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  • Feature Paper
  • Article
  • Open Access
11 Citations
3,106 Views
15 Pages

Dynamic Evaluation of Circulating miRNA Profile in EGFR-Mutated NSCLC Patients Treated with EGFR-TKIs

  • Alessandro Leonetti,
  • Mjriam Capula,
  • Roberta Minari,
  • Giulia Mazzaschi,
  • Alessandro Gregori,
  • Btissame El Hassouni,
  • Filippo Papini,
  • Paola Bordi,
  • Michela Verzè and
  • Elisa Giovannetti
  • + 2 authors

16 June 2021

Background: Resistance to EGFR-TKIs constitutes a major challenge for the management of EGFR-mutated NSCLC, and recent evidence suggests that deregulation of specific microRNAs (miRNAs) may influence resistance to targeted agents. In this retrospecti...

  • Review
  • Open Access
15 Citations
8,977 Views
14 Pages

25 June 2014

In the era of personalized medicine, epidermal growth factor receptor (EGFR) inhibition with tyrosine kinase inhibitor (TKI) has been a mainstay of treatment for non-small cell lung cancer (NSCLC) patients with an EGFR mutation. Acquired resistance,...

  • Article
  • Open Access
5 Citations
3,029 Views
13 Pages

Benefit from Adjuvant TKIs Versus TKIs Plus Chemotherapy in EGFR-Mutant Stage III-pN2 Lung Adenocarcinoma

  • Qiwen Li,
  • Li Ma,
  • Bo Qiu,
  • Yuzhi Wen,
  • Wenhua Liang,
  • Wanming Hu,
  • Naibin Chen,
  • Tian Zhang,
  • Shuangbing Xu and
  • Hui Liu
  • + 10 authors

7 April 2021

Background: Recent studies have demonstrated benefits from adjuvant tyrosine-kinase inhibitors (TKIs) compared with chemotherapy in non-small cell lung cancer. We launched a multi-center retrospective study to evaluate the efficacy and toxicity of ad...

  • Review
  • Open Access
4 Citations
3,111 Views
17 Pages

Making the Best Use of Available Weapons for the Inevitable Rivalry-Resistance to EGFR-TKIs

  • Dongyu Li,
  • Jingnan Wang,
  • Chengming Liu,
  • Yuejun Luo,
  • Haiyan Xu,
  • Yan Wang,
  • Nan Sun and
  • Jie He

The emergence of epidermal growth factor receptor-tyrosine kinase inhibitors (EGFR-TKIs) revolutionized the treatment of advanced-stage non-small cell lung cancer (NSCLC). Detected in more than 50% of late-stage lung adenocarcinoma in Asian patients,...

  • Review
  • Open Access
37 Citations
12,216 Views
25 Pages

Treatment Strategies for Non-Small Cell Lung Cancer with Common EGFR Mutations: A Review of the History of EGFR TKIs Approval and Emerging Data

  • Julian A. Marin-Acevedo,
  • Bruna Pellini,
  • ErinMarie O. Kimbrough,
  • J. Kevin Hicks and
  • Alberto Chiappori

19 January 2023

The development of targeted therapies over the past two decades has led to a dramatic change in the management of EGFR-mutant non-small cell lung cancer (NSCLC). While there are currently five approved EGFR tyrosine kinase inhibitors (TKIs) for treat...

  • Review
  • Open Access
1 Citations
5,392 Views
14 Pages

13 December 2023

The discovery of the efficacy of tyrosine kinase inhibitors (TKIs) in epidermal growth factor receptor (EGFR)-mutated non-small-cell lung cancer (NSCLC) patients has revolutionized lung cancer therapy. Although almost all responders acquire drug resi...

  • Article
  • Open Access
9 Citations
2,905 Views
8 Pages

Prognostic Factors in Lung Adenocarcinoma with Bone Metastasis Treated with EGFR-TKIs

  • Tzu-Hsuan Chiu,
  • Chun-Yu Lin,
  • Meng-Heng Hsieh,
  • Shu-Min Lin and
  • Yueh-Fu Fang

15 September 2021

Background and Objectives: Patients who have advanced lung cancer and bone metastasis (BM) often suffer from skeletal-related events (SREs) that lead to poor quality of life and poor prognosis. Our study aimed to investigate the prognostic factors in...

