Figet

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

250 mg once daily, at about the same time each day.

May be taken with or without food: Swallow whole w/ some water or if dosing of whole tab is not possible, tab may be administered as a dispersion in water (non-carbonated). No other liqd should be used. W/o crushing, drop tab in ½ a glass of drinking water, swirl occasionally until tab is dispersed (may take up to 20 min). The dispersion should be drunk immediately after dispersion is complete (ie, w/in 60 min). The glass should be rinsed w/ ½ of glass of water which should also be drunk. The dispersion can also be administered through a nasogastric or gastrostomy tube.

Hypersensitivity. Breast-feeding.

Discontinue treatment if ILD is confirmed or if changes in liver function are severe. Interrupt treatment in case of ulcerative keratitis; permanently discontinue if symptoms do not resolve or if symptoms recur on treatment reintroduction. Cautiously use in presence of mild to moderate changes in liver function. Patients should be advised to seek medical advice immediately if experiencing severe or persistent diarrhoea, nausea, vomiting or anorexia as these may indirectly lead to dehydration. Reports of CNS haemorrhages in a phase I/II trial studying the use of gefitinib & radiation in paed patients w/ newly diagnosed brain stem glioma or incompletely resected supratentorial malignant glioma. Reports of GI perforation. Periodic LFT is recommended. Closely monitor for adverse reactions in patients w/ CYP2D6 poor metaboliser genotype & in patients w/ moderate to severe hepatic impairment. Concomitant use w/ warfarin; medicinal products causing significant sustained elevation in gastric pH eg, PPIs & H₂-antagonists; antacids; vinorelbine. Avoid concomitant administration w/ CYP3A4 inducers (eg, phenytoin, carbamazepine, rifampicin, barbiturates or herbal prep containing St. John's wort/Hypericum perforatum). Reports of asthenia; patients experiencing this symptom should be cautious when driving or using machines. Patients w/ CrCl ≤20 mL/min. Women of childbearing potential must be advised not to get pregnant during therapy. Not to be used during pregnancy unless clearly necessary.

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

Increased plasma conc w/ potent CYP3A4 inhibitors (eg, ketoconazole, posaconazole, voriconazole, PIs, clarithromycin, telithromycin); potent CYP2D6 inhibitors. Increased mean AUC during pre-treatment w/ itraconazole (potent CYP3A4 inhibitor). Decreased plasma conc w/ CYP3A4 inducers (eg, phenytoin, carbamazepine, rifampicin, barbiturates or St. John's wort/Hypericum perforatum). Reduced mean AUC during pre-treatment w/ rifampicin (potent CYP3A4 inducer). Reduced plasma conc w/ substances that cause significant sustained elevation in gastric pH or high doses of short-acting antacids. Reduced mean AUC w/ ranitidine at a dose that caused sustained elevations in gastric pH ≥5. Increased exposure to metoprolol (CYP2D6 substrate). Dose modification of CYP2D6 substrate should be considered especially for those w/ narrow therapeutic window. Reports of INR elevations &/or bleeding w/ warfarin. May exacerbate neutropenic effect of vinorelbine.

Targeted Cancer Therapy

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

Rx