Gefitinib provides similar effectiveness and improved safety than erlotinib for advanced non-small cell lung cancer

Zhang, Wen‐Xiong; Wei, Yiping; Yu, Dongliang; Xu, Jianjun; Peng, Jinhua

doi:10.1097/md.0000000000010460

Cited by 10 publications

(10 citation statements)

References 65 publications

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“…In line with the PFS data, EGFR exon 19 mutations were also associated with improved OS compared to exon 21 mutations. As for treatment-related data, no significant differences were observed in PFS or OS regarding treatment line and therapeutic agents, which is in line with the findings of others (39)(40)(41)(42).…”

Section: In the Era Of Precision And Individualized Cancer Therapy Prsupporting

confidence: 89%

EGFR variant allele frequency predicts EGFR-TKI efficacy in lung adenocarcinoma: a multicenter study

Gieszer¹,

Dulai²,

Pápay³

et al. 2021

Transl Lung Cancer Res

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Background: Although lung adenocarcinoma (LADC) with sensitizing mutations of the epidermal growth factor receptor (EGFR) is highly sensitive to EGFR tyrosine kinase inhibitors (EGFR-TKIs), in most cases disease progression inevitably occurs. Our aim was to investigate the predictive and prognostic significance of adjusted tumoral EGFR variant allele frequency (EGFR-aVAF) in the above setting.Methods: Eighty-nine Caucasian advanced-stage LADC patients with known exon-specific EGFR mutations undergoing EGFR-TKI treatment were included. The correlations of EGFR-aVAF with clinicopathological variables including progression-free and overall survival (PFS and OS, respectively) were retrospectively analyzed.Results: Of 89 EGFR-mutant LADC patients, 46 (51.7%) had exon 19 deletion, while 41 (46.1%) and 2 (2.2%) patients had exon 21-and exon 18-point mutations, respectively. Tumoral EGFR-aVAF was significantly higher in patients harboring EGFR exon 19 mutations than in those with exon 21-mutant tumors (P<0.001). Notably, patients with EGFR exon 19 mutant tumors demonstrated significantly improved PFS (P=0.003) and OS (P=0.02) compared to patients with exon 21 mutations. Irrespective of specific exon mutations, a statistically significant positive linear correlation was found between EGFR-aVAF of tumoral tissue and PFS (r=0.319; P=0.002). High (≥70%) EGFR-aVAF was an independent predictor of longer PFS [vs. low (<70%) EGFR-aVAF; median PFSs were 52 vs. 26 weeks, respectively; P<0.001]. Additionally, patients with high EGFR-aVAF also had significantly improved OS than those with low EGFR-aVAF (P=0.011).Conclusions: Our study suggests that high (≥70%) EGFR-aVAF of tumoral tissue predicts benefit from Gieszer et al. EGFR-VAF predicts EGFR-TKI efficacy

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Section: In the Era Of Precision And Individualized Cancer Therapy Prsupporting

confidence: 89%

EGFR variant allele frequency predicts EGFR-TKI efficacy in lung adenocarcinoma: a multicenter study

Gieszer¹,

Dulai²,

Pápay³

et al. 2021

Transl Lung Cancer Res

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“…Gefitinib erlotinibe göre daha iyi tolere edilse de akne benzeri döküntüler, bulantı, diyare, anoreksi, stomatit ve dehidratasyon görülebilmektedir. Erlotinib ile deri döküntüsü, bulantı, kusma, yorgunluk ve stomatit bildirilmiştir 15 . Afatinib ve dacomitinib ikinci jenerasyon EGFR-TKİ olup geri dönüşümsüz inhibisyon yapmaktadırlar.…”

Section: Egfr Tirozin Kinaz İnhibitörleriunclassified

Targeted Cancer Therapy: Tyrosine Kinase Inhibitors

Küpeli

2022

Arşiv Kaynak Tarama Dergisi

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Cancers generally contain multiple genetic and epigenetic abnormalities, but several key genes maintain the malignant phenotype and cellular survival. Tyrosine kinases are often involved in the cellular response with growth factors, cytokines, and hormones. These molecules are responsible for tumor growth by various mechanisms. It is thought that tyrosine kinase inhibitors may have a wide range of therapeutic efficacy. Significant response rates could not be obtained in phase 1 studies with any of the agents in monotherapy, and other options are being investigated by administering high doses in short periods and combining drugs that may affect different pathways.

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“…The first generation of EGFR inhibitors, e.g., erlotinib ( Figure 1 : 5) and gefitinib ( Figure 1 : 6), have applications in therapy of patients with non-small cell lung cancer (NSCLC) with EGFR mutations ( Faehling et al, 2018 ; Zhang et al, 2018 ) and have a reversible mechanism of action. The second generation of inhibitors, including afatinib ( Figure 1 : 7), with irreversible inhibitors of mutant EGFR, also express high efficacy against NSCLC ( Sharma and Graziano, 2018 ).…”

Section: Antitumor Effects Of Quinazoline Derivativesmentioning

confidence: 99%

Quinazoline Derivatives as Potential Therapeutic Agents in Urinary Bladder Cancer Therapy

et al. 2021

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Cancer diseases remain major health problems in the world despite significant developments in diagnostic methods and medications. Many of the conventional therapies, however, have limitations due to multidrug resistance or severe side effects. Bladder cancer is a complex disorder, and can be classified according to its diverse genetic backgrounds and clinical features. A very promising direction in bladder cancer treatment is targeted therapy directed at specific molecular pathways. Derivatives of quinazolines constitute a large group of chemicals with a wide range of biological properties, and many quinazoline derivatives are approved for antitumor clinical use, e.g.,: erlotinib, gefitinib, afatinib, lapatinib, and vandetanib. The character of these depends mostly on the properties of the substituents and their presence and position on one of the cyclic compounds. Today, new quinazoline-based compounds are being designed and synthesized as potential drugs of anticancer potency against bladder cancers.

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Gefitinib provides similar effectiveness and improved safety than erlotinib for advanced non-small cell lung cancer

Abstract: Supplemental Digital Content is available in the text

Cited by 10 publications

References 65 publications

EGFR variant allele frequency predicts EGFR-TKI efficacy in lung adenocarcinoma: a multicenter study

EGFR variant allele frequency predicts EGFR-TKI efficacy in lung adenocarcinoma: a multicenter study

Targeted Cancer Therapy: Tyrosine Kinase Inhibitors

Quinazoline Derivatives as Potential Therapeutic Agents in Urinary Bladder Cancer Therapy

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