Osimertinib, sold under the brand name Tagrisso, is a medication used to treat non-small-cell lung carcinomas with specific mutations. (wikipedia.org)
The generic ingredient in TAGRISSO is osimertinib mesylate . (drugpatentwatch.com)
Tagrisso (osimertinib) is a kinase inhibitor indicated for patients with metastatic epidermal growth factor T790M mutation-positive lung cancer. (shu.edu)
T790M13
In a subgroup of these patients we identified an association between selection of EGFR T790M -negative but EGFR G724S -positive subclones and osimertinib resistance. (nature.com)
Third-generation EGFR inhibitors such as osimertinib have been designed to overcome acquired resistance induced by the EGFR T790M gatekeeper mutation 10 . (nature.com)
Clinical results show that patients treated with osimertinib respond in up to 71% in the background of an acquired EGFR T790M mutation 11 , 12 . (nature.com)
Patient P1 (UICC stage IIIA, 59 years old, female) received osimertinib within the AURA trial (NCT01802632) after progression on erlotinib and the detection of an acquired EGFR T790M mutation (T1) (Fig. 1a ). (nature.com)
Osimertinib is used to treat locally advanced or metastatic non-small-cell lung cancer (NSCLC), if the cancer cells are positive for the T790M mutation in the gene coding for EGFR or for activating EGFR mutations. (wikipedia.org)
In the US, 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 companion diagnostic test. (wikipedia.org)
Recently, osimertinib has been recommended as the first-line treatment for patients with advanced or metastatic NSCLC who carry EGFR-sensitive mutations or acquired T790M resistant mutations after using first or second-generation EGFR-TKIs [ 8 ]. (biomedcentral.com)
Osimertinib is a kinase inhibitor of the epidermal growth factor receptor (EGFR), which binds irreversibly to certain mutant forms of EGFR (T790M, L858R, and exon 19 deletion) at approximately 9-fold lower concentrations than wild-type. (drugcentral.org)
In cultured cells and animal tumor implantation models, osimertinib exhibited anti-tumor activity against NSCLC lines harboring EGFR-mutations (T790M/L858R, L858R, T790M/exon 19 deletion, and exon 19 deletion) and, to a lesser extent, wild-type EGFR amplifications. (drugcentral.org)
Osimertinib is an oral, irreversible EGFR-TKI that is selective for both EGFR and T790M resistance mutations with activity in the central nervous system (CNS). (shu.edu)
These findings were confirmed in a pooled analysis of two subsequent phase 2 studies of osimertinib (at a dose of 80 mg once daily) in 411 patients with T790M-positive non-small-cell lung cancer, in which the response rate was 66% on blinded independent central review and the median duration of progression-free survival was 11.0 months. (shu.edu)
Interstitial Lung Disease Induced by Osimertinib for Epidermal Growth Factor Receptor (EGFR) T790M-positive Non-small Cell Lung Cancer. (cdc.gov)
Among the third-generation EGFR TKIs, osimertinib is today the only drug approved by the Food and Drug Administration and the European Medicines Agency to treat metastatic EGFR T790M NSCLC patients who have progressed on or after EGFR TKI therapy. (researchgate.net)
Tyrosine kinase inh1
A rapid, sensitive and reproducible ultra-high performance liquid chromatography mass spectrometry method was developed and validated for simultaneous determination of seven tyrosine kinase inhibitors (dasatinib, foretinib, osimertinib, gefitinib, ibrutinib, linifanib and motesanib) in human plasma samples using quizartinib as internal standard (IS). (ampksignal.com)
Diagnosed in osimertinib-resistant1
Here, we characterized the role of the acquired EGFR G724S mutation that was diagnosed in osimertinib-resistant lesions of four individual EGFR 19del -mutant LADC patients. (nature.com)
NSCLC3
The widespread clinical use of osimertinib in patients with NSCLC has made acquired resistance an urgent issue. (biomedcentral.com)
The subgroup of patients with epidermal growth factor receptor ( EGFR ) mutation-positive advanced squamous non-small cell lung cancer (NSCLC) benefitted from the addition of necitumumab to gemcitabine plus cisplatin, a late-breaking study presented at the European Lung Cancer Conference (ELCC) 2016 has shown. (cancertherapyadvisor.com)
His leadership in targeted therapeutics resulted in a 2020 ASCO plenary talk and publication of results of the third-generation EGFR-inhibitor osimertinib for the treatment of resected EGFR-mutant NSCLC in the New England Journal of Medicine. (yale.edu)
Resistance6
In people treated with osimertinib, resistance usually develops within approximately 10 months. (wikipedia.org)
Upregulation of BETs contributed to the osimertinib resistance of H1975 cells. (biomedcentral.com)
Our findings provided new strategies for the treatment of osimertinib resistance. (biomedcentral.com)
Clarifying the mechanism of osimertinib resistance would provide new therapeutic strategies for patients and facilitate the design of drugs that targeting key molecules involved in resistance. (biomedcentral.com)
The objective of this project is to find new targeted treatments and drug combinations that can tackle cancer evolution and osimertinib resistance. (prnewswire.com)
