Erlotinib (Tarceva)

Erlotinib at a glance

• Generic name: erlotinib. A verified brand is Tarceva.
• Type: an epidermal growth factor receptor, or EGFR, tyrosine kinase inhibitor.
• Form: tablets in 25 mg, 100 mg and 150 mg strengths in the reviewed product information.
• Routine: usually once daily, on an empty stomach, at least one hour before or two hours after food.
• Important issues: rash, diarrhoea, eye symptoms, liver and kidney problems, and uncommon serious lung or bowel complications.
• Smoking and acid-reducing medicines can lower the amount absorbed or available in the body. Tell your pharmacist before starting, stopping or changing them.

What erlotinib is and how it works

EGFR is a protein involved in signals that tell cells to grow and divide. Some cancers have changes in the EGFR gene that make this signalling particularly active. Erlotinib blocks the kinase part of EGFR, helping interrupt growth signals in cells that depend on this pathway. It is a small-molecule targeted medicine, not a checkpoint-inhibitor immunotherapy.

The same pathway has normal roles in skin and other tissues. Blocking it explains why a treatment directed at cancer can also cause rash, diarrhoea or eye-surface problems. “Targeted” does not mean side-effect free. Conversely, the absence of a rash does not let you decide on your own that the medicine is ineffective.

Your team assesses benefit using your symptoms and planned investigations. The intended duration of treatment depends on benefit, tolerability and the complete treatment plan.

How the team decides whether it is suitable

Your oncologist considers the diagnosis, molecular results, previous treatments, health conditions and current prescribing information. Where EGFR testing guides selection, the exact mutation matters. Examples in the US label include exon 19 deletions and the exon 21 L858R change; simply being told a tumour is “EGFR positive” is not a complete description of the test.

Testing may use tumour tissue or a blood sample looking for tumour DNA. A negative blood result does not always exclude an EGFR alteration. The labels advise testing tissue when available in that situation. Ask which result supports your plan and whether further testing would change the decision.

Tell the team about liver or kidney disease, previous lung inflammation, stomach ulcers or diverticular disease, severe dry eyes, corneal problems and contact-lens use. Disclose allergies. Tarceva contains lactose: European information says patients with rare hereditary galactose intolerance, total lactase deficiency or glucose-galactose malabsorption should not take it. Safety and effectiveness in children are not established.

Some people receive another cancer medicine alongside erlotinib. The combination can change both benefit and risk, and it brings its own instructions. This article focuses on erlotinib and does not replace information about those medicines.

Before treatment starts

Blood tests generally assess blood counts, liver function, kidney function and blood salts such as potassium. The team reviews your weight, appetite, bowel pattern and existing symptoms.

Describe your skin and eye history, including medicines or creams you already use. If you have contact lenses or severe dry eyes, ask whether an eye assessment or a change to glasses is advisable. An examination is particularly important when symptoms suggest damage to the cornea, the clear front surface of the eye.

Bring every medicine and supplement to the review, including non-prescription antacids. Mention smoking honestly, including any plan to stop. Agree how to contact the team on the day your smoking changes, because an increased erlotinib dose may need prompt reduction. Help to stop smoking should be part of the plan, not something you have to arrange alone.

Discuss pregnancy prevention and fertility questions before the first dose. Ask for a written diarrhoea plan and a skin-care plan, including what can be started at home and which symptoms mean you should call. Make sure you know your own hospital's urgent contact arrangements outside office hours.

How to take erlotinib

A consistent empty-stomach routine

Take the prescribed dose once daily. Use plain water and leave at least one hour before eating or at least two hours after food. For example, a morning dose can be followed by breakfast at least an hour later. A bedtime dose may suit someone whose last food was at least two hours earlier. Food increases absorption, so taking the tablet with a meal is not a harmless change.

Usual labelled adult starting doses include 150 mg daily for a single-agent plan and 100 mg daily in a specified combination with gemcitabine. These are examples, not a choice for you to make. Your prescribed dose may be lower because of side effects or different because of a supervised interaction-management plan.

