Drug reference

Erlotinib

Tyrosine Kinase Inhibitor · Antineoplastic

Tyrosine Kinase InhibitorAntineoplasticATC null

CDSCO approved

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

FDA category + note

Top interactionssee all 12 →

Aminolevulinic AcidSevereDatabaseDDInter
DexlansoprazoleSevereDatabaseDDInter
EsomeprazoleSevereDatabaseDDInter
FamotidineSevereDatabaseDDInter

Mechanism

Erlotinib is a tyrosine kinase inhibitor. It is an epidermal growth factor receptor (EGFR) inhibitor.

Indications

Treatment of locally advanced or metastatic non-small cell lung cancer after failure of previous chemotherapyMonotherapy for maintenance treatment of locally advanced or metastatic non-small cell lung cancer with stable disease after four cycles of platinum-based chemotherapylung NSCLC (EGFR deletion of exon 19 or L858R mutation)advanced or metastatic NSCLC after failure of platinum-based chemotherapy treatmentnewly diagnosed NSCLC in patients with EGFR mutationslocally advanced, unresectable, or metastatic pancreatic cancer (in combination with gemcitabine)Non-small cell lung cancerAdvanced/metastatic pancreatic cancer

Dosing

Adult: 150 mg by mouth

Pharmacokinetics

Half-life

36 h

Bioavailability

about 60% (oral)

Protein binding

93 (92–95)%

Metabolism

CYP3A4 (major), CYPs 1A2 and 1A1 (minor)

Excretion

—

Side effects

Common

rashdiarrheaanorexiafatiguedyspneanail disordersnauseavomitingSkin rashDiarrhoeaItchingRise in serum transaminase

Serious

Keratitis
Ulcerative keratitis
Corneal perforation
Blindness
severe rash (>10%)
fatal interstitial lung disease (0.7%-2.5%)
fatal hepatic failure
GI perforation
renal failure
arterial thrombosis
microangiopathic hemolytic anemia
hand-foot skin reaction
corneal perforation or ulceration
Stevens-Johnson syndrome
toxic epidermal necrolysis
Serious hepatic dysfunction

Pregnancy & lactation

Pregnancy

Drug interactions

Aminolevulinic Acid

Severe

Database

Drug interaction classified as: synergy

Source: DDInter

Dexlansoprazole

Severe

Database

Reduced plasma levels and potentially reduced efficacy of erlotinib.

Source: DDInter

Esomeprazole

Severe

Database

Reduced plasma levels and potentially reduced efficacy of erlotinib.

Source: DDInter

Famotidine

Severe

Database

Significantly reduced plasma concentrations of erlotinib, leading to decreased efficacy in treating non-small cell lung cancer or pancreatic cancer.

Coadministration is generally not recommended. If acid suppression is required, consider antacids given at least 2 hours before or after erlotinib. Avoid H2-receptor antagonists and proton pump inhibitors.

Source: DDInter

Lansoprazole

Severe

Database

Reduced plasma levels and potentially reduced efficacy of erlotinib.

Avoid concomitant use. If an acid-suppressing agent is required, consider alternative agents (e.g., H2-receptor antagonists with careful timing, or antacids with strict separation). If lansoprazole is essential, monitor for signs of reduced erlotinib efficacy and consider dose adjustments, though this may not fully overcome the interaction.

Source: DDInter

Leflunomide

Severe

Database

Drug interaction classified as: synergy

Source: DDInter

Lomitapide

Severe

Database

Drug interaction classified as: synergy

Source: DDInter

Mipomersen

Severe

Database

Drug interaction classified as: synergy

Source: DDInter

Omeprazole

Severe

Database

Reduced plasma levels and potentially reduced efficacy of erlotinib.

Source: DDInter

Pantoprazole

Severe

Database

Reduced plasma levels and potentially reduced efficacy of erlotinib.

Avoid concomitant use if possible. If co-administration is necessary, consider administering erlotinib at least 10 hours after the last dose of pantoprazole and at least 2 hours before the next dose. Monitor for therapeutic response.

Source: DDInter

Pexidartinib

Severe

Database

Drug interaction classified as: synergy

Source: DDInter

Rabeprazole

Severe

Database

Reduced plasma levels and potentially reduced efficacy of erlotinib.

Source: DDInter