  • Review
  • Open Access
137 Citations
13,211 Views
8 Pages

Activating mutations of the epidermal growth factor receptor gene (EGFR) are a driving force for some lung adenocarcinomas. Several randomized phase III studies have revealed that treatment with first- or second-generation EGFR tyrosine kinase inhibi...

  • Article
  • Open Access
10 Citations
5,416 Views
17 Pages

Lysine Deprivation Induces AKT-AADAT Signaling and Overcomes EGFR-TKIs Resistance in EGFR-Mutant Non-Small Cell Lung Cancer Cells

  • Chia-Chi Hsu,
  • Albert Ying-Po Yang,
  • Jui-Yi Chen,
  • Hsin-Hui Tsai,
  • Shu-Heng Lin,
  • Pei-Chen Tai,
  • Ming-Hung Huang,
  • Wei-Hsun Hsu,
  • Anya Maan-Yuh Lin and
  • James Chih-Hsin Yang

13 January 2021

Epidermal growth factor receptor (EGFR) mutations are the most common driver genes in non-small cell lung cancer (NSCLC), especially in the Asian population. Although EGFR-tyrosine kinase inhibitors (TKIs) are influential in the treatment of EGFR-mut...

  • Review
  • Open Access
65 Citations
9,195 Views
31 Pages

Resistance to TKIs in EGFR-Mutated Non-Small Cell Lung Cancer: From Mechanisms to New Therapeutic Strategies

  • Andreas Koulouris,
  • Christos Tsagkaris,
  • Anna Chiara Corriero,
  • Giulio Metro and
  • Giannis Mountzios

8 July 2022

Resistance to tyrosine kinase inhibitors (TKIs) of the epidermal growth factor receptor (EGFR) in advanced mutant Non-Small Cell Lung Cancer (NSCLC) constitutes a therapeutic challenge. This review intends to summarize the existing knowledge about th...

  • Communication
  • Open Access
3,181 Views
7 Pages

RANK-C Expression Sensitizes ER-Negative, EGFR-Positive Breast Cancer Cells to EGFR-Tyrosine Kinase Inhibitors (TKIs)

  • Chaido Sirinian,
  • Anastasios D. Papanastasiou,
  • Soren E. Degn,
  • Theodora Frantzi,
  • Christos Aronis,
  • Dimitrios Chaniotis,
  • Thomas Makatsoris,
  • Angelos Koutras and
  • Haralabos P. Kalofonos

23 October 2021

Background: We have previously shown that overexpression of RANK-c in ER-negative breast cancer cell lines attenuates aggressive properties of cancer cells, partially through a RANK-c/EGFR interaction. EGFR inhibition through TKIs in breast cancer ha...

  • Systematic Review
  • Open Access
4 Citations
2,431 Views
17 Pages

Investigating the Efficacy of EGFR-TKIs and Anti-VEGFR Combination in Advanced Non-Small Cell Lung Cancer: A Meta-Analysis

  • Prashant Sakharkar,
  • Sonali Kurup,
  • Subrata Deb,
  • Kaitlin Assaad,
  • Dayna Gesinski and
  • Erysa J. Gayle

18 March 2024

Introduction: The epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs) in combination with anti-vascular endothelial growth factor receptor (VEGFR) agents have shown improved survival outcomes in recent studies. However, its effica...

  • Article
  • Open Access
10 Citations
3,228 Views
16 Pages

26 September 2022

Assessing tumor EGFR mutation status is necessary for the proper management of patients with advanced non–small cell lung cancer (NSCLC). We evaluated the impact of dynamic analyses of the plasma and tissue EGFR mutation using ultra-sensitive d...

