Erlotinib
TARCEVA
Pronunciation: er-LOE-ti-nib
“Ear lobe nibbler, Tar receiver”
What it isEGFR tyrosine-kinase inhibitor; EGFR-mutant lung cancer and pancreatic cancer.
Why this oneIts remaining distinctive role is combination therapy for pancreatic cancer; osimertinib has displaced it in most EGFR-mutant lung cancer.
What limits itAcneiform rash, diarrhea, and interstitial lung disease can end use; PPIs reduce absorption.
FDA-approved for
- EGFR-mutated non-small cell lung cancer (2004)
- pancreatic cancer
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Metastatic NSCLC (EGFR exon 19 del or exon 21 L858R) | Adults | 150 mg QD | 150 mg QD | 150 mg QD |
| Pancreatic cancer (with gemcitabine) | Adults | 100 mg QD | 100 mg QD | 100 mg QD |
Renal Withhold and consider discontinuation for severe (grade 3-4) renal toxicity; monitor renal function/electrolytes
Hepatic Withhold/consider discontinuation for severe or worsening liver tests; caution with pre-existing hepatic impairment or biliary obstruction
Instructions
- Take on empty stomach (>=1 h before or 2 h after food)
- Continue until disease progression or unacceptable toxicity
- Pancreatic cancer dose given with gemcitabine
- Regularly monitor INR in patients on warfarin/coumarin anticoagulants
Available strengths
- tab 25, 100, 150 mg
Cautions
- Interstitial lung disease (withhold; discontinue if confirmed)
- Renal failure incl. hepatorenal syndrome
- Hepatotoxicity incl. hepatic failure
- GI perforation (discontinue)
- Bullous/exfoliative skin disorders (discontinue)
- Cerebrovascular accident and microangiopathic hemolytic anemia (pancreatic cancer)
- Ocular disorders (corneal perforation/ulceration/keratitis)
- Bleeding in patients on warfarin
- Embryo-fetal toxicity
Adverse reactions
- Rash
- Diarrhea
- Anorexia
- Fatigue
- Dyspnea
- Cough
- Nausea
- Vomiting
Pregnancy Can cause fetal harm; advise contraception and of potential risk to fetus
Lactation Do not breastfeed during treatment and for 2 weeks after final dose
Cost
Generic entry2014
NO BOXED WARNINGS
Principal riskInterstitial lung disease; superseded by osimertinib
Classes and tags
Clinical profile
Legacy pregnancy categoryD
Defining liabilityMyelosuppression and agent-specific hepatic, cardiac, pulmonary, neurologic or reproductive toxicity require oncology monitoring.