Tagrisso

Osimertinib

Adjuvant treatment after complete tumour resection (stage IB, II, or resectable IIIA) in adults w/ NSCLC whose tumours have epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 (L858R) substitution mutations. 1st-line treatment of patients w/ locally advanced or metastatic NSCLC whose tumours have EGFR exon 19 deletions or exon 21 (L858R) substitution mutations. Adults w/ locally advanced or metastatic EGFR T790M mutation +ve NSCLC whose disease has progressed on or after EGFR tyrosine kinase inhibitor (TKI) therapy.

80 mg once daily, may be reduced to 40 mg once daily if necessary. Patient in adjuvant setting Duration of treatment: Until disease recurrence or unacceptable toxicity; max: 3 yr. Patient w/ locally advanced or metastatic lung cancer Duration of treatment: Until disease progression or unacceptable toxicity.

May be taken with or without food: Swallow whole, do not chew/crush/split. For patients w/ swallowing difficulties, disperse tab in 50 mL non-carbonated water & stir w/o crushing. Take soln immediately. Rinse glass w/ another ½ glass of water & drink. Alternatively, disperse in 15 mL non-carbonated water & administer via nasogastric tube. Rinse w/ another 15 mL of water & administer. Administer soln w/in 30 min.

Hypersensitivity. Concomitant use w/ St. John's wort.

Perform a validated test using tumour tissue DNA from biopsy or surgical specimen when considering use as an adjuvant therapy after complete tumour resection in patients w/ NSCLC, EGFR mutation +ve status; using either tumour tissue DNA or circulating tumour DNA obtained from a plasma sample when considering use for locally advanced or metastatic NSCLC. Determine for +ve EGFR mutation status (activating EGFR mutations for 1st-line treatment or T790M mutations following progression on or after EGFR TKI therapy). Permanently discontinue if ILD is confirmed or w/hold treatment & promptly investigate if worsening of resp symptoms occur; & in patients who develop QTc interval prolongation in combination w/ Torsade de pointes, polymorphic ventricular tachycardia, signs & symptoms of serious arrhythmia. Immediately interrupt or discontinue use if signs & symptoms suggestive of SJS appear. Avoid use in patients w/ congenital long QT syndrome. Periodic monitoring w/ ECGs & electrolytes in patients w/ CHF, electrolyte abnormalities or those taking QTc prolonging medications. W/hold treatment in patients who develop a QTc interval >500 msec on at least 2 separate ECGs until the QTc interval is <481 msec or recovery to baseline if the QTc interval is ≥481 msec, resume treatment at a reduced dose. Consider cardiac monitoring including left ventricular ejection fraction (LVEF) assessment at baseline & during treatment in patients w/ cardiac risk factors & those w/ conditions that can affect LVEF; who develop relevant cardiac signs & symptoms during treatment. Promptly refer to an ophthalmologist if patient presents w/ signs & symptoms suggestive of keratitis (eg, acute or worsening of eye inflammation, lacrimation, light sensitivity, blurred vision, eye pain &/or red eye). Contact lens use may also be a risk factor for keratitis & ulceration. Do not drive or use machines if patient experience symptoms affecting the ability to conc & react. Not recommended in moderate or severe hepatic impairment. Severe & end-stage renal impairment. May impair fertility. Advise women of childbearing potential to avoid becoming pregnant while receiving therapy; use effective contraception after completion of treatment (ie, for at least 6 wk for females; 4 mth for males). Not recommended during pregnancy & in women of childbearing potential not using contraception. Discontinue breast-feeding during treatment. Childn or adolescent <18 yr. Closely monitor elderly >65 yr or patients w/ low body wt <50 kg.

Decreased appetite; diarrhoea, stomatitis; rash, dry skin, paronychia, pruritus; decreased platelet count, leucocytes, lymphocytes & neutrophils. Epistaxis, ILD; palmar-plantar erythrodysaesthesia syndrome, alopecia, urticaria; increased blood creatinine & blood creatine phosphokinase.

Decreased exposure w/ strong (eg, phenytoin, rifampicin, & carbamazepine) & moderate (eg, bosentan, efavirenz, etravirine, modafinil) CYP3A4 inducers; avoid concomitant use. Increased AUC & C_max of rosuvastatin. Decreased AUC & C_max of simvastatin. Increased exposure of medications w/ disposition dependent upon P-gp & w/ narrow therapeutic index (eg, digoxin, dabigatran, aliskiren). Concomitant use of St. John's wort is contraindicated.

Targeted Cancer Therapy

L01EB04 - osimertinib ; Belongs to the class of epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors. Used in the treatment of cancer.

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