  • Article
  • Open Access
20 Citations
4,939 Views
14 Pages

Efficacy of the CDK7 Inhibitor on EMT-Associated Resistance to 3rd Generation EGFR-TKIs in Non-Small Cell Lung Cancer Cell Lines

  • Wonjun Ji,
  • Yun Jung Choi,
  • Myoung-Hee Kang,
  • Ki Jung Sung,
  • Dong Ha Kim,
  • Sangyong Jung,
  • Chang-Min Choi,
  • Jae Cheol Lee and
  • Jin Kyung Rho

3 December 2020

Epithelial to mesenchymal transition (EMT) is associated with resistance during EGFR tyrosine kinase inhibitor (EGFR-TKI) therapy. Here, we investigated whether EMT is associated with acquired resistance to 3rd generation EGFR-TKIs, and we explored t...

  • Article
  • Open Access
3 Citations
3,835 Views
18 Pages

Comparing the Efficacy of Two Generations of EGFR-TKIs: An Integrated Drug–Disease Mechanistic Model Approach in EGFR-Mutated Lung Adenocarcinoma

  • Hippolyte Darré,
  • Perrine Masson,
  • Arnaud Nativel,
  • Laura Villain,
  • Diane Lefaudeux,
  • Claire Couty,
  • Bastien Martin,
  • Evgueni Jacob,
  • Michaël Duruisseaux and
  • Adèle L’Hostis
  • + 2 authors

Mutationsin epidermal growth factor receptor (EGFR) are found in approximately 48% of Asian and 19% of Western patients with lung adenocarcinoma (LUAD), leading to aggressive tumor growth. While tyrosine kinase inhibitors (TKIs) like gefitinib and os...

  • Review
  • Open Access
4 Citations
4,650 Views
25 Pages

11 February 2025

Epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs) have demonstrated remarkable efficacy in treating non-small cell lung cancer (NSCLC), but acquired resistance greatly reduces efficacy and poses a significant challenge to patien...

  • Article
  • Open Access
811 Views
19 Pages

Proteomic Profiling Reveals TPR and FGA as Predictive Serum Biomarkers of Relapse to First- and Second-Generation EGFR-TKIs in Advanced Lung Adenocarcinoma

  • Pritsana Raungrut,
  • Wararat Chiangjong,
  • Thipphanet Masjon,
  • Saowanee Maungchanburi,
  • Thidarat Ruklert and
  • Narongwit Nakwan

Background: Epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs) significantly enhance the median survival of patients with lung adenocarcinoma (ADC) that harbor EGFR-sensitive mutations. However, most patients inevitably experienc...

  • Article
  • Open Access
21 Citations
5,600 Views
11 Pages

FGFR Fusions as an Acquired Resistance Mechanism Following Treatment with Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors (EGFR TKIs) and a Suggested Novel Target in Advanced Non-Small Cell Lung Cancer (aNSCLC)

  • Ari Raphael,
  • Elizabeth Dudnik,
  • Dov Hershkovitz,
  • Suyog Jain,
  • Steve Olsen,
  • Lior Soussan-Gutman,
  • Taly Ben-Shitrit,
  • Addie Dvir,
  • Hovav Nechushtan and
  • on behalf of the Israel Lung Cancer Group
  • + 3 authors

28 April 2022

Background. FGFR1/2/3 fusions have been reported infrequently in aNSCLC, including as a rare, acquired resistance mechanism following treatment with EGFR TKIs. Data regarding their prevalence and therapeutic implications are limited. Methods. The Gua...

  • Review
  • Open Access
22 Citations
5,045 Views
18 Pages

Mechanisms of EGFR-TKI-Induced Apoptosis and Strategies Targeting Apoptosis in EGFR-Mutated Non-Small Cell Lung Cancer

  • Shigetoshi Nishihara,
  • Toshimitsu Yamaoka,
  • Fumihiro Ishikawa,
  • Kensuke Higuchi,
  • Yuki Hasebe,
  • Ryo Manabe,
  • Yasunari Kishino,
  • Sojiro Kusumoto,
  • Koichi Ando and
  • Junji Tsurutani
  • + 4 authors

22 November 2022

Homeostasis is achieved by balancing cell survival and death. In cancer cells, especially those carrying driver mutations, the processes and signals that promote apoptosis are inhibited, facilitating the survival and proliferation of these dysregulat...

