What It Is and What It Treats
Gefiren contains gefitinib, a targeted therapy that blocks
the EGFR (epidermal growth factor receptor) tyrosine kinase enzyme — a protein
that EGFR-mutant cancer cells rely on to grow and divide. By disrupting this signaling
pathway, gefitinib induces cancer cell death and arrests tumor progression.
It is indicated as first-line monotherapy for locally
advanced or metastatic non-small cell lung cancer (NSCLC) in adults whose tumors
carry confirmed activating EGFR mutations — specifically exon 19 deletions or
exon 21 L858R substitutions.
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EGFR TESTING MANDATORY Gefitinib must only
be initiated after laboratory confirmation of an activating EGFR mutation. In
unselected NSCLC, gefitinib confers no survival benefit. Mutation testing
should be performed on tumor tissue (FFPE biopsy) or plasma circulating
tumour DNA (liquid biopsy). |
Dosing and Administration
Recommended dose: 250mg once daily, taken with or without
food, at the same time each day. Swallow tablets whole with water.
• Missed dose: take as soon as
remembered, unless the next dose is within 12 hours — in that case, skip the
missed dose. Never double up.
• Cannot swallow whole: dissolve in
half a glass of still water, stir for approximately 15 minutes, drink
immediately, then rinse and drink the glass residue.
• Dose modifications for Grade 3+
toxicity (rash, diarrhoea, ILD): interrupt therapy until resolved to Grade 1 or
less; restart at 250mg. Recurrence warrants permanent discontinuation.
• Hepatic impairment: no routine dose
adjustment for mild-moderate impairment; use with caution in severe impairment
(Child-Pugh C).
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PATIENT TIP:
Take
your tablet at the same time every day. Contact your oncologist the same day
if you develop new shortness of breath, cough, or fever — do not wait for
your next scheduled appointment. |
Side Effects
|
Frequency |
Side Effects |
|
Very Common (>1 in 10) |
Acneiform skin rash (50–70%), diarrhoea, dry
skin, nausea, reduced appetite, mouth sores, elevated liver enzymes (ALT/AST) |
|
Common |
Paronychia (nail fold infection),
conjunctivitis, hair thinning, fatigue, vomiting |
|
Serious — Seek Urgent Help |
Interstitial lung disease (ILD): acute
breathlessness, dry cough, fever — STOP gefitinib immediately. Severe
hepatotoxicity: jaundice, dark urine, right upper quadrant pain. Corneal
erosion. Stevens-Johnson syndrome (rare). |
Contraindications and Cautions
• Known severe hypersensitivity to
gefitinib
• Pre-existing interstitial lung
disease or pulmonary fibrosis — use with extreme caution; ILD risk is higher
• Severe hepatic impairment — risk of
significant drug accumulation
• Pregnancy: Gefitinib is embryotoxic
and teratogenic. Effective contraception is required during treatment and for at
least 1 month after the last dose.
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CAUTION:
ILD
occurs in approximately 1–3% of patients (higher in Japanese patients). It
may present acutely. Permanently discontinue gefitinib if ILD is confirmed.
Treat with high-dose corticosteroids. |
Key Drug Interactions
• Strong CYP3A4 inducers (rifampicin,
phenytoin, carbamazepine, St. John's Wort): significantly reduce gefitinib
plasma levels. Consider a dose increase to 500mg if co-administration is
unavoidable.
• Proton pump inhibitors (omeprazole,
pantoprazole): raise gastric pH and reduce gefitinib absorption by
approximately 47%. Use H2 blockers or antacids at separate times where
possible.
• Warfarin: gefitinib inhibits CYP2C9,
increasing warfarin effect. Monitor INR weekly for the first month, then
monthly.
• Strong CYP3A4 inhibitors
(itraconazole, ketoconazole): increase gefitinib exposure — monitor for
increased toxicity.
Clinical Monitoring Schedule
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PRESCRIBER NOTE LFTs: monthly for
first 3 months, then every 3 months. CT chest: baseline, 8–12 weeks (first
response assessment), then every 3 months. INR: weekly for the first month in
warfarin patients. On disease progression, re-biopsy or liquid biopsy for
T790M mutation — T790M-positive: switch to osimertinib (3rd generation EGFR
TKI). |
Storage
• Store below 30°C in original blister
packaging. Protect from moisture and heat. Keep out of reach of children and
pregnant women.
Frequently Asked Questions
Q: What is Gefiren used for?
Gefiren treats
non-small cell lung cancer (NSCLC) in adults whose tumours carry specific EGFR
gene mutations. It is a targeted therapy — it selectively attacks cancer cells
with a specific molecular abnormality rather than all rapidly dividing cells.
Q: Do I need a genetic test before starting?
Yes, without exception.
Gefitinib only works if your tumour carries certain EGFR mutations (exon 19
deletion or L858R). The test is performed on a biopsy sample or a blood test
(liquid biopsy). Your oncologist will arrange this before prescribing.
Q: What should I do if I develop breathlessness?
Stop taking Gefiren
immediately and go to the hospital or contact your oncologist the same day. New
breathlessness, dry cough, or fever may indicate interstitial lung disease
(ILD) — a rare but potentially life-threatening complication requiring urgent
assessment.
Q: Does gefitinib interact with my stomach acid medicines?
Yes — proton pump
inhibitors like omeprazole reduce gefitinib absorption significantly. Discuss
alternatives with your oncologist. If a PPI is essential, take it at different
times from gefitinib where possible.