ERLOTINIB
| ERLOTINIB (er-lo'ti-nib) Tarceva Classifications: antineoplastic agent; tyrosine kinase inhibitor; epidermal growth factor receptor (egfr) inhibitor; Therapeutic: antineoplastic; egfr inhibitor Prototype: Gefitinib Pregnancy Category: D |
Availability
25 mg, 100 mg, 150 mg tablets
Action
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.
Therapeutic Effect
Inhibition of EGFR in cancer cells diminishes their capacity for cell proliferation, cell survival, and decreases metastases.
Uses
Treatment of patients with locally advanced or metastatic non–small cell lung cancer (NSCLC) after failure of at least one prior chemotherapy regimen.
Unlabeled Uses
Pancreatic cancer.
Contraindications
Hypersensitivity to erlotinib; pregnancy (category D); lactation.
Cautious Use
Hepatic dysfunction, interstitial pulmonary disease (interstitial pneumonia, pneumonitis, alveolitis); myelosuppression; ocular toxicities (corneal ulcer, eye pain).
Route & Dosage
| Metastatic Non–Small Cell Lung Cancer Adult: PO 150 mg once daily at least 1 h before or 2 h after meals |
Administration
Oral- 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, anorexia, fatigue, 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.Interactions
Drug: Atazanavir, clarithromycin, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin, troleandomycin, voriconazole 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.Pharmacokinetics
Absorption: 60% absorbed orally; food can increase to 100%. Peak: 4 h. Metabolism: In liver by CYP3A4. Elimination: Primarily in feces (83%). Half-Life: 36.2 h.Nursing Implications
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.
Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; 
Canadian drug name; 
Prototype drug