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Kinase inhibitor

Erlotinib is a kinase inhibitor used to treat certain types of cancer. It is primarily used for patients with specific mutations in non-small cell lung cancer (NSCLC) and for the first-line treatment of pancreatic cancer when used with gemcitabine.

How it worksErlotinib works by blocking a protein called the epidermal growth factor receptor (EGFR). By inhibiting this receptor, the drug helps stop cancer cells from growing and surviving.

Brand names:Erlotinib

Used for
Metastatic non-small cell lung cancer (NSCLC) with specific EGFR mutations (exon 19 deletions or exon 21 L858R substitution)First-line treatment of locally advanced, unresectable, or metastatic pancreatic cancer (used with gemcitabine)
Conditions
Metastatic non-small cell lung cancerLocally advanced pancreatic cancerUnresectable pancreatic cancerMetastatic pancreatic cancer
Class
Kinase inhibitorRespiratoryGastrointestinalIntegumentaryHepaticRenalOcular

How to take

FormsTablets
RoutesOral

For lung cancer, the dose is 150 mg once daily. For pancreatic cancer, the dose is 100 mg once daily in combination with gemcitabine. Both should be taken on an empty stomach.

Take erlotinib at least one hour before or two hours after eating.

Key warnings

  • ·Lung disease: Monitor for new or worsening cough, fever, or shortness of breath.
  • ·Liver and kidney health: Periodic testing of liver and kidney function is necessary.
  • ·Skin reactions: Severe skin conditions may require stopping the drug.
  • ·Pregnancy: This drug can cause harm to an unborn baby.
  • ·Interactions: Smoking and certain stomach acid medications can change how the drug works.

Do not use if

  • ·None listed

Side effects

Common

RashDiarrheaFatigueNauseaVomitingDecreased appetiteCoughShortness of breath

Serious

  • ·Lung disease (interstitial lung disease)
  • ·Kidney failure
  • ·Liver problems (hepatotoxicity)
  • ·Stomach/intestinal perforation
  • ·Severe skin blistering or peeling
  • ·Stroke (cerebrovascular accident)
  • ·Blood disorders (microangiopathic hemolytic anemia)
  • ·Eye problems (corneal issues)

Seek help if

  • ·Severe abdominal pain
  • ·New or worsening shortness of breath
  • ·Severe skin blistering
  • ·Eye pain or vision changes
  • ·Signs of liver problems

Interactions

  • ·Strong CYP3A4 inhibitors (like certain antifungals or grapefruit juice) can increase erlotinib levels.
  • ·CYP3A4 inducers (like rifampin or St. John's wort) can decrease erlotinib levels.
  • ·Cigarette smoking can decrease the amount of erlotinib in your body.
  • ·Stomach acid reducers (like proton pump inhibitors) can decrease erlotinib levels.
  • ·Blood thinners like warfarin may have increased effects, requiring regular monitoring.
FoodFood increases the absorption of erlotinib; it should be taken on an empty stomach (1 hour before or 2 hours after eating).

Special populations

PregnancyErlotinib can cause fetal harm. Women of reproductive potential should use effective contraception during treatment and for one month after the last dose.

BreastfeedingDo not breastfeed while taking erlotinib and for 2 weeks after the final dose.

PediatricThe safety and effectiveness of erlotinib in children have not been established.

GeriatricNo significant differences in safety or effectiveness were found in patients aged 65 and older compared to younger patients.

Talk to your doctor

Monitor

  • ·Lung symptoms (cough, fever, dyspnea)
  • ·Liver function tests
  • ·Renal function and electrolytes
  • ·Skin condition
  • ·INR if taking warfarin

Questions to ask

  • ·Should I have my liver and kidney function tested regularly?
  • ·How will my smoking status affect my dose?
  • ·What should I do if I develop a new cough or shortness of breath?
  • ·Are there specific skin creams I should use for the rash?

Pharmacokinetics

OnsetPeak plasma levels occur 4 hours after dosing
Half-life36.2 hours
DurationSteady state reached in 7 to 8 days
BioavailabilityApproximately 60% absorbed; increases to 100% with food
Protein binding93% protein bound to plasma albumin and alpha-1 acid glycoprotein (AAG)
MetabolismPrimarily by CYP3A4, less by CYP1A2 and CYP1A1
Excretion91% recovered: 83% in feces, 8% in urine

Practical

OverdoseIf an overdose is suspected, stop taking erlotinib and seek medical attention for symptom management.

Ingredients

Allergens

lactose

Inactive

colloidal silicon dioxidecrospovidonehypromelloselactose monohydratemagnesium stearatemicrocrystalline cellulosepolyethylene glycolsodium lauryl sulfatetalctitanium dioxide

Educational summary derived from FDA labeling, AI-assisted. Not medical advice — consult a healthcare professional. Updated 2026-04-25.