Article
Chemistry, Medicinal
Hajer AlRasheed, Aliyah Almomen, Haya I. Aljohar, Maria Arafah, Rana Y. Almotawa, Manal A. Alossaimi, Nourah Z. Alzoman
Summary: This study evaluated the influence of aspartame on the pharmacokinetics of erlotinib and gefitinib in rats. The results showed that aspartame could alter the pharmacokinetic parameters of both drugs and significantly increase liver enzyme activity. Therefore, the use of aspartame-containing products should be avoided during erlotinib or gefitinib therapy.
Article
Biotechnology & Applied Microbiology
Wei Cao, Jun Ma, Xuan Jiang, Guangyi Gao
Summary: This study investigated the clinical intervention effect of afatinib targeted therapy in patients with non-small-cell lung cancer. The results showed that afatinib targeted therapy significantly improved the treatment effective rate, immune function, and serum EGFR and pro-GRP levels in patients.
Article
Oncology
Chunsheng Wang, Kewei Zhao, Shanliang Hu, Wei Dong, Yan Gong, Minghuan Li, Conghua Xie
Summary: By studying the outcomes of gefitinib and erlotinib in patients with uncommon EGFR mutations in non-small cell lung cancer (NSCLC), it was found that patients with compound mutations had better treatment response, with those containing exon 19 deletion or L858R mutations showing the most significant benefits in response and survival. Additionally, the gefitinib group showed superior treatment efficacy and PFS benefit compared to the erlotinib group.
Article
Pharmacology & Pharmacy
Po-Yen Chen, Chin-Chou Wang, Chien-Ning Hsu, Chung-Yu Chen
Summary: This study compared the relative survival rate of gefitinib, erlotinib, and afatinib in EGFR-mutated advanced lung adenocarcinoma patients in Taiwan. Afatinib showed better overall survival and time to treatment failure outcomes compared to gefitinib and erlotinib, especially in patients with initial brain metastases.
FRONTIERS IN PHARMACOLOGY
(2021)
Article
Critical Care Medicine
Shun Lu, Jianying Zhou, Hong Jian, Lin Wu, Ying Cheng, Yun Fan, Jian Fang, Gongyan Chen, Zhihong Zhang, Dongqing Lv, Liyan Jiang, Rong Wu, Xiangming Jin, Xiaodong Zhang, Junhong Zhang, Conghua Xie, Gengyun Sun, Dongning Huang, Jiuwei Cui, Renhua Guo, Zhigang Han, Zhendong Chen, Jin Liang, Wu Zhuang, Xingsheng Hu, Aimin Zang, Yi Zhang, Shundong Cang, Yuanbo Lan, Xi Chen, Laiyu Liu, Xingya Li, Jun Chen, Rui Ma, Yanzhen Guo, Ping Sun, Panwen Tian, Yueyin Pan, Zhe Liu, Peiguo Cao, Lieming Ding, Yang Wang, Xiaobin Yuan, Pengxiang Wu
Summary: This phase 3 trial compared the efficacy and safety of befotertinib with icotinib as a first-line treatment for patients with EGFR mutation-positive NSCLC. The study found that befotertinib demonstrated superior efficacy in terms of progression-free survival compared to icotinib, although it was associated with more frequent adverse events.
LANCET RESPIRATORY MEDICINE
(2023)
Review
Medicine, General & Internal
Jun Xia, Jiping Zhu, Lei Li, Shiqin Xu
Summary: This meta-analysis found that concomitant use of gastric acid suppressants (AS) in NSCLC patients taking TKIs may be associated with poor survival outcomes.
INTERNATIONAL JOURNAL OF CLINICAL PRACTICE
(2022)
Article
Oncology
Wang Chun Kwok, James Chung Man Ho, Terence Chi Chun Tam, Mary Sau Man Ip, David Chi Leung Lam
Summary: This study found that among NSCLC patients with EGFR mutations, the treatment regimen of using afatinib as the first-line therapy followed by osimertinib after T790M mutation significantly improved overall survival when compared to other EGFR-TKIs in the first-line setting.
Article
Chemistry, Multidisciplinary
Wei Feng, Xi Chen, Shao-xing Guan, Hong-lian Ruan, Yan Huang, Hui-zhen Zhang, Yun-peng Yang, Wen-feng Fang, Hong-yun Zhao, Wei Zhuang, Shuang Xin, You-hao Chen, Fei Wang, Yue Gao, Min Huang, Xue-ding Wang, Li Zhang
Summary: For NSCLC patients with EGFR sensitive mutations, the standard dose of gefitinib may be too high and could potentially be decreased for better efficacy. The metabolite M2 plays a significant role in efficacy and may be more effective in the treatment of metastatic tumors compared to gefitinib.
