← Search & browse all drugs
ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors
erlotinib
L01EB02
Forms & Strengths
- Oral tablets: 25 mg
- Oral tablets: 100 mg
- Oral tablets: 150 mg
Adult Dosing
- Non-Small Cell Lung Cancer (NSCLC): 150 mg orally once daily taken on an empty stomach (at least 1 hour before or 2 hours after food)
- Pancreatic Cancer: 100 mg orally once daily in combination with gemcitabine
- Dose reduction: Reduce in steps of 50 mg for toxicity management
Pediatric Dosing
- Safety and efficacy in pediatric patients have not been established
Indications
- Treatment of metastatic non-small cell lung cancer (NSCLC) with EGFR exon 19 deletions or exon 21 (L858R) substitution mutations
- First-line treatment of locally advanced, unresectable, or metastatic pancreatic cancer in combination with gemcitabine
Mechanism of Action
- Reversible inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase
- Blocks intracellular phosphorylation of tyrosine kinases associated with EGFR, halting downstream oncogenic signaling and inhibiting cellular proliferation
Contraindications
- Known severe hypersensitivity to erlotinib or any component of its formulation
Adverse Reactions
- Rash (acneiform)
- Diarrhea
- Fatigue
- Dyspnea
- Nausea and vomiting
- Anorexia
- Stomatitis
- Interstitial lung disease (ILD)-like events
- Hepatotoxicity
- Gastrointestinal perforation
Drug Interactions
- CYP3A4 inducers (e.g., rifampin, carbamazepine): Significantly decrease erlotinib plasma concentrations
- CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin): Significantly increase erlotinib plasma concentrations and toxicity risk
- Gastric pH-increasing agents (e.g., proton pump inhibitors, H2 blockers, antacids): May decrease erlotinib solubility and reduce bioavailability
- Coumarin anticoagulants (e.g., warfarin): Increased international normalized ratio (INR) and bleeding events reported
Curated Content: Needs Vetting Before Put to Clinical Use