  • Article
  • Open Access
11 Citations
2,947 Views
13 Pages

Clinical and Molecular Features of Epidermal Growth Factor Receptor (EGFR) Mutation Positive Non-Small-Cell Lung Cancer (NSCLC) Patients Treated with Tyrosine Kinase Inhibitors (TKIs): Predictive and Prognostic Role of Co-Mutations

  • Paolo Bironzo,
  • Maria Lucia Reale,
  • Tessa Sperone,
  • Fabrizio Tabbò,
  • Andrea Caglio,
  • Angela Listì,
  • Francesco Passiglia,
  • Massimo Di Maio,
  • Luisella Righi and
  • Silvia Novello
  • + 2 authors

17 May 2021

Background: Tyrosine kinase inhibitors (TKIs) show variable efficacy in epidermal growth factor receptor mutation-positive (EGFR+) NSCLC patients, even in patients harbouring the same mutation. Co-alterations may predict different outcomes to TKIs. M...

  • Review
  • Open Access
88 Citations
12,048 Views
18 Pages

Molecular and Clinical Features of EGFR-TKI-Associated Lung Injury

  • Tohru Ohmori,
  • Toshimitsu Yamaoka,
  • Koichi Ando,
  • Sojiro Kusumoto,
  • Yasunari Kishino,
  • Ryou Manabe and
  • Hironori Sagara

The tyrosine kinase activity of epidermal growth factor receptors (EGFRs) plays critical roles in cell proliferation, regeneration, tumorigenesis, and anticancer resistance. Non-small-cell lung cancer patients who responded to EGFR-tyrosine kinase in...

  • Article
  • Open Access
6 Citations
3,829 Views
14 Pages

Effectiveness and Safety of EGFR-TKI Rechallenge Treatment in Elderly Patients with Advanced Non-Small-Cell Lung Cancer Harboring Drug-Sensitive EGFR Mutations

  • Yutaka Yamada,
  • Hisao Imai,
  • Tomohide Sugiyama,
  • Hiroyuki Minemura,
  • Kenya Kanazawa,
  • Takashi Kasai,
  • Koichi Minato,
  • Kyoichi Kaira and
  • Takayuki Kaburagi

3 September 2021

Background and Objectives: Epidermal growth factor receptor–tyrosine kinase inhibitors (EGFR-TKIs) are effective first-line chemotherapeutic agents for patients with advanced non-small-cell lung cancer (NSCLC) harboring drug-sensitive EGFR mutations....

  • Article
  • Open Access
9 Citations
3,815 Views
25 Pages

Real-World Data on Combined EGFR-TKI and Crizotinib Treatment for Acquired and De Novo MET Amplification in Patients with Metastatic EGFR-Mutated NSCLC

  • Edyta M. Urbanska,
  • Morten Grauslund,
  • Peter R. Koffeldt,
  • Sarah L. B. Truelsen,
  • Johan O. Löfgren,
  • Junia C. Costa,
  • Linea C. Melchior,
  • Jens B. Sørensen and
  • Eric Santoni-Rugiu

23 August 2023

Amplification of the mesenchymal epithelial transition (MET) gene is a mechanism of acquired resistance to epidermal growth factor receptor (EGFR)-tyrosine-kinase-inhibitors (TKIs) in over 20% of patients with advanced EGFR-mutated (EGFRm+) non-small...

  • Article
  • Open Access
24 Citations
4,879 Views
14 Pages

The Significance of MMP-1 in EGFR-TKI–Resistant Lung Adenocarcinoma: Potential for Therapeutic Targeting

  • Ryoko Saito,
  • Yasuhiro Miki,
  • Naoya Ishida,
  • Chihiro Inoue,
  • Masayuki Kobayashi,
  • Shuko Hata,
  • Hisafumi Yamada-Okabe,
  • Yoshinori Okada and
  • Hironobu Sasano

18 February 2018

Epidermal growth factor receptor–tyrosine kinase inhibitor (EGFR-TKI) resistance is one of the most important problems in lung cancer therapy. Lung adenocarcinoma with EGFR-TKI resistance was reported to have higher abilities of invasion and migratio...

