- Drugs List
- Therapeutic Indications
- Precautions and Warnings
- Pregnancy and Lactation
- Side Effects
Oral formulations of erlotinib.
Advanced/metastatic non-small cell lung cancer with EGFR-TK mutations
Metastatic pancreatic cancer in combination with gemcitabine
Locally advanced or metastatic non-small cell lung cancer with EGFR activating mutations:
- First line Treatment
- Treatment after failure of at least one other chemotherapy regimen
- Maintenance treatment as a monotherapy with stable disease after 4 cycles of standard platinum-based first-line chemotherapy
Treatment of metastatic pancreatic cancer in combination with gemcitabine.
Whilst the doses stated below are those recommended by the manufacturer, local cancer network protocols for the relevant indication should be consulted.
In patients who do not develop a rash within the first 4 - 8 weeks of treatment, further treatment with erlotinib should be re-assessed. Post hoc analysis of clinical trials concluded that patients who developed a rash had a longer overall survival compared to patients who did not develop a rash.
Non-small cell lung cancer:
Recommended dose is 150mg daily.
Reduce in 50mg steps if dose adjustment is necessary.
Recommended dose is 100mg daily in combination with gemcitabine. See gemcitabine prescribing information for dose.
Reduce in 50mg steps if dose adjustment is necessary.
Tablets should be taken at least one hour before or two hours after food.
Children under 18 years
Elevated serum transaminases - greater than 5 times upper limit of normal
Severe renal impairment
Precautions and Warnings
Wearing of contact lenses
Glucose-galactose malabsorption syndrome
History of keratitis
History of peptic ulcer
Severe dry eyes
Refer patients with symptoms of keratitis to an ophthalmology specialist
Confirm EGFR mutation status of tumour prior to treatment
Treatment to be prescribed under the supervision of a specialist
Consult local policy on the safe use of oral anti-cancer drugs
Staff: Not to be handled by pregnant staff
Monitor hepatic function in patients with hepatic impairment
Monitor pulmonary function regularly
Monitor renal function in patients with dehydration or severe diarrhoea
Monitor serum electrolytes in patients with dehydration or severe diarrhoea
Patients with new pulmonary symptoms should be investigated
Persistent diarrhoea - monitor patient; reduce dose or discontinue therapy
Advise patient to report any blurred vision or any other eye symptoms
Discontinue / interrupt treatment if ulcerative keratitis develops
Discontinue treatment if interstitial lung disease develops
Discontinue if severe skin reaction occurs
Discontinue if significant/persistent hepatic function abnormalities occur
Discontinue or interrupt treatment with acute/worsening ocular disorders
Discontinue treatment if gastrointestinal perforation occurs
If dehydration occurs, discontinue treatment until patient has recovered
Dose adjustment required if patient starts/stops smoking during therapy
Advise patient not to self medicate with antacids or acid suppressants
Advise patient not to take St John's wort concurrently
Advise patients to avoid aspirin and NSAID use
Avoid antacids 4 hours before or 2 hours after dose
Female: Contraception required during and for 2 weeks after treatment
Breastfeeding: Do not breastfeed during & for 2 weeks after treatment
Advise patient on appropriate sun protection methods
Advise patient on giving up smoking
Cigarette smoking has been shown to reduce erlotinib exposure by 50-60%. The 300mg dose did not show improved efficacy in patients who smoke cigarettes when compared to the 150mg dose. Efficacy and long term safety of a dose higher than the recommended starting doses have not been established in patients who continue to smoke cigarettes. Therefore, current smokers should be advised to stop smoking, as plasma concentrations of erlotinib in smokers as compared to non-smokers are reduced.
Rare cases of hepatic failure have been reported during erlotinib treatment. Hepatic function testing should be considered in patients with pre-existing hepatic disease or concomitant hepatotoxic medications.
In cases of moderate or severe diarrhoea, patients should be treated with loperamide or other antidiarrhoeal agents. In some cases, dose reduction may be necessary. In the event of severe or persistent diarrhoea, nausea, anorexia, or vomiting associated with dehydration, erlotinib should be interrupted and appropriate measures should be taken to treat the dehydration.
There have been reports of hypokalaemia and renal failure secondary to severe dehydration mainly in patients receiving concomitant chemotherapy. In patients with aggravating risk factors (concomitant medications, symptoms or diseases or other predisposing factors such as advanced age) therapy should be interrupted and steps taken to intensively rehydrate patients intravenously. Renal function and serum electrolytes including potassium should be monitored in patients at risk of dehydration.
Pregnancy and Lactation
Erlotinib is contraindicated during pregnancy.
The manufacturer does not recommend using erlotinib during pregnancy.
There are no studies in pregnant women using erlotinib and the potential risk for humans is unknown, but animal studies in rabbits and rats have shown some reproductive toxicity.
Erlotinib is contraindicated during breastfeeding.
The manufacturer does not recommend breastfeeding whilst taking erlotinib and for at least two weeks after treatment.
There is limited information on the use of erlotinib during breastfeeding. It is not known whether the drug passes into breast milk but the long elimination half life and the molecular weight suggest this is likely. The effects on the nursing infant are unknown, but because of the potential for serious adverse reactions, breastfeeding should be stopped if treatment with erlotinib is necessary.
Hyperpigmentation of skin
Increase in serum ALT/AST
Interstitial lung disease
Palmar-Plantar Erythrodysaesthesia syndrome
Serum bilirubin increased
Toxic epidermal necrolysis
It is strongly recommended that the UK National Poisons Information Service be consulted on cases of suspected or actual overdose where there is doubt over the degree of risk or about appropriate management.
The following number will direct the caller to the relevant local centre (0844) 892 0111
Information may be obtained if you have access to ToxBase the primary clinical toxicology database of the National Poisons Information Service. This is available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).
Last Full Review Date: October 2019
British National Formulary, 63rd Edition (2012) Pharmaceutical Press, London.
Drugs During Pregnancy and Lactation: Treatment Options and Risk Assessment, 2nd edition (2007) ed. Schaefer, C., Peters, P. and Miller, R. Elsevier, London.
Drugs in Pregnancy and Lactation: A Reference Guide to Fetal and Neonatal Risk, 9th edition (2011) ed. Briggs, G., Freeman, R. and Yaffe, S. Lippincott Williams & Wilkins, Philadelphia.
Martindale: The Complete Drug Reference, 37th edition (2011) ed. Sweetman, S. Pharmaceutical Press, London.
Medications and Mothers' Milk, 14th Edition (2010) Hale, T. Hale Publishing, Amarillo, Texas.
Summary of Product Characteristics: Tarceva 25mg, 100mg and 150mg Film-Coated Tablets. Roche Products Ltd. Revised December 2018.
The Renal Drug Handbook. 3rd edition. (2009) ed. Ashley, C and Currie, Radcliffe Publishing Ltd, Abingdon.
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Medscape UK | Univadis prescription drug monographs & interactions are based on FDB Multilex Content
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