Geftinat

1st-line monotherapy for adults w/ locally advanced or metastatic NSCLC w/ activating mutations of EGFR-TK. Locally advanced or metastatic NSCLC in patients who have previously received chemotherapy.

250 mg once daily. Patients w/ poorly tolerated diarrhoea or skin adverse reactions Reinstate 250 mg dose after 14 days of therapy interruption.

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

Hypersensitivity. Breast-feeding.

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. Cerebral haemorrhage; severe or persistent diarrhoea, nausea, vomiting or anorexia; signs & symptoms of acute or worsening of keratitis (eg, eye inflammation, lacrimation, light sensitivity, blurred vision, eye pain &/or red eye); GI perforation. Patients w/ underlying history of GI ulceration, age, smoking or bowel metastases at sites of perforation. Assess EGFR mutation of tumour tissue. Periodically monitor liver function. Regularly monitor prothrombin time or INR changes in patients taking warfarin. Concomitant use w/ CYP3A4 inducers eg, phenytoin, carbamazepine, rifampicin, barbiturates or St. John's wort; medicinal products causing significant sustained gastric pH elevations eg, PPIs, H₂-antagonists; vinorelbine; steroids or NSAIDs. Not to be taken by patients w/ galactose intolerance, total lactase deficiency or glucose-galactose malabsorption. May affect ability to drive & use machines. Moderate to severe hepatic impairment (Child-Pugh B or C). Patients w/ CrCl ≤20 mL/min. Women of childbearing potential should not get pregnant during therapy. Not to be used during pregnancy. Discontinue breast-feeding while on therapy. Childn & adolescents <18 yr.

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

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

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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