Gefitinib
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Molecule Summary
| Uses | Non-Small Cell Lung Cancer |
| Therapy | Anti-Neoplastic |
| Side Effects | Rash, Diarrhoea, Dry Skin, Loss Of Appetite |
Assurance
available
Regulated
Molecule Description
Gefitinib is a prescription oral anticancer medication belonging to a class of drugs known as epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs). It is used to treat certain types of locally advanced or metastatic non-small cell lung cancer (NSCLC) with specific EGFR mutations. It blocks EGFR signals that help cancer cells grow and survive, slowing cancer growth and spread. This medicine is supplied as film-coated oral tablets designed for once-daily dosing. It can be taken either with or without food. For patients who have difficulty swallowing tablets whole, the tablet may be dispersed in half a glass of non-carbonated water by dropping it in without crushing, stirring until dissolved, and drinking immediately.
Treatment with Gefitinib requires careful medical supervision by an experienced oncologist. Because this medication can cause significant dermatological reactions, gastrointestinal disturbances, and potential liver or lung complications, regular clinical monitoring and routine laboratory blood tests may be required throughout the course of therapy.
Patients receiving this treatment must be fully informed about potential risks, including characteristic skin rashes, diarrhea, elevated liver enzymes, and rare cases of interstitial lung disease. Close communication with your healthcare team is essential to manage side effects promptly and ensure treatment safety.
Uses
- First-line treatment of adult patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) with activating mutations of EGFR-TK.
Contraindications
When should one not use Gefitinib
- If you have a known hypersensitivity or severe allergic reaction to gefitinib or any of the inactive ingredients in the tablet formulation.
- Pregnancy and breastfeeding require specific medical advice before treatment.
Side effects
Common side effects of this drug are:
- Rash (acneiform skin rash, which can occur or worsen in sun-exposed areas)
- Diarrhea and nausea
- Dry skin, pruritus (itching), and acne
- Decreased appetite and weight loss
- Asthenia (mild weakness) and fatigue
- Elevated liver enzymes
- Vomiting and stomatitis (mouth sores)
- Eye irritation, conjunctivitis, blepharitis, or dry eyes
- Hair thinning or hair loss (alopecia)
- Nail disorders (such as nail bed infections or brittleness)
- Hemorrhagic events (such as nosebleeds or mild hematuria)
- Interstitial Lung Disease (ILD)-like events (severe, potentially fatal lung inflammation causing sudden cough, fever, and breathing difficulties)
- Severe, dehydrating diarrhea leading to acute kidney injury
- Severe hepatic toxicity or liver failure
- Gastrointestinal perforation
- Severe skin reactions (such as toxic epidermal necrolysis or Stevens-Johnson syndrome)
- Corneal erosion or severe eye ulceration
Precautions and Warnings
Pregnancy
Breast Feeding
Driving
Alcohol
Other General Warnings
Talk to your doctor if
- You experience sudden breathing difficulties, cough, or fever, which require immediate evaluation for lung inflammation.
- You develop severe, persistent diarrhea that does not respond to anti-diarrheal treatment.
- You notice signs of liver problems, such as yellowing of the skin or eyes, dark urine, or upper abdominal pain.
- You experience severe eye pain, redness, blurred vision, or eye watering.
- Protect your skin from sun exposure by using broad-spectrum sunscreens and wearing protective clothing, as gefitinib-induced rash often worsens in sunlight.
- Report any sudden onset or worsening of shortness of breath, cough, or fever immediately, as these can be signs of interstitial lung disease.
- Stay well hydrated, and inform your doctor early if you experience persistent diarrhea so they can prescribe appropriate anti-diarrheal medications.
- Keep all scheduled liver function tests and medical evaluations.
- Inform all your healthcare providers that you are taking this medication before undergoing any other medical procedures or eye examinations.
Mode of Action
How Does It Work?
Gefitinib blocks a protein called EGFR, which can send signals that tell cancer cells to grow and multiply. By blocking these signals, Gefitinib can slow cancer cell growth, particularly in cancers that depend on EGFR to grow.
Interactions
Interactions with other medicines
- Rifampicin, phenytoin, carbamazepine, and St. John’s wort may reduce the amount of gefitinib in your body and make it less effective. Generally, avoid these unless your doctor advises otherwise.
- Ketoconazole and itraconazole may increase the amount of gefitinib in your body and increase the risk of side effects. Your doctor may adjust your treatment if needed.
- Medicines for acidity, such as proton pump inhibitors, H2 blockers, and antacids, may reduce gefitinib absorption and make it less effective. Ask your doctor before using them.
- Tell your doctor about all prescription medicines, over-the-counter medicines, vitamins, supplements, and herbal products you take, especially blood thinners such as warfarin.
Interactions with food items
You can take the tablets with or without food, giving you flexibility in your daily dosing schedule. Avoid grapefruit or grapefruit juice unless your doctor advises otherwise, as they may affect drug metabolism.
Dosage
Overdose
If an overdose is suspected, contact your doctor or seek immediate medical attention. Symptoms of an overdose can include severe diarrhea, intense skin toxicity, and elevated liver enzymes. Management involves supportive hospital care, symptomatic treatment, and close clinical monitoring.
Missed a Dose
If you miss a dose of Gefitinib, take it as soon as you remember on the same day. If it is almost time for your next scheduled dose, skip the missed dose and resume your normal dosing schedule. Do not take a double dose to make up for a missed dose.
Frequently Asked Questions (FAQs)
Articles
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References:
- DailyMed. Gefitinib prescribing information. 2026 [Cited 17th Sep 2026]
- electronic medicines compendium (emc). Gefitinib Summary of Product Characteristics. 2026 [Cited 17th Sep 2026]
- Central Drugs Standard Control Organisation (CDSCO). Drugs@CDSCO [Internet]. New Delhi: Directorate General of Health Services, Ministry of Health & Family Welfare, Government of India. 2026 [Cited 17th Sep 2026]
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