Every day, we watch fellow patients struggle with osimertinib resistance or small cell transformation. (prnewswire.com)
Mesylate2
Additional details are available on the osimertinib mesylate profile page. (drugpatentwatch.com)
There is one tentative approval for the generic drug ( osimertinib mesylate ), which indicates the potential for near-term generic launch. (drugpatentwatch.com)
20211
Methods: CT imaging of patients operated in our center from January 2016 to August 2021 for mediastinal lesions was reviewed. (bvsalud.org)
Anticancer1
Anticancer research 2016 Sep 36 (9): 4951-4. (cdc.gov)
Epidermal growth f1
Osimertinib preferentially binds irreversibly to mutated epidermal growth factor receptor proteins, particularly those with more common mutations in lung cancer such as L858R mutation or an exon 19 deletion. (wikipedia.org)
Inhibitors2
Our data provide a mechanistic basis for the osimertinib-induced selection of EGFR G724S -mutant clones and a rationale to treat these patients with clinically approved second-generation EGFR inhibitors. (nature.com)
More recent data indicate that osimertinib treatment is even superior to single agent first-generation inhibitors such as erlotinib or gefitinib in terms of PFS and overall survival (OS) in the first-line setting 13 . (nature.com)
Erlotinib2
Patients were randomly assigned between November 2012 and August 2016 to receive erlotinib 150 mg daily plus bevacizumab 15 mg/kg every 3 weeks (n = 43) or erlotinib alone (n = 45). (ascopost.com)
among patients with available data, osimertinib was received by 10 patients in the combination group and 13 patients in the erlotinib group. (ascopost.com)
Tumor1
Despite high tumor response rates, patients treated with EGFR targeted therapies, such as osimertinib, inevitably develop disease progression. (prnewswire.com)
Metastatic1
In the phase 3 study , all patients had evidence of advanced or metastatic non-small-cell lung cancer and of disease progression after first-line EGFR-TKI therapy and were randomized in a 2:1 ratio to receive oral osimertinib (at a dose of 80 mg once daily) or intravenous pemetrexed (500 mg per square meter of body-surface area) plus either carboplatin or cisplatin. (shu.edu)
Selective1
He led the first-in man clinical trial of the mutant selective EGFR inhibitor osimertinib which was approved by the Food and Drug Administration in 2015. (voronoi.io)
Clinical1
He is an elected member to the American Society of Clinical Investigation (2008), American Association of Physicians (2016) and the Finnish Academy of Science and Letters (2016). (voronoi.io)
Lung4
His team had tested the use of Osimertinib in a Phase-III trial of 682 patients with later-stage non-small-cell lung cancer that presented with a mutated form of a cell growth gene and the protein it produces. (onlysky.media)
Osimertinib in Resected EGFR -Mutated Non-Small-Cell Lung Cancer. (nih.gov)
In 2016, there will be an estimated 224,390 new cases of lung cancer accounting for about 14 percent of all cancers: an estimated 117,920 cases will be diagnosed in men and 106,470 in women. (healthywomen.org)
Lung cancer is the leading cause of cancer-related mortality in the U.S. According to NCI SEER data, approximately 6.3% of men and women will be diagnosed with lung and bronchus cancer at some point during their lifetime (based on 2014-2016 data). (medpagetoday.com)
Patients2
Between October 2014 and September 2016, 32 eligible patients were enrolled in ABC-study at our institutes. (oncotarget.com)
Seven of these 8 patients underwent osimertinib therapy. (oncotarget.com)
Approvals1
In 2016, watch for the approvals of new drugs to treat Duchenne muscular dystrophy (DMD), as well as breakthrough therapies for cancer and more options to treat hepatitis C. More information about selected specialty pipeline medications can be found below. (pharmacytimes.com)
Approval2
Osimertinib was designated as a Breakthrough Therapy in April 2014, based on Phase I trial results, and the drug was provisionally approved under the FDA accelerated approval program with a priority review voucher, in November 2015. (wikipedia.org)
In February 2016, the EMA provisionally approved osimertinib under an accelerated process-the first approval under the program. (wikipedia.org)
Treatment1
Osimertinib treatment resulted in a partial response (54% reduction based on RECIST 1.1) (Supplementary Fig. 1B , 1D ). (nature.com)
Year1
The four-year disease-free survival (DFS) rate, over a placebo, was 70 percent for those on Osimertinib, versus 29 percent for those on the placebo. (onlysky.media)
Effect1
2016. The effect of potential electronic nicotine delivery system regulations on nicotine product selection. . (cornell.edu)
Osimertinib resistant cell lines were established by culturing sensitive cells in chronically increasing doses of osimertinib. (biomedcentral.com)
We found that bromodomain and extra-terminal proteins (BETs) were upregulated in osimertinib resistant (H1975-OR) cells compared with those in the paired parental cells (H1975-P), and that knockdown of BETs significantly inhibited the growth of H1975-OR cells. (biomedcentral.com)
BETs were not upregulated in osimertinib resistant HCC827 cells compared with parental cells, while TSA and vorinostat exhibited equal inhibitory effects on both cell types. (biomedcentral.com)