EGFR tyrosine kinase inhibitor (specialist) Pregnancy: Can cause fetal harm based on animal data and mechanism of action; advise pregnant women of the potential risk to a fetus (US label §8.1)

Erlotinib

Brand names: Tarceva

Erlotinib is an oral epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor used in EGFR-mutation-positive non-small-cell lung cancer and, with gemcitabine, in pancreatic cancer.

Auto-extracted from the source labelling — not yet independently clinician-verified. These values were distilled from the UK SPC (or the US label where noted) but have not had a clinician sign-off. Confirm against the current SmPC before prescribing.

Adult dose

Dose: 150 mg

Route: Oral

Frequency: Once daily

Max: 450 mg once daily (only when increasing the dose in 50 mg increments for concomitant CYP3A4 inducers)

US labelling (no UK SPC in bundle). NSCLC: recommended daily dose 150 mg once daily, taken on an empty stomach (at least one hour before or two hours after food); patients selected based on EGFR exon 19 deletions or exon 21 (L858R) substitution mutations. Pancreatic cancer: recommended daily dose 100 mg once daily in combination with gemcitabine, taken on an empty stomach. Treatment continued until disease progression or unacceptable toxicity. Dose modifications: reduce in 50 mg decrements for dose-limiting toxicity; discontinue for ILD, GI perforation, severe bullous/exfoliative skin conditions, or corneal perforation/severe ulceration. With strong CYP3A4 inhibitors (or combined CYP3A4/CYP1A2 inhibitors), reduce by 50 mg decrements and avoid if possible. With CYP3A4 inducers, increase by 50 mg increments at 2-week intervals to a maximum of 450 mg. Concurrent cigarette smoking: increase by 50 mg increments at 2-week intervals to a maximum of 300 mg, then reduce back to the recommended dose (150 mg or 100 mg) on smoking cessation. Paediatric: safety and effectiveness not established; a trial used 85 mg/m2/day in recurrent/refractory ependymoma but was terminated for lack of efficacy — clinician to verify against a children's formulary.

Dose adjustments

Renal

Monitor renal function and electrolytes, particularly in patients at risk of dehydration; withhold for severe (CTCAE grade 3-4) renal toxicity and consider discontinuation

Dose auto-extracted from US FDA prescribing information (openFDA / DailyMed) — cross-check; US labelling may differ from UK — not yet clinician-verified. Always confirm against the product SmPC and your local formulary before prescribing.

Contraindications

None stated (US label §4: None)

Side effects

Rash
Diarrhoea
Anorexia
Fatigue
Dyspnoea, cough, nausea and vomiting (most common, greater or equal to 20%)

Interactions

Strong CYP3A4 inhibitors or combined CYP3A4/CYP1A2 inhibitors (e.g. clarithromycin, itraconazole, ketoconazole, ritonavir, voriconazole, ciprofloxacin, grapefruit) — increase erlotinib exposure; avoid, reduce dose if unavoidable
CYP3A4 inducers (e.g. rifampin, rifabutin, phenytoin, carbamazepine, phenobarbital, St John's wort) — decrease erlotinib exposure; avoid, increase dose if unavoidable
Proton pump inhibitors and H2-receptor antagonists (e.g. ranitidine) — reduce erlotinib exposure via raised gastric pH; avoid PPIs, separate H2-antagonist dosing
Cigarette smoking — decreases erlotinib exposure
Warfarin / coumarin anticoagulants — hemorrhage reported; monitor INR regularly

Clinical monograph

How it works

It reversibly inhibits the intracellular tyrosine kinase domain of EGFR, blocking downstream signalling that drives tumour cell proliferation and survival.

Prescribing in practice

Interstitial lung disease, which can be fatal, is a key risk; stop treatment and investigate promptly if new or worsening breathlessness, cough or fever develops.
Initiate only under specialist supervision after confirmation of EGFR mutation status, taking food and acid-suppressant interactions into account as these reduce absorption.
Acneiform rash and diarrhoea are common and may require dose modification or supportive treatment.

Monitoring

Monitor liver function, renal function and for pulmonary, dermatological and gastrointestinal toxicity during treatment.

Counselling the patient

Take on an empty stomach, well before or after food, and avoid smoking as it lowers drug levels.
Report any new breathlessness or worsening cough urgently.
Use sun protection and report severe or persistent rash or diarrhoea.

Evidence & guidelines

NICE technology appraisal guidance supports erlotinib in EGFR-mutation-positive non-small-cell lung cancer, reflecting pivotal trial evidence of progression-free survival benefit.

Reference: NICE TA258/TA374; ESMO NSCLC; SmPC; Drug verified in RxNorm (NLM); confirm dosing against the manufacturer SPC (eMC). Verify against your local formulary and current prescribing references before prescribing. The structured dose values shown have been reviewed by a clinician. Monograph status: clinician-reviewed (2026-07-04).

Curated clinical cross-links plus same-class fallbacks.

Calculators

Pathways