Treatment of metastatic epidermal growth factor receptor (EGFR) T790M mutation-positive non-small cell lung cancer (NSCLC), as detected by an approved test, in patients who have progressed on or after EGFR tyrosine kinase inhibitor (TKI) therapy.

Osimertinib is an irreversible epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor which binds to select mutant forms of EGFR, including T790M, L858R, and exon 19 deletion at lower concentrations than wild-type. Osimertinib is selective for sensitizing mutations and the T790M resistance mutation, which is the most common mechanism of resistance to EGFR tyrosine kinase inhibitors.

Metabolism: Hepatic; predominantly oxidation (via CYP3A4) and dealkylation to 2 active metabolites (AZ7550 and AZ5104); Bioavailability: AUC is increased by 19% with a high-fat, high-calorie meal; Elimination: faces (68%), urine (14%); Elimination Half-life: Mean (estimated): 48 hours.

None

Based on data from animal reproduction studies and the mechanism of action, use during pregnancy is expected to cause fetal harm. Women of reproductive potential should use effective contraception during therapy and for 6 weeks after the last dose. Males with female partners of reproductive potential should also use effective contraception during therapy and for 4 months after the last dose.

Advise women not to breastfeed during treatment with TAGRISSO and for 2 weeks after the final dose.

Skin rash (41%, including erythematous rash, macular rash, maculopapular rash, papular rash, pustular rash, erythema, folliculitis, acne vulgaris, dermatitis, dermatitis acneiform), xeroderma (31%), nail disease (25%), pruritus (14%);  Diarrhea (42%); Hyponatremia (26%), hypermagnesemia (20%); Lymphopenia (63%), thrombocytopenia (54%,), anemia (44%), neutropenia (33%).

Oral: 80 mg once daily until disease progression or unacceptable toxicity. May be administered with or without food.

• For patients who have difficulty swallowing tablets, disperse tablet in ~50 mL of noncarbonated water (only), stir until tablet is completely dispersed and immediately swallow or administer through NG tube. Rinse container with 120 to 240 mL water and immediately drink or administer through NG tube. Do not crush, heat, or ultrasonicate during preparation.