Afatinib: An overview of its clinical development in non-small-cell lung cancer and other tumors

Giordano, Pasqualina; Manzo, Anna; Montanino, Agnese; Costanzo, Raffaele; Sandomenico, Claudia; Piccirillo, Maria Carmela; Daniele, Gennaro; Normanno, Nicola; Carillio, Guido; Rocco, Gaetano; Bianco, Roberto; Perrone, Francesco; Morabito, Alessandro

doi:10.1016/j.critrevonc.2015.08.016

Cited by 30 publications

(17 citation statements)

References 44 publications

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“…During the last decade, different EGFR tyrosine kinase inhibitors (TKIs) have been developed, and three main inhibitors (gefitinib, erlotinib and afatinib) have been effectively approved for individuals with NSCLC [ 5 ]. Currently, EGFR-TKI treatments are the standard first-line therapies for patients with advanced NSCLCs harboring activating EGFR mutations [ 6 ]. However, these therapeutic agents are ultimately limited by the emergence of secondary EGFR mutations and other molecular mechanisms that confer drug resistance [ 7 , 8 ].…”

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confidence: 99%

Tumor-suppressive miR-218-5p inhibits cancer cell proliferation and migration via EGFR in non-small cell lung cancer

et al. 2016

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Lung cancer remains the leading cause of cancer-related death worldwide, and non-small cell lung cancer (NSCLC) accounts for approximately 80% of lung cancer cases. Recently, microRNAs (miRNAs) have been consistently demonstrated to be involved in NSCLC and to act as either tumor oncogenes or tumor suppressors. In this study, we identified a specific binding site for miR-218-5p in the 3′-untranslated region of the epidermal growth factor receptor (EGFR). We further experimentally validated miR-218-5p as a direct regulator of EGFR. We also identified an inverse correlation between miR-218-5p and EGFR protein levels in NSCLC tissue samples. Moreover, we demonstrated that miR-218-5p plays a critical role in suppressing the proliferation and migration of lung cancer cells probably by binding to EGFR. Finally, we examined the function of miR-218-5p in vivo and revealed that miR-218-5p exerts an anti-tumor effect by negatively regulating EGFR in a xenograft mouse model. Taken together, the results of this study highlight an important role for miR-218-5p in the regulation of EGFR in NSCLC and may open new avenues for future lung cancer therapies.

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Section: Introductionmentioning

confidence: 99%

Tumor-suppressive miR-218-5p inhibits cancer cell proliferation and migration via EGFR in non-small cell lung cancer

et al. 2016

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“…2). In the Lux-Lung-8 study [9, 18], afatinib, an irreversible inhibitor of multiple members of the EGFR family, was superior to erlotinib, with 5% of patients being long-term responders (median overall survival of nearly 2 years). Exploratory analyses are ongoing to better define the molecular characteristics of patients associated to prolonged survival and, to date, a Veristrat-Good serum protein test and the presence of ErbB family mutations have been highlighted as potential biomarkers of long-term response to afatinib [19, 20].…”

Section: Introductionmentioning

confidence: 99%

Second-line treatment for advanced NSCLC without actionable mutations: is immunotherapy the ‘panacea’ for all patients?

Morabito

2018

BMC Med

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The therapeutic approach for the second-line treatment of patients with advanced non-small cell lung cancer (NSCLC) without actionable mutations has been revolutionized by the recent approval of new effective drugs with various mechanisms of action, including nintedanib, ramucirumab, nivolumab, pembrolizumab, atezolizumab, and afatinib. The recent network meta-analysis of Créquit et al. (BMC Medicine, 15:193, 2017) compared the effectiveness and tolerability of the second-line treatments for advanced NSCLC with wild-type or unknown status for EGFR. The authors found that immunotherapy might be more efficacious than the currently recommended treatments. However, their meta-analysis does not take into account the role of predictive biomarkers – this is indeed a crucial point in the decision-making process considering that only a fraction of advanced NSCLC patients might derive a long-term benefit from second-line immunotherapy. The identification of molecular biomarkers that can predict a response to immune checkpoints, angiogenesis, and EGFR inhibitors remains an important goal of clinical research in order to maximize the benefit of these agents and to aid clinicians in the decision-making process.Please see related article: https://bmcmedicine.biomedcentral.com/articles/10.1186/s12916-017-0954-x

