التفاصيل البيبلوغرافية
العنوان:
Data from AC0010, an Irreversible EGFR Inhibitor Selectively Targeting Mutated EGFR and Overcoming T790M-Induced Resistance in Animal Models and Lung Cancer Patients
المؤلفون:
Li Zhang , Hongyun Zhao , Pei Hu , Ji Jiang , Xiaobo Wang , Li Zhao , Ce Fang , Jia Liu , Xin Fang , Rongda Xu , Biao Xi , Xiaoying Zhang , Wei Tang , Wanhong Xu , Long Mao , Xiao Xu
بيانات النشر:
American Association for Cancer Research (AACR), 2023.
سنة النشر:
2023
الوصف:
AC0010 is a pyrrolopyrimidine-based irreversible EGFR inhibitor, structurally distinct from previously reported pyrimidine-based irreversible EGFR inhibitors, such as osimertinib and rociletinib. AC0010 selectively inhibits EGFR-active and T790M mutations with up to 298-fold increase in potency compared with wild-type EGFR. In a xenograft model, oral administration of AC0010 at a daily dose of 500 mg/kg resulted in complete remission of tumors with EGFR-active and T790M mutations for over 143 days with no weight loss. Three major metabolites of AC0010 were tested and showed no wild-type EGFR inhibition or off-target effects, such as inhibition of IGF-1R. AC0010 is safe in non–small cell lung cancer (NSCLC) patients at a dose range between 50 and 550 mg once per day, and no hyperglycemia or other severe adverse effects were detected, such as grade 3 QT prolongation. The objective responses were observed in NSCLC patients with EGFR T790M mutation. Mol Cancer Ther; 15(11); 2586–97. ©2016 AACR.
URL الوصول:
https://explore.openaire.eu/search/publication?articleId=doi_________::97152cd0dd1be73595146cc57ab86145 https://doi.org/10.1158/1535-7163.c.6538302.v1
حقوق:
OPEN
رقم الأكسشن:
edsair.doi...........97152cd0dd1be73595146cc57ab86145
قاعدة البيانات:
OpenAIRE
