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 ... Read more 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.

Composition

Pharmacology

Dosage & Administration

NSCLC : The recommended daily dose of Erlotinib for NSCLC is 150 mg taken on an empty stomach, i.e., at least one hour before or two hours after the ingestion of food. Treatment should continue until disease progression or unacceptable toxicity occurs. Pancreatic Cancer : The recommended daily dose of Erlotinib for pancreatic cancer is 100 mg taken once daily in combination with gemcitabine. Take Erlotinib on an empty stomach, i.e., at least one hour before or two hours after the ingestion of food. Treatment should continue until disease progression or unacceptable toxicity occurs. Reduce Erlotinib by 50 mg decrements : If severe reactions occur with concomitant use of strong CYP3A4 inhibitors (such as atazanavir, Clarithromycin, Indinavir, Itraconazole, Ketoconazole, Nefazodone, Nelfinavir, Ritonavir, Saquinavir, Telithromycin, Voriconazole or grapefruit or grapefruit juice] or when using concomitantly with an inhibitor of both CYP3A4 and CYP1A2 (e.g., Ciprofloxacin). Increase Erlotinib by 50 mg increments as tolerated for : Concomitant use with CYP3A4 inducers, such as rifampin, rifabutin, rifapentine, phenytoin, carbamazepine, phenobarbital, or St. John's Wort. Increase doses by 50 mg increments at 2 week intervals to a maximum of 450 mg. Avoid concomitant use, if possible. Concurrent cigarette smoking : Increase by 50 mg increments at 2 week intervals to a maximum of 300 mg. Immediately reduce the dose of Erlotinib to the recommended dose (150 mg or 100 mg daily) upon cessation of smoking.

Contraindications

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

Pregnancy & Lactation

Pregnancy category D. Based on its mechanism of action, Erlotinib can cause fetal harm when administered to a pregnant woman. It is not known whether Erlotinib is present in human milk. Because many drugs are present in human milk and because of the potential for serious adverse reactions in nursing infants from Erlotinib, a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.

Precautions & Warnings

Interstitial Lung Disease (ILD): Occurs in 1.1% of patients. Withhold Erlotinib for acute onset of new or progressive unexplained pulmonary symptoms, such as dyspnea, cough and fever. Discontinue Erlotinib if ILD is diagnosed. Renal Failure: Monitor renal function and electrolytes, particularly in patients at risk of dehydration. Withhold Erlotinib for severe renal toxicity. Hepatotoxicity with or without hepatic impairment including hepatic failure and hepatorenal syndrome: Monitor periodic liver testing. Withhold or discontinue Erlotinib for severe or worsening liver tests. Gastrointestinal perforations-discontinue Erlotinib. Bullous and exfoliative skin disorders-discontinue Erlotinib. Myocardial infarction (Ml)/ischemia: The risk of Ml is increased in patients with pancreatic cancer.

Therapeutic Class

Targeted Cancer Therapy

Storage Conditions

Store at a temperature not exceeding 30°C in a dry place. Protect from light and moisture.