  • Review
  • Open Access
13 Citations
4,203 Views
17 Pages

Emerging Role of Noncoding RNAs in EGFR TKI-Resistant Lung Cancer

  • Jingwei Li,
  • Peiyi Li,
  • Jun Shao,
  • Shufan Liang,
  • Yuntian Wan,
  • Qiran Zhang,
  • Changshu Li,
  • Yalun Li and
  • Chengdi Wang

12 September 2022

Lung cancer accounts for the majority of malignancy-related mortalities worldwide. The introduction of epidermal growth factor receptor (EGFR)-tyrosine kinase inhibitors (TKIs) has revolutionized the treatment and significantly improved the overall s...

  • Review
  • Open Access
68 Citations
2,710 Views
10 Pages

Management of egfr tki—Induced Dermatologic Adverse Events

  • B. Melosky,
  • N.B. Leighl,
  • J. Rothenstein,
  • R. Sangha,
  • D. Stewart and
  • K. Papp

1 April 2015

Targeting the epidermal growth factor receptor (EGFR) pathway has become standard practice for the treatment of advanced non-small-cell lung cancer. Compared with chemotherapy, EGFR tyrosine kinase inhibitors (TKIS) have been associated with improved...

  • Article
  • Open Access
9 Citations
3,026 Views
10 Pages

Histological Transformation after Acquired Resistance to the Third-Generation EGFR-TKI in Patients with Advanced EGFR-Mutant Lung Adenocarcinoma

  • Po-Hsin Lee,
  • Yen-Hsiang Huang,
  • Ho Lin,
  • Kuo-Hsuan Hsu,
  • Kun-Chieh Chen,
  • Jeng-Sen Tseng,
  • Gee-Chen Chang and
  • Tsung-Ying Yang

Background and Objectives: Third-generation epidermal growth factor receptor (EGFR)-tyrosine kinase inhibitor (TKI) is one of the standard-of-care therapies in patients with EGFR-mutant lung adenocarcinoma; however, acquired resistance inevitably dev...

  • Article
  • Open Access
8 Citations
2,835 Views
11 Pages

14 June 2022

Background: Acquired resistance after EGFR-tyrosine kinase inhibitor (TKI) treatment is the rule rather than the exception. Overcoming resistance to EGFR-TKIs is essential if we are to develop better therapeutic strategies for lung cancer patients. H...

  • Article
  • Open Access
10 Citations
2,995 Views
14 Pages

Objective: Epidermal growth factor receptor–tyrosine kinase inhibitor (EGFR-TKI) is a first-line treatment for lung adenocarcinoma with EGFR-sensitive mutations, but acquired resistance to EGFR-TKIs remains a problem in clinical practice. The d...

  • Article
  • Open Access
33 Citations
5,525 Views
19 Pages

Mediating EGFR-TKI Resistance by VEGF/VEGFR Autocrine Pathway in Non-Small Cell Lung Cancer

  • Chike Osude,
  • Leo Lin,
  • Meet Patel,
  • Adam Eckburg,
  • Joseph Berei,
  • Adijan Kuckovic,
  • Namrata Dube,
  • Aayush Rastogi,
  • Shruti Gautam and
  • Neelu Puri
  • + 2 authors

19 May 2022

NSCLC treatment includes targeting of EGFR with tyrosine kinase inhibitors (TKIs) such as Erlotinib; however, resistance to TKIs is commonly acquired through T790M EGFR mutations or overexpression of vascular endothelial growth factor receptor-2 (VEG...

  • Article
  • Open Access
4 Citations
2,360 Views
14 Pages

EGFR Mutation and TKI Treatment Promote Secretion of Small Extracellular Vesicle PD-L1 and Contribute to Immunosuppression in NSCLC

  • Hai-Ming Liu,
  • Zi-Li Yu,
  • Hou-Fu Xia,
  • Lin-Zhou Zhang,
  • Qiu-Yun Fu,
  • Yi Wang,
  • Hong-Yun Gong and
  • Gang Chen

In Asian populations with non-small-cell lung cancer (NSCLC), EGFR mutations are highly prevalent, occurring in roughly half of these patients. Studies have revealed that individuals with EGFR mutation typically fare worse with immunotherapy. In pati...

