Classifications: antineoplastic agent; tyrosine kinase inhibitor; epidermal growth factor receptor (egfr) inhibitor; Therapeutic: antineoplastic; egfr inhibitor
Pregnancy Category: D
25 mg, 100 mg, 150 mg tablets
Erlotinib is a human epidermal growth factor receptor type 1 (HER1/EGFR) inhibitor. Antitumor action of erlotinib is believed
to be due to inhibition of EGFR present on the cell surface of both normal and cancer cells.
Inhibition of EGFR in cancer cells diminishes their capacity for cell proliferation, cell survival, and decreases metastases.
Treatment of patients with locally advanced or metastatic nonsmall cell lung cancer (NSCLC) after failure of at least
one prior chemotherapy regimen.
Hypersensitivity to erlotinib; pregnancy (category D); lactation.
Hepatic dysfunction, interstitial pulmonary disease (interstitial pneumonia, pneumonitis, alveolitis); myelosuppression; ocular
toxicities (corneal ulcer, eye pain).
Route & Dosage
|Metastatic NonSmall Cell Lung Cancer
Adult: PO 150 mg once daily at least 1 h before or 2 h after meals
- Give at least 1 h before or 2 h after eating.
- Store at 15°30° C (59°86° F). Keep container tightly closed. Protect from light.
Adverse Effects (≥1%)Body as a Whole: Infection
. GI: Diarrhea,
nausea, vomiting, stomatitis
, abdominal pain. Metabolic:
Increased LFTs. Respiratory: Dyspnea,
cough, interstitial lung disease (sometimes fatal)
. Skin: Acneiform rash,
pruritus, dry skin. Special Senses: Conjunctivitis
, dry eyes.
InteractionsDrug: Atazanavir, clarithromycin, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin,
may increase erlotinib levels and toxicity
; rifampin, rifabutin, rifapentine, phenytoin, carbamazepine, phenobarbital
may decrease erlotinib levels. Herbal: St. John's wort
may decrease erlotinib levels.
60% absorbed orally; food can increase to 100%. Peak:
4 h. Metabolism:
In liver by CYP3A4. Elimination:
Primarily in feces (83%). Half-Life:
Assessment & Drug Effects
- Monitor closely changes in pulmonary function.
- Withhold drug and notify physician for acute onset of new or progressive pulmonary symptoms (e.g., dyspnea, cough, or fever)
or significant changes in liver functions as indicated by elevated transaminases, bilirubin, and alkaline phosphatase.
- Lab tests: periodic LFTs.
Patient & Family Education
- Report promptly any of the following: severe or persistent diarrhea, nausea, anorexia, or vomiting; onset or worsening of
unexplained shortness of breath or cough; eye irritation.
- Monitor closely PT/INR values with concurrent warfarin therapy.
- Women should use effective means to avoid pregnancy while taking this drug.