrahepatic isoform CYP1A1
Excretion: Feces 83%; urine 8%
Erlotinib inhibits the tyrosine kinase (TK) domain of epidermal growth factors receptors (EGFRs) expressed on cell surface of lung cancers
Patients with EGFR exon 19 deletion or exon 21 L858R mutation have significantly better response to EGFR-TKIs
Genetic testing laboratories
- The following companies currently offer testing for mutations in the EGFR-TK domain
- Genzyme Genetics (http://www.genzymegenetics.com)
- LabCorp (http://www.labcorp.com)
- Response Genetics (http://www.responsegenetics.com)
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