  • Systematic Review
  • Open Access
7 Citations
4,619 Views
19 Pages

EGFR-Tyrosine Kinase Inhibitor Retreatment in Non-Small-Cell Lung Cancer Patients Previously Exposed to EGFR-TKI: A Systematic Review and Meta-Analysis

  • Isabella Michelon,
  • Maysa Vilbert,
  • Caio Ernesto do Rego Castro,
  • Carlos Stecca,
  • Maria Inez Dacoregio,
  • Manglio Rizzo,
  • Vladmir Cláudio Cordeiro de Lima and
  • Ludimila Cavalcante

15 July 2024

We performed a systematic review and meta-analysis to assess the efficacy of EGFR-tyrosine kinase inhibitors (TKI) retreatment in advanced/metastatic non-small-cell lung cancer (NSCLC) patients. We systematically searched PubMed, Embase, Cochrane dat...

  • Article
  • Open Access
2 Citations
2,505 Views
13 Pages

15 September 2023

The present study aimed to investigate the influence of the mutation abundance of the epidermal growth factor receptor (EGFR) and its co-mutation with TP53 on the therapeutic efficacy of tyrosine kinase inhibitor (TKI) treatment in patients with meta...

  • Article
  • Open Access
342 Views
20 Pages

Leveraging Acquired EGFR-TKI-Resistant Models to Identify MUC16 as a Therapeutic Vulnerability in Lung Adenocarcinoma

  • Yinhua Tan,
  • Chunxiu Xiao,
  • Zhifan Wang,
  • Yuhang Kong,
  • Yamei Huang,
  • Zhichang Liu,
  • Qiang Wu,
  • Chenyu Wu,
  • Manyu Zhao and
  • Kai Xiao
  • + 1 author

25 December 2025

Background/Objectives: Acquired resistance to epidermal growth factor receptor (EGFR)-tyrosine kinase inhibitors (TKIs) remains a major challenge in the treatment of EGFR-mutant lung adenocarcinoma (LUAD). This study aimed to develop and characterize...

  • Article
  • Open Access
25 Citations
3,237 Views
17 Pages

Resistance to epidermal growth factor receptor tyrosine kinase inhibitors (EGFR TKIs) is a major obstacle in managing lung cancer. The root of Scutellaria baicalensis (SB) traditionally used for fever clearance and detoxification possesses various bi...

  • Review
  • Open Access
7 Citations
4,999 Views
22 Pages

The Role of Proteomics and Phosphoproteomics in the Discovery of Therapeutic Targets and Biomarkers in Acquired EGFR-TKI-Resistant Non-Small Cell Lung Cancer

  • Sutpirat Moonmuang,
  • Apichat Tantraworasin,
  • Santhasiri Orrapin,
  • Sasimol Udomruk,
  • Busyamas Chewaskulyong,
  • Dumnoensun Pruksakorn and
  • Parunya Chaiyawat

The discovery of potent EGFR-tyrosine kinase inhibitors (EGFR-TKIs) has revolutionized the treatment of EGFR-mutated lung cancer. Despite the fact that EGFR-TKIs have yielded several significant benefits for lung cancer patients, the emergence of res...

  • Case Report
  • Open Access
4 Citations
6,409 Views
7 Pages

EGFR Targeting TKI-Related Skin Toxicities in a Patient with Darker Skin: A Case Report

  • Arman Zereshkian,
  • Alia Thawer,
  • David M. Hwang and
  • Susanna Cheng

5 April 2022

Epidermal growth factor receptor (EGFR) targeting tyrosine kinase inhibitors (TKIs) can result in significant skin toxicities that may impact patients’ quality of life. While these skin reactions are well documented in patients with lighter ski...

