Osimertinib (AZD-9291) is an EGFR third-generation inhibitor that inhibits the T790M resistance mutation produced by second-generation EGFR inhibitors with irreversible and oral activity. Osimertinib has antitumor activity for the treatment of EGFR-mutated non-small-cell lung cancer. ...
Resistance to tyrosine kinase inhibitors (TKIs) in non-small cell lung carcinoma (NSCLC) remains a significant clinical challenge. Osimertinib, a third-generation TKI, has demonstrated efficacy in overcoming resistance, but novel resistance mechanisms continue to emerge. This cas...
Recent work has revealed the role that miRNAs, particularly tumor suppressor let-7c, play in the invasiveness and acquired resistance of NSCLCs, but the mechanistic details, particularly in Osimertinib resistance, remain elusive. Using two cells lines, H1975 (endogenous T790M mutation) and HCC827-...
regardless of T790M status [22,23,24,25]. However, similar to early-generation EGFR-TKIs, patients receiving osimertinib inevitably experience acquired resistance, and multiple mechanisms encompassing EGFR-dependent and EGFR-independent resistance mechanisms have been identified [26,27,28,29]. The ...
The main challenge that we are all facing is what's next. We used to use gefitinib or erlotinib as frontline therapy. If patients developed a T790M mutation, we sequenced with osimertinib. Now that we are using osimertinib first, we don't see the T790M resistance mutation. We are seeing ...
[2]。体内：Osimertinib（0.1-25 mg/kg；口服；每日一次，持续 14 天）在 PC-9 (ex19del) 和 H1975 (L858R/T790M) 肿瘤异种移植模型中诱导显着的剂量依赖性消退[1] .参考文献：[1]. Cross DA, et al. AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in ...
[1]. Cross DA, et al. AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer. Cancer Discov. 2014 Sep;4(9):1046-61. [2]. Hirano T, et al. Pharmacological and Structural Characterizations of Naquotinib, a Novel Third-Generation EGFR Tyro...
Patients were eligible for the study if they received a diagnosis of advanced lung adenocarcinoma, evidence of EFGR-TKI resistance, acquired EGFR T790M mutation, and an ECOG performance status of 0-1. The primary end point was PFS determined by investigator and secondary end points were ...
Successful salvage therapy using high-dose furmonertinib (AST2818) for non-small-cell lung cancer after Osimertinib resistance: a case report. Anti-Cancer Drugs 33: 768-772, No. 8, Sep 2022. Available from: URL: http://doi.org/10.1097/CAD.0000000000001368 Download references Rights and ...
Osimertinib, a 3rd generation epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI), is the first-line standard-of-care for EGFR-mutant non-small cell lung cancer (NSCLC) patients, while acquired drug resistance will inevitably occur. Int