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GEFIREN (GEFITINIB) 250MG 30`S

Ksh 11,999

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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.

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.

 

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.

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