  • Article
  • Open Access
9 Citations
4,042 Views
16 Pages

Elevating CDCA3 Levels Enhances Tyrosine Kinase Inhibitor Sensitivity in TKI-Resistant EGFR Mutant Non-Small-Cell Lung Cancer

  • Katherine B. Sahin,
  • Esha T. Shah,
  • Genevieve P. Ferguson,
  • Christopher Molloy,
  • Priyakshi Kalita-de Croft,
  • Sarah A. Hayes,
  • Amanda Hudson,
  • Emily Colvin,
  • Hannah Kamitakahara and
  • Mark N. Adams
  • + 11 authors

16 September 2021

Tyrosine kinase inhibitors (TKIs) are the first-line therapy for non-small-cell lung cancers (NSCLC) that harbour sensitising mutations within the epidermal growth factor receptor (EGFR). However, resistance remains a key issue, with tumour relapse l...

  • Article
  • Open Access
2 Citations
2,737 Views
11 Pages

The Presence of EGFR T790M in TKI-Naïve Lung Cancer Samples of Patients Who Developed a T790M-Positive Relapse on First or Second Generation TKI Is Rare

  • Weiting Li,
  • Klaas Kok,
  • Geok Wee Tan,
  • Pei Meng,
  • Mirjam Mastik,
  • Naomi Rifaela,
  • Frank Scherpen,
  • T. Jeroen N. Hiltermann,
  • Harry J. M. Groen and
  • Anke van den Berg
  • + 1 author

19 July 2022

EGFR-mutated non-small cell lung cancer (NSCLC) patients can be effectively treated with tyrosine kinase inhibitors (TKI) but frequently present with an EGFR T790M resistance mutation at relapse. We aimed to screen for T790M in pre-treatment formalin...

  • Article
  • Open Access
30 Citations
5,463 Views
24 Pages

Blocking Aerobic Glycolysis by Targeting Pyruvate Dehydrogenase Kinase in Combination with EGFR TKI and Ionizing Radiation Increases Therapeutic Effect in Non-Small Cell Lung Cancer Cells

  • Sissel E. Dyrstad,
  • Maria L. Lotsberg,
  • Tuan Zea Tan,
  • Ina K. N. Pettersen,
  • Silje Hjellbrekke,
  • Deusdedit Tusubira,
  • Agnete S. T. Engelsen,
  • Thomas Daubon,
  • Arnaud Mourier and
  • Gro V. Røsland
  • + 4 authors

24 February 2021

Increased glycolytic activity is a hallmark of cancer initiation and progression and is often observed in non-small cell lung cancer (NSCLC). Pyruvate dehydrogenase (PDH) complex acts as a gatekeeper between glycolysis and oxidative phosphorylation,...

  • Article
  • Open Access
16 Citations
4,752 Views
16 Pages

30 June 2022

Integrin β3 plays a key role in the resistance to epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKI), but the development of integrin β3 inhibitors has been stalled due to the failure of phase III clinical trials for can...

  • Article
  • Open Access
19 Citations
4,753 Views
16 Pages

31 December 2020

Oncogenic mutations of epidermal growth factor receptor (EGFR) are responsive to targeted tyrosine kinase inhibitor (TKI) treatment in non-small-cell lung cancer (NSCLC). However, NSCLC patients harboring activating EGFR mutations inevitably develop...

  • Systematic Review
  • Open Access
12 Citations
4,651 Views
12 Pages

Drug resistance is a common barrier to continued effective treatment in cancer. In non-small-cell lung cancer (NSCLC), tyrosine kinase inhibitors that target the epidermal growth factor receptor (EGFR-TKIs) exhibit good efficacy in cancer treatment u...

  • Article
  • Open Access
12 Citations
4,751 Views
17 Pages

Physiologically Based Pharmacokinetic (PBPK) Modeling to Predict PET Image Quality of Three Generations EGFR TKI in Advanced-Stage NSCLC Patients

  • I. H. Bartelink,
  • E. A. van de Stadt,
  • A. F. Leeuwerik,
  • V. L. J. L. Thijssen,
  • J. R. I. Hupsel,
  • J. F. van den Nieuwendijk,
  • I. Bahce,
  • M. Yaqub and
  • N. H. Hendrikse

Introduction: Epidermal growth factor receptor (EGFR) mutated NSCLC is best treated using an EGFR tyrosine kinase inhibitor (TKI). The presence and accessibility of EGFR overexpression and mutation in NSCLC can be determined using radiolabeled EGFR T...