Swallow tablets whole. Do not chew, break or crush them. If swallowing is difficult, tell the pharmacist before changing how you take them. The reviewed routine patient instructions do not establish a standard home-made liquid or feeding-tube method; a specialist must check a suitable approach for your exact product.

Missed doses, vomiting and extra tablets

If you miss one or more doses, contact your treatment team or pharmacist promptly for advice. Do not take a double dose. This is the advice in the European leaflet and Macmillan information; do not borrow a twelve-hour rule from another targeted medicine.

If you vomit after taking erlotinib, do not take a replacement tablet. Take the next dose at the usual time unless the team tells you to pause. Repeated vomiting, inability to drink or much less urine needs prompt advice. If you accidentally take more than prescribed, contact the team immediately rather than waiting for symptoms.

Treatment holds and dose changes

Treatment commonly continues while it is helping and its side effects remain manageable. A pause may allow skin, bowel, liver or other problems to improve. When restarting after dose-limiting toxicity, labels describe reductions in 50 mg steps, but the actual prescription is determined by your clinician. Never restart from leftover tablets without a clear instruction.

Some serious complications mean treatment must stop permanently, including confirmed interstitial lung disease or a bowel perforation. A temporary reduction for an ordinary rash is a different situation. Ask the team to explain both the reason for any change and how response will continue to be checked.

Monitoring and checking response

Expect regular appointments and blood tests. Liver tests and kidney function need periodic monitoring; blood salts are particularly important if diarrhoea or vomiting puts you at risk of dehydration. Liver disease or blockage of the bile ducts requires closer liver monitoring. The labels do not give one universal monthly timetable for everyone.

The team also reviews rash, bowel symptoms, food and fluid intake, weight, breathing and eye symptoms. Report changes between visits rather than waiting for blood results. A normal blood test cannot exclude corneal inflammation or an early lung complication. If you take warfarin, you need additional clotting-test monitoring because erlotinib can increase bleeding risk.

Scans and other disease-specific assessments show whether treatment is helping. Ask when these are planned and how results will affect decisions. Tell the team if you have missed doses, changed heartburn treatment or changed smoking; these can influence drug exposure and the interpretation of your treatment course.

Common side effects and practical management

Acne-like rash and dry skin

A rash often appears on the face, scalp, neck, chest or back, sometimes in the first few weeks. It can look like acne, but ordinary acne products may irritate it. Tell the team early; prescribed creams or antibiotics may prevent worsening and make it easier to continue treatment. Do not scrub or squeeze inflamed areas.

Use gentle, unperfumed cleansers and moisturisers. Protect skin from the sun with clothing, a hat and sunscreen of at least SPF 30. Avoid alcohol-containing skin products and unprescribed acne remedies. Seek prompt help for spreading redness, increasing pain, discharge or fever, which may indicate infection. Blistering or peeling is a different, urgent problem described below.

Diarrhoea

Count loose stools relative to your usual pattern and note whether you can drink and pass urine normally. Follow your prescribed anti-diarrhoea plan, which may include loperamide. Contact the team early if symptoms are persistent, frequent or difficult to control; do not keep increasing medicines beyond the plan.

Take regular fluids and ask whether oral rehydration solution is suitable. Your fluid target should account for kidney or heart conditions. Severe diarrhoea, dizziness, very little urine, inability to keep fluids down, blood in the stool or significant abdominal pain needs urgent assessment. Erlotinib may need withholding while dehydration is treated.

Appetite, nausea and mouth soreness

Small meals can be easier when appetite is poor, but keep the required food-free interval around your tablet. Use prescribed anti-sickness medicine. Report ongoing weight loss or reduced intake so a dietitian can help. Persistent vomiting needs review rather than simply missing meals to preserve the dosing schedule.

Clean your mouth gently with a soft toothbrush and follow recommended mouth care. Report ulcers, white patches or pain that limits eating and drinking. Mouth soreness with widespread skin blistering or eye symptoms needs urgent assessment, not routine mouthwash alone.

