Trexa

Gefitinib

Adult patients w/ locally advanced or metastatic NSCLC w/ activating mutations of epidermal growth factor receptor tyrosine kinase (EGFR-TK).

250 mg once daily.

May be taken with or without food: May also be dispersed in ½ glass of plain, non-carbonated water. Drop tab in water & stir w/o crushing until it disperses (approx 15 min). Drink immediately. Rinse glass w/ another ½ glass of water & drink. Dispersed liqd may also be administered via nasogastric tube.

Hypersensitivity. Lactation.

Discontinue use if ILD, ulcerative keratitis is confirmed. Severe or persistent diarrhoea, nausea, vomiting or anorexia; keratitis; GI ulceration, bowel metastases at perforation site; age, smoking. Assess EGFR mutation of tumour tissue prior to treatment. Periodically monitor LFTs. Regularly monitor prothrombin time or INR changes in patients 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)-containing herbal prep. Concomitant use w/ medicinal products causing significant sustained gastric pH elevations eg, PPIs & H₂-antagonists, antacids; steroids or NSAIDs. May affect ability to drive & use machines. Mild to moderate hepatic function changes. Women of childbearing potential should use effective contraception. Not to be used during pregnancy. Not recommended in childn or adolescents.

Anorexia; diarrhoea, vomiting, nausea, stomatitis; elevated ALT; skin reactions eg, pustular rash including skin fissures; asthenia. Conjunctivitis, blepharitis, dry eye; haemorrhage eg, epistaxis, haematuria; ILD; dehydration, dry mouth; elevated 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. Reduced efficacy w/ CYP3A4 inducers eg, phenytoin, carbamazepine, rifampicin, barbiturates or St. John's wort (Hypericum perforatum). Altered plasma conc of CYP2D6 substrates 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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