gefitinib at a glance
Medicine class
EGFR tyrosine kinase inhibitor
Cancer type
EGFR mutation-positive, locally advanced or metastatic non-small-cell lung cancer
Food
May be taken with or without food
Swallowing support
The tablet can be dispersed in still water if it cannot be swallowed whole
What is gefitinib used for?
Gefitinib is licensed for:
Adults with locally advanced or metastatic non-small-cell lung cancer with activating EGFR tyrosine-kinase mutations.
How does gefitinib work?
Some lung cancers have an altered EGFR signal that promotes cancer-cell growth, survival and spread. Gefitinib blocks EGFR tyrosine-kinase activity; tumours without a sensitising EGFR mutation are unlikely to benefit.
gefitinib preparations and strengths
Tablet
Route: Oral
Strengths: 250 mg
How to take gefitinib
Gefitinib may be taken with or without food.
Swallow the tablet whole with water where possible.
If swallowing is difficult, place the tablet—without crushing it—in half a glass of still water. Swirl occasionally until dispersed, drink promptly, then rinse the glass with more water and drink the rinse.
Do not use another liquid for dispersion. Trained carers or clinicians may give the dispersion through an appropriate feeding tube.
gefitinib side effects
Common or expected effects
- Diarrhoea, nausea, vomiting, sore mouth or reduced appetite
- Rash, acne-like spots, itching, dry or cracked skin
- Weakness or tiredness
- Changes in liver blood tests
- Dry, irritated or inflamed eyes
- Nail changes or hair loss
Get urgent medical advice
- New or worsening breathlessness, cough or fever—possible interstitial lung disease
- Severe or persistent gastrointestinal symptoms with dehydration
- Eye pain, marked redness, light sensitivity or blurred vision—possible keratitis
- Blistering, peeling or widespread severe skin reaction
- Facial swelling, hives or breathing difficulty—possible allergic reaction
- Severe abdominal pain—possible gastrointestinal perforation
- Symptoms or blood tests suggesting severe liver injury
gefitinib in pregnancy
Pregnancy should be avoided during treatment. Human pregnancy data are unavailable and animal studies found reproductive toxicity. Gefitinib should be used during pregnancy only when the specialist considers it clearly necessary. Discuss pregnancy and contraception with the oncology team.
gefitinib while breastfeeding
Breastfeeding is contraindicated during treatment. It is unknown whether gefitinib enters human milk, and breastfeeding must be stopped if treatment is required.
gefitinib interactions
The cancer team should review prescribed, over-the-counter and herbal products before treatment and whenever medicines change.
Phenytoin, carbamazepine, rifampicin, barbiturates and St John's wort
These CYP3A4 inducers can lower gefitinib exposure and may reduce its effect, so concurrent use should be avoided.
Potent CYP3A4 inhibitors, including itraconazole, ketoconazole, posaconazole, voriconazole, clarithromycin and some protease inhibitors
These can increase gefitinib exposure and adverse effects, requiring close clinical monitoring.
Proton-pump inhibitors, H2-receptor antagonists and regularly used antacids
Sustained reduction of stomach acidity can reduce gefitinib absorption and potentially its effectiveness.
Common questions about gefitinib
Answers are fully visible for fast scanning and source review.
Why is an EGFR test needed?
Gefitinib targets cancers driven by activating EGFR mutations. Reliable tumour testing—and sometimes validated plasma ctDNA testing—is needed because mutation-negative tumours have not shown clinically relevant activity.
Can gefitinib be taken with food?
Yes. It may be taken with or without food.
Can the tablet be dispersed?
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.