ACTA PHARMACOLOGICA SINICA
(2022)
Article
Oncology
Chiao-En Wu, Ching-Fu Chang, Chen-Yang Huang, Cheng-Ta Yang, Chih-Hsi Scott Kuo, Ping-Chih Hsu, John Wen-Cheng Chang
Summary: This study reviewed the clinical outcomes and safety of EGFR-TKI treatment in lung adenocarcinoma patients with poor performance status and identified independent prognostic factors. The results showed that patients treated with 40 mg afatinib had better survival outcomes and dose adjustment was an independent prognostic factor for both progression-free survival and overall survival. This study provided evidence and prognostic factors for the use of EGFR-TKIs in patients with poor performance status.
Article
Biophysics
Gamaleldin I. Harisa, Abdelrahman Y. Sherif, Fars K. Alanazi, Essam A. Ali, Gamal A. Omran, Fahd A. Nasr, Sabry M. Attia, Ali S. Alqahtani
Summary: This study aims to develop TPGS decorated nanostructure lipid carrier gefitinib loaded (TPGS-NLC-GEF) for lymphatic drug delivery (LDD) in the prevention and treatment of cancer metastasis. The prepared TPGS-NLC and TPGS-NLC-GEF showed desirable physicochemical properties and biocompatibility. In vitro and in vivo studies demonstrated the enhanced cellular uptake, bioavailability, and tissue distribution of GEF when delivered by TPGS-NLC. This approach holds promise for the treatment of metastatic lung cancer with reduced systemic toxicity.
COLLOIDS AND SURFACES B-BIOINTERFACES
(2023)
Article
Chemistry, Multidisciplinary
Rene J. Boosman, Cornedine J. de Gooijer, Stefanie L. Groenland, Jacobus A. Burgers, Paul Baas, Vincent van der Noort, Jos H. Beijnen, Alwin D. R. Huitema, Neeltje Steeghs
Summary: This study showed that the pharmacokinetic exposure of 75 mg erlotinib combined with ritonavir is similar to 150 mg erlotinib. Ritonavir-boosting is a promising strategy to reduce treatment costs of erlotinib and potentially other expensive therapies metabolized by CYP3A4.
PHARMACEUTICAL RESEARCH
(2022)
Article
Medicine, General & Internal
Ming-Yi Huang, Kun-Pin Hsieh, Ru-Yu Huang, Jen-Yu Hung, Li-Tzong Chen, Ming-Ju Tsai, Yi-Hsin Yang
Summary: This study compared the overall survival and time to next treatment of patients receiving different EGFR TKIs, suggesting that afatinib may provide better effectiveness as the first-line targeted therapy for patients with advanced lung adenocarcinoma harboring EGFR mutation.
JOURNAL OF THE FORMOSAN MEDICAL ASSOCIATION
(2022)
Review
Medicine, General & Internal
Dailong Li, Ling Yao, Lu Xu, Wanqiang Li, Yuan Che
Summary: Icotinib is found to be more effective and safer than gefitinib or erlotinib in treating advanced EGFR mutation-positive NSCLC according to a systematic evaluation.
Article
Pharmacology & Pharmacy
Shaoxing Guan, Xi Chen, Youhao Chen, Guohui Wan, Qibiao Su, Heng Liang, Yunpeng Yang, Wenfeng Fang, Yan Huang, Hongyun Zhao, Wei Zhuang, Shu Liu, Fei Wang, Wei Feng, Xiaoxu Zhang, Min Huang, Xueding Wang, Li Zhang
Summary: This study investigated the effective predictor and alternative treatment for hepatotoxicity induced by gefitinib in non-small cell lung cancer patients using a multi-omics approach. It was found that the rs4946935 AA variant in the FOXO3 gene was associated with a higher risk of hepatotoxicity, particularly at high gefitinib concentrations. Functional experiments revealed that the rs4946935_Lambda variant impaired the expression of FOXO3, leading to an imbalance in autophagy and contributing to gefitinib-induced liver injury. In contrast, liver injury induced by erlotinib was independent of the FOXO3 variant and expression levels. FOXO3 mutation serves as an effective predictor for gefitinib-induced hepatotoxicity, and erlotinib may be a suitable and well-tolerated treatment option for patients carrying the rs4946935 AA variant.
ACTA PHARMACEUTICA SINICA B
(2022)
Article
Oncology
K. Tamura, T. Yoshida, K. Masuda, Y. Matsumoto, Y. Shinno, Y. Okuma, Y. Goto, H. Horinouchi, N. Yamamoto, Y. Ohe
Summary: This retrospective study investigated the activity of EGFR-TKIs in untreated EGFR-mutated NSCLC patients with leptomeningeal metastases (LM). The results showed that osimertinib had better outcomes in LM compared to first-generation TKIs, especially in patients with exon 19 deletion.
