Tarceva

• Non-Small Cell Lung Cancer (NSCLC): First-line treatment of metastatic NSCLC with EGFR exon 19 deletions or exon 21 substitution mutations.
• Pancreatic Cancer: First-line treatment of locally advanced, unresectable or metastatic pancreatic cancer in combination with gemcitabine.

Erlotinib, a kinase inhibitor, is a quinazolinamine. It reversibly inhibits the kinase activity of EGFR, preventing autophosphorylation of tyrosine residues associated with the receptor and thereby inhibiting further downstream signaling. Erlotinib binding affinity for EGFR exon 19 deletion or exon 21 (L858R) mutations is higher than its affinity for the wild-type receptor.

Adult Dose:

• NSCLC: 150 mg PO once daily (empty stomach); continue until disease progression or unacceptable toxicity.
• Pancreatic Cancer (with gemcitabine): 100 mg PO once daily (empty stomach); continue until disease progression or unacceptable toxicity.
• With strong CYP3A4 inhibitors: Reduce by 50 mg decrements.
• With CYP3A4 inducers: Increase by 50 mg increments at 2-week intervals (max 450 mg).
• Smoking patients: Increase by 50 mg increments at 2-week intervals (max 300 mg); reduce dose upon smoking cessation.

Hepatic Impairment: Mild-moderate: No dosage adjustment needed; Severe: Limited data.

Renal Impairment: Safe; no dose adjustment recommended (severe kidney disease: not advised).

Common Side Effects (≥20%):

• Rash
• Diarrhea
• Anorexia/Decreased appetite
• Fatigue
• Dyspnea
• Cough
• Nausea
• Vomiting
• Abdominal pain
• Weight loss
• Stomatitis

Serious Side Effects: Interstitial Lung Disease (ILD), Renal Failure, Hepatotoxicity, Gastrointestinal Perforation, Bullous and Exfoliative Skin Disorders, MI/Ischemia, Cerebrovascular Accident.

Use in Pregnancy: Category D. Can cause fetal harm when administered to a pregnant woman. Doctor may prescribe in life-threatening situations if benefits outweigh risks.

Precautions:

• It is not known whether Erlotinib alters the ability to drive. Do not drive if you experience any symptoms that affect your ability to concentrate and react.
• Take on an empty stomach (1 hour before or 2 hours after meal).
• Diarrhea may occur; drink plenty of fluids and inform doctor if blood in stools.
• Use reliable contraceptive method during treatment and for one month after stopping.
• Makes skin sensitive to sunlight; apply sunscreen or wear protective clothing.
• Avoid smoking while taking this medicine.
• Do not take with medications lowering stomach acid (antacids, H2 blockers, PPIs).
• Inform doctor if mouth ulceration, vision changes, worsening cough, or breathing difficulties occur.
• Regular blood tests to monitor liver function required.

Overdose: Single oral doses up to 1,000 mg in healthy subjects tolerated. 200 mg twice daily was poorly tolerated. Overdose may cause severe diarrhea, rash, and liver transaminase elevation. Withhold Erlotinib and institute symptomatic treatment.

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