The date on which a patent was filed with the relevant government.There is additional data available for commercial users including Adverse Effects, Contraindications, and Blackbox Warnings.
Development of third-generation EGFR-TKIs, such as osimertinib, has been in response to altered tumour resistance patterns following treatment and toxic side effects that impact patient quality of life. 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. Learn more about the TAGRISSO mechanism of action. Developed by AstraZeneca, the medication was approved as a cancer treatment in 2017 by both the Food and Drug Administration and the European Commission.
2014 Oct 23;57(20):8249-67. doi: 10.1021/jm500973a. MOA TAGRISSO: Designed to potently and selectively inhibit EGFR sensitising and resistance mutations 1,2 TAGRISSO is a third-generation, irreversible EGFR TKI designed to 1,2:. Caution should also be taken in people with a predisposition to Very common (greater than 10% of clinical trial subjects) adverse effects include diarrhea, Common (between 1% and 10% of clinical trial subjects) adverse effects include It exhibits linear pharmacokinetics; the median time to Cmax is 6 hours (range 3–24 hours). Osimertinib is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) that binds to certain mutant forms of EGFR (T790M, L858R, and exon 19 deletion) that predominate in non-small cell lung cancer (NSCLC) … The main metabolic pathways are oxidation (predominantly by CYP3A) and dealkylation. Epub 2014 Oct 1. Osimertinib is primarily eliminated through excretion in the feces (68%), to a lesser extent through urine (14%), while only 2% is excreted unchanged. Treatment with first-generation EGFR-TKIs (gefitinib and erlotinib) has been associated with the development of resistance through activating mutations in the EGFR gene. Osimertinib is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) that binds to certain mutant forms of EGFR (T790M, L858R, and exon 19 deletion) that predominate in non-small cell lung cancer (NSCLC) tumours following treatment with first-line EGFR-TKIs.
MECHANISM OF ACTION: Osimertinib is a third-generation, oral, irreversible epidermal growth factor receptor (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. J Med Chem. The mean volume of distribution at steady state is 986 L.Plasma protein binding is likely high due to its physiochemical properties.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. 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. Know how this interaction affects the subject drug.A unique ID assigned by the FDA when a product is submitted for approval by the labeller.A governmentally-recognized ID which uniquely identifies the product within its regulatory market.Finlay MR, Anderton M, Ashton S, Ballard P, Bethel PA, Box MR, Bradbury RH, Brown SJ, Butterworth S, Campbell A, Chorley C, Colclough N, Cross DA, Currie GS, Grist M, Hassall L, Hill GB, James D, James M, Kemmitt P, Klinowska T, Lamont G, Lamont SG, Martin N, McFarland HL, Mellor MJ, Orme JP, Perkins D, Perkins P, Richmond G, Smith P, Ward RA, Waring MJ, Whittaker D, Wells S, Wrigley GL: Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor. Osimertinib is an oral, third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) drug developed by AstraZeneca Pharmaceuticals. Osimertinib is used to treat locally advanced or metastatic In the USA, EGFR exon 19 deletions, exon 21 L858R mutations or the T790M status of the patient prior to treatment with osimertinib must be detected by a federally approved companion diagnostic test.In people treated with osimertinib, resistance usually develops within approximately 10 months.It can cause fetal harm, so should not be used in women who are pregnant, and women who take it should avoid becoming pregnant.Caution should be taken in people with a history of interstitial lung disease (ILD), as they were excluded from clinical trials, since the drug can cause severe ILD or pneumonitis.