Other name


International/Other brands





Prescription products

TagrissoTablet, film coated40 mgOralAstra Zeneca Ab
TagrissoTablet80 mgOralAstra Zeneca
TagrissoTablet, film coated81OralAstra Zeneca Lp
TagrissoTablet40 mgOralAstra Zeneca
TagrissoTablet, film coated80 mgOralAstra Zeneca Ab
TagrissoTablet, film coated41OralAstra Zeneca Lp




Osimertinib is an oral, third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) drug developed by AstraZeneca Pharmaceuticals. Its use is indicated for the treatment of metastatic non-small cell lung cancer (NSCLC) in cases where tumour EGFR expression is positive for the T790M mutation as detected by FDA-approved testing and which has progressed following therapy with a first-generation EGFR tyrosine kinase inhibitor. Approximately 10% of patients with NSCLC have a rapid and clinically effective response to EGFR-TKIs due to the presence of specific activating EGFR mutations within the tumour cells. More specifically, deletions around the LREA motif in exon 19 and exon 21 L858R point mutations are correlated with response to therapy.


Metastatic Non-Small Cell Lung Cancer

Other indications


Mechaism of action



The median time to Cmax was found to be 6 hours.


Osimertinib is metabolized to at least two pharmacologically active metabolites, AZ7550 and AZ5104, that circulate at approximately 10% of the concentration of the parent compound. Biochemical assays have shown that AZ7550 has similar potency and efficacy to osimertinib, while AZ5104 is more potent against mutant and wild-type EGFR. The main metabolic pathways are oxidation (predominantly by CYP3A) and dealkylation.


Across clinical trials, interstitial lung disease (ILD)/pneumonitis occurred in 3.3% of treated patients with 0.5% of these being fatal. There is also a change of QTc interval prolongation; electrocardiogram and electrolytes should be monitored in patients with a history or predisposition for QTc prolongation. Cardiomyopathy occurred in 1.4% of patients, therefore left ventricular ejection fraction (LVEF) should be measured at baseline and then every 3 months during treatment. Osimertinib can cause embryo-fetal toxicity, requiring female patients to take effective birth control during therapy and for 6 weeks after final dose.