Hair, nails, fatigue and mood

Hair may become thinner or change texture. Eyelashes can grow longer or turn towards the eye, causing irritation. Nails may become brittle or tender, and the surrounding skin can become inflamed. Report painful nail folds or eyelash irritation; avoid trying to solve an eye problem by cutting lashes yourself.

Pace activities and include manageable movement and rest. Marked fatigue deserves assessment for dehydration, anaemia, infection or other causes. Tell the team about persistent low mood, sleep disruption, numbness or tingling. Other medicines and the illness can contribute, so the solution may involve more than changing erlotinib.

Less common but important side effects

Lung inflammation

Interstitial lung disease, sometimes called pneumonitis, is inflammation affecting lung tissue. It can be serious or fatal and can develop early or after months of treatment. New or worsening unexplained cough, breathlessness or fever needs immediate assessment. Stop taking further erlotinib doses while urgent investigation for possible lung inflammation is arranged. If interstitial lung disease is confirmed, erlotinib is permanently discontinued.

Infection, a blood clot and the underlying illness can cause similar symptoms. Do not diagnose the cause yourself or assume that a familiar cough makes a new deterioration harmless. Severe breathing difficulty is an emergency.

Liver injury and kidney failure

Liver injury can occur even when liver function was previously normal. Tests may detect it before symptoms develop. Yellow skin or eyes, dark urine, pale stools, unusual exhaustion or upper-abdominal discomfort needs prompt advice. Significant abnormalities may require withholding treatment; persistent severe toxicity can mean stopping it.

Severe dehydration can injure the kidneys, and other kidney problems have also been reported. Passing much less urine, dizziness, confusion or marked weakness needs urgent assessment. Do not assume that drinking a little more will be enough if diarrhoea or vomiting is continuing.

Eye-surface damage

Dryness, abnormal eyelashes and inflammation can damage the cornea. Contact the team urgently for eye pain, redness, light sensitivity, increased watering or blurred vision. You may need rapid ophthalmology assessment and a treatment hold. Corneal ulceration or perforation can threaten sight; US guidance requires discontinuation for corneal perforation or severe ulceration. Remove contact lenses if your eyes are irritated and seek advice before using them again.

Bowel perforation and severe skin reactions

A perforation is a hole in the stomach or bowel. Warning symptoms include sudden or severe abdominal pain, a rigid or swollen abdomen, fever or collapse. Vomiting blood or black, tarry stools also needs urgent medical assessment. Risk may be higher with previous ulcers or diverticular disease and certain accompanying medicines. Confirmed perforation requires permanent discontinuation.

Rare severe reactions can cause blisters, skin peeling and sores on the lips, mouth, eyes or genitals. Stop further doses and seek emergency assessment for a widespread or severe reaction. US information recommends discontinuing erlotinib for severe blistering or peeling conditions; the team must determine subsequent treatment.

Bleeding and combination-specific risks

Erlotinib can interact with warfarin and related anticoagulants, occasionally causing serious bleeding. Report unusual bruising, persistent nosebleeds, blood in urine or stools promptly. Do not stop a necessary anticoagulant independently.

Stroke and a disorder involving breakdown of red blood cells with low platelets were reported in the gemcitabine combination study. These findings should not be presented as the same risk for erlotinib alone. Sudden facial droop, one-sided weakness, speech difficulty or loss of vision is an emergency. Unusual bruising with profound weakness or reduced urine also needs urgent assessment.

Other medicines, smoking and vaccinations

Medicines for reflux or heartburn

Erlotinib needs an acidic environment for reliable absorption. Proton-pump inhibitors, such as omeprazole, should be avoided with it where possible. Moving the PPI to another time may not solve the interaction because its effect lasts much longer than a few hours. Do not stop prescribed stomach protection without a replacement plan from your team.

If an H2 blocker is necessary, ask the pharmacist to write a timetable. US instructions place erlotinib ten hours after an H2-blocker dose and at least two hours before the next dose. European information describes staggered dosing from ranitidine studies. This is a product-information timing example, not a recommendation to obtain ranitidine.

