Indications

First-line treatment of patients with metastatic Non-Small Cell Lung cancer (NSCLC) whose tumors have Epidermal Growth Factor Receptor (EGFR) exon 19 deletions or exon 21 substitution mutations as detected.Maintenance treatment of patients with locally advanced or metastatic NSCLC whose disease has not progressed after four cycles of platinum based first-line chemotherapy.Treatment of locally advanced or metastatic NSCLC after failure of at least one prior chemotherapy regimen.First-line treatment of patients with locally advanced, unresectable or metastatic pancreatic cancer, in combination with gemcitabine.

Interaction

Anticoagulants: Interaction with coumarin-derived anticoagulants, including warfarin, leading to increased International Normalized Ratio (INR) and bleeding adverse reactions.CYP3A4 inhibitors: Erlotinib is metabolized predominantly by CYP3A4. Co-treatment with the potent CYP3A4 inhibitor ketoconazole increased Erlotinib AUC by 67%. When Erlotinib was co-administered with Ciprofloxacin, an inhibitor of both CYP3A4 and CYP1A2, the Erlotinib exposure [AUC] and maximum concentration [Cmax] increased by 39% and 17%, respectively.CYP3A4 inducers: Pre-treatment with the CYP3A4 inducer Rifampicin for 7-11 days prior to Erlotinib decreased Erlotinib AUC by 58% to 80%. Dose modifications are recommended.Drugs affecting gastric pH: Co-administration of Erlotinib with omeprazole decreased Erlotinib AUC by 46% and co-administration of Erlotinib with Ranitidine 300 mg decreased Erlotinib AUC by 33%.

Contraindications

n/a

Side Effects

The most common adverse reactions (20%) with Erlotinib from a pooled analysis of studies were rash, diarrhea, anorexia, fatigue, dyspnea, cough, nausea, and vomiting. The following serious adverse reactions, which may include fatalities.

Interstitial Lung Disease (ILD)
Renal Failure
Hepatotoxicity with or without Hepatic Impairment
Gastrointestinal Perforation
Bullous and Exfoliative Skin Disorders
Myocardial Infarction/Ischemia
Cerebrovascular Accident
Microangiopathic Hemolytic Anemia with Thrombocytopenia
Ocular Disorders
Hemorrhage in Patients Taking Warfarin