  • Review
  • Open Access
336 Views
21 Pages

Lineage Plasticity and Histologic Transformation in EGFR-TKI Resistant Lung Cancer

  • Li Yieng Eunice Lau,
  • Anders Jacobsen Skanderup and
  • Aaron C. Tan

31 December 2025

Lineage plasticity, the ability of cancer cells to alter their differentiated state through transcriptional and epigenetic reprogramming, has emerged as a key mechanism of therapeutic resistance across cancers. This adaptive process can manifest in m...

  • Article
  • Open Access
28 Citations
5,576 Views
19 Pages

Downregulation of miR-506-3p Facilitates EGFR-TKI Resistance through Induction of Sonic Hedgehog Signaling in Non-Small-Cell Lung Cancer Cell Lines

  • Inamul Haque,
  • Hameem I. Kawsar,
  • Hannah Motes,
  • Mukut Sharma,
  • Snigdha Banerjee,
  • Sushanta K. Banerjee,
  • Andrew K. Godwin and
  • Chao H. Huang

6 December 2020

Non-small-cell lung cancer (NSCLC) patients with epidermal growth factor receptor (EGFR) mutation eventually develop resistance to EGFR-targeted tyrosine kinase inhibitors (TKIs). Treatment resistance remains the primary obstacle to the successful tr...

  • Article
  • Open Access
8 Citations
3,558 Views
13 Pages

12 July 2019

The emergence of epidermal growth factor receptor-tyrosine kinase inhibitor (EGFR-TKI) caused a paradigm shift in the treatment of non-small cell lung cancer (NSCLC). Although several clinicopathologic factors to predict the response to and survival...

  • Article
  • Open Access
1,059 Views
19 Pages

Integrating Clinical and Imaging Markers for Survival Prediction in Advanced NSCLC Treated with EGFR-TKIs

  • Thanika Ketpueak,
  • Phumiphat Losuriya,
  • Thanat Kanthawang,
  • Pakorn Prakaikietikul,
  • Lalita Lumkul,
  • Phichayut Phinyo and
  • Pattraporn Tajarernmuang

3 August 2025

Background: Epidermal growth factor receptor (EGFR) mutations are presented in approximately 50% of East Asian populations with advanced non-small cell lung cancer (NSCLC). While EGFR-tyrosine kinase inhibitors (TKIs) are the standard treatment, pati...

  • Article
  • Open Access
16 Citations
4,262 Views
14 Pages

Detection of EGFR Mutations in Plasma Cell-Free Tumor DNA of TKI-Treated Advanced-NSCLC Patients by Three Methodologies: Scorpion-ARMS, PNAClamp, and Digital PCR

  • Annamaria Siggillino,
  • Paola Ulivi,
  • Luigi Pasini,
  • Maria Sole Reda,
  • Elisa Chiadini,
  • Francesca Romana Tofanetti,
  • Sara Baglivo,
  • Giulio Metro,
  • Lucio Crinó and
  • Vienna Ludovini
  • + 3 authors

7 December 2020

Analysis of circulating cell-free tumor DNA (cftDNA) has emerged as a specific and sensitive blood-based approach to detect epidermal growth factor receptor (EGFR) mutations in non-small cell lung cancer (NSCLC) patients. Still, there is some debate...

  • Review
  • Open Access
38 Citations
6,821 Views
33 Pages

The Resistance to EGFR-TKIs in Non-Small Cell Lung Cancer: From Molecular Mechanisms to Clinical Application of New Therapeutic Strategies

  • Carmelo Laface,
  • Felicia Maria Maselli,
  • Anna Natalizia Santoro,
  • Maria Laura Iaia,
  • Francesca Ambrogio,
  • Marigia Laterza,
  • Chiara Guarini,
  • Pierluigi De Santis,
  • Martina Perrone and
  • Palma Fedele

Almost 17% of Western patients affected by non-small cell lung cancer (NSCLC) have an activating epidermal growth factor receptor (EGFR) gene mutation. Del19 and L858R are the most-common ones; they are positive predictive factors for EGFR tyrosine k...

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