Simple antacids have different instructions. US information says to separate them by several hours; European Tarceva specifies taking the antacid at least four hours before or two hours after erlotinib. Check the actual preparation, since combination heartburn remedies may contain more than one medicine. Never increase erlotinib yourself to compensate for acid suppression.

Smoking changes the dose-management plan

Cigarette smoking lowers erlotinib exposure. Tell the team if you smoke, stop or restart. US information allows carefully supervised dose increases for continuing smokers, but an increased dose must be reduced promptly when smoking stops. Contact the prescribing team the same day so the next dose is correct.

European information notes that 300 mg did not improve efficacy compared with 150 mg in a study of continuing smokers and recommends stopping smoking. A higher dose is therefore not a proven way to cancel smoking's effects. Ask for cessation support and have any stop-smoking medicines checked with your full prescription.

Other interactions and vaccines

Avoid grapefruit, grapefruit juice and St John's wort. Some antibiotics, antifungals, seizure medicines, tuberculosis treatments and antivirals can substantially change erlotinib levels through liver enzymes. Strong interacting medicines should generally be avoided; unavoidable combinations need specialist management. Report every new prescription, even a short course.

Warfarin requires regular INR testing, which measures its effect on clotting. Statins can add a risk of muscle injury: report unexplained severe muscle pain, weakness or dark urine promptly. Check before taking anti-inflammatory painkillers such as ibuprofen, particularly with an ulcer history or other bowel-risk medicines.

Discuss flu, COVID-19 and other vaccines with the team. Non-live vaccines may be appropriate; live vaccines may be unsuitable if your immune system is weakened. Timing depends on your complete treatment and immune function, so do not apply a fixed waiting interval from another medicine.

Everyday life, storage and practical support

Use a daily reminder that includes the food-free interval. Keep a record of diarrhoea, skin changes and missed doses, and arrange repeat supplies before tablets run out. If costs, work or travel interfere with treatment, tell the team early rather than rationing doses.

Continue activities within your energy level. Do not drive if sleepy, dizzy or visually impaired. Protect your skin during outdoor activity, and carry your medicine list and urgent contact details when travelling. Tell dentists and other clinicians about erlotinib and any accompanying treatment before procedures.

Store tablets in their labelled packaging, out of children's reach and away from heat, moisture and direct sunlight. Follow your pack's temperature instructions; the reviewed US product specifies 20–25°C (68–77°F). Return unwanted tablets to the pharmacy or treatment unit as instructed.

Fertility, contraception, pregnancy and breastfeeding

Erlotinib can harm a developing baby. If you could become pregnant, discuss effective contraception before starting. US prescribing information specifies protection during treatment and for one month after the final dose; European Tarceva specifies at least two weeks afterwards. Agree a clear plan for your supplied product, and follow any longer interval required by accompanying treatment. Contact the team immediately if pregnancy is suspected.

The checked erlotinib labels do not specify a separate fixed male contraception interval. Ask for advice for you and your partner based on the whole regimen, rather than assuming that a female interval applies identically to everyone. Future fertility effects in people are uncertain; discuss fertility preservation before treatment if relevant.

Do not breastfeed during treatment or for at least two weeks after the final dose. The presence and effects of erlotinib in human milk are not established, but possible serious harm to an infant supports this precaution. Another medicine in your regimen may require a longer wait.

After treatment finishes

Ask why treatment has stopped, which medicines continue and when follow-up tests are due. Keep reporting breathing symptoms, persistent diarrhoea, eye problems or jaundice rather than assuming that stopping tablets removes the need for assessment. Continue skin protection and supportive care while symptoms settle.

Follow the agreed contraception and breastfeeding intervals. If treatment was held temporarily, obtain the exact restart date and dose. Never restart after a serious reaction or copy a previous prescription without the team's instruction. Smoking and other medicines should be reviewed again if erlotinib is restarted.

Frequently asked questions