Gefitinib 250 Eurodrug

Gefitinib

Monotherapy for locally advanced or metastatic NSCLC w/ activating mutations of epidermal growth factor receptor tyrosine kinase in adults.

250 mg once daily.

May be taken with or without food: Take at the same time each day. Swallow whole w/ water or may be dispersed in ½ glass of non-carbonated drinking water. No other liqd should be used. Drop the tab in water & w/o crushing it, swirl until dispersed (approx 20 min). Drink immediately or w/in 60 min. Rinse the glass w/ another ½ glass of water & drink. Dispersed liqd may also be administered via nasogastric or gastrostomy tube.

Hypersensitivity. Lactation.

Discontinue use if ILD is confirmed. Consider discontinuation in case of severe changes in liver function; permanently if symptoms of ulcerative keratitis recur. Interrupt treatment in worsening resp symptoms eg, dyspnoea, cough & fever; if ulcerative keratitis is confirmed. Abnormal LFTs; hepatic failure. Smoking, poor performance status (PS ≥2), CT scan evidence of reduced normal lung (≤50%), recent diagnosis of NSCLC (<6 mth), pre-existing ILD, concurrent cardiac disease, & extensive areas adherent to pleura (≥50%). Severe or persistent diarrhoea, nausea, vomiting or anorexia; signs & symptoms of keratitis; GI perforation. Assess epidermal growth factor receptor mutation of tumour tissue prior to treatment. Periodically test liver function. Regularly monitor prothrombin time or INR changes in patients concomitantly taking warfarin. Not to be taken by patients w/ galactose intolerance, total lactase deficiency or glucose-galactose malabsorption. Avoid concomitant use w/ CYP3A4 inducers eg, phenytoin, carbamazepine, rifampicin, barbiturates or St. John's wort (Hypericum perforatum). Concomitant use w/ potent CYP3A4 inhibitors; medicinal products causing significant sustained gastric pH elevations eg, PPIs & H₂ antagonists, antacids; vinorelbine; steroids or NSAIDs. May affect ability to drive & use machines. Mild to moderate liver function changes. Moderate to severe hepatic impairment (Child-Pugh B or C). Renal impairment (CrCl ≤20 mL/min). Women of childbearing potential should not get pregnant during therapy. Not to be used during pregnancy. Discontinue lactation while on therapy. Childn or adolescents <18 yr. Elderly (≥65 yr).

Mild or moderate anorexia; mild or moderate diarrhoea & vomiting, mild nausea & stomatitis; mild to moderate elevations in ALT; mild or moderate skin reactions (eg, pustular rash, itchy w/ dry skin including skin fissures on erythematous base); mild asthenia. Mild conjunctivitis, blepharitis & dry eye; haemorrhage eg, epistaxis & haematuria; severe ILD; dehydration, secondary to diarrhoea, nausea, vomiting or anorexia, mild dry mouth; mild to moderate elevations in AST; nail disorder, alopecia, allergic reactions including angioedema & urticaria; asymptomatic lab elevations in blood creatinine, proteinuria, cystitis; pyrexia. Bullous conditions including TEN, SJS & erythema multiforme.

Increased plasma conc w/ potent CYP3A4 inhibitors eg, ketoconazole, posaconazole, voriconazole, PIs, clarithromycin, telithromycin. Increased mean AUC w/ itraconazole as pre-treatment. Increased metabolism & decreased plasma conc w/ CYP3A4 inducers eg, phenytoin, carbamazepine, rifampicin, barbiturates or St. John's wort (Hypericum perforatum). Reduced mean AUC w/ rifampicin as pre-treatment; ranitidine. Reduced plasma conc & efficacy w/ substances causing significant sustained gastric pH elevation; high-dose short-acting antacids. Increased exposure w/ metoprolol. INR elevations &/or bleeding events w/ warfarin. Concomitant use w/ CYP2D6 substrates & products w/ narrow therapeutic window.

Targeted Cancer Therapy

L01EB01 - gefitinib ; Belongs to the class of epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors. Used in the treatment of cancer.

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