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“…Tirozin kinaz inhibitörleri, bu tip kinazların etkinliğini baskılayarak hücrenin büyümesine ve bölünmesine müdahale ederek işlev gösterirler. Akciğer kanseri gibi EGFR (+) kanserlerin engellenmesinde kullanılan Afatinib, kronik miyelositik lösemiye karşı kullanılan Bosutinib, KHDAK'de kullanılan Erlotinib ve Gefinitib gibi ilaçlar, bu tip etkinliğe sahip olan ilaçların sadece bir kısmını oluşturmaktadır [48][49][50] . Hücre büyümesi, çoğalması, protein sentezi ve transkripsiyondan sorumlu bir serin/treonin kinaz olan mTOR (mammalian target of rapamycin)'un baskılanmasının kanserde görülen hücrenin kontrolsüz büyümesi ve çoğalmasının önüne geçebildiği bilinmektedir.…”

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Current Modalities in Treatment of Cancer

Baykara¹

2016

BSBD

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bsbd@balikesir.edu.tr www.bau-sbdergisi.com ÖZET Kanser, hücrelerin kontrolsüz bölünmesi ve çoğalması ile ortaya çıkan ve genetik ve çevresel koşulların etkisi altında olan kompleks bir hastalıktır. Bilinen 100'den fazla kanser türü olmasına ve belli tipteki kanserler için olabildiğince standart yaklaşımlar geliştirilmesine rağmen kanser aynı zamanda kişisel bir hastalıktır. Dünya üzerindeki hiçbir insanın DNA'sı birbirine benzemediği için kişilerin benzer tedavilere farklı cevaplar vermesi şaşırtıcı olmayan bir gerçektir. Teknolojinin ilerlemesi ile birlikte günümüzde var olan tedavilere ek olarak yeni tedavi yöntemleri geliştirilmektedir. Standart olarak kabul edilen kemoterapi, radyoterapi ve cerrahi yöntemlere ek olarak aşılar, biyolojik, hormonal, hedeflenmiş ve gen terapiler giderek artan sayıda kullanılmaya başlanmıştır. Kanser ve tedavisi hakkında bilgi edinmek isteyen bir kişinin karşısına farklı tedaviler, yaklaşımlar, bilimsel makaleler ve hurafelerden oluşan sonsuz bir kaynak denizi ortaya çıkmaktadır. Gerekli bilgiye ulaşmak için uzun ve detaylı araştırmalar yapmak gerekebilir. Bu derlemenin amacı çok basit veya çok karmaşık bilgiler arasında bir köprü oluşturmak, başarı ile uygulanan yöntemleri karşılaştırmak, günümüzde kullanılan tüm metodlar hakkında okuyucuya bilgi vermektir. Anahtar Kelimeler: Kanser tedavisi, gen terapi, radyoterapi, kemoterapi SUMMARYCancer is a complex disease emerging from uncontrolled cell proliferation and division due to various genetic and environmental factors. Even though standard procedures are applied to specific types of cancers, it is also a personal disease with more than 100 types. It is not surprising why every human being responses same to treatments as human DNA is unique. As technology progresses, new therapies including but not limited to biological, hormonal, targeted and gene therapies are developed besides current approaches such as chemotherapy, radiotherapy and surgery. One can easily get lost in a huge ocean of knowledge when he wants to learn about cancer as different types of treatments, approaches, scintific papers and superstitions are widely accesible through internet and it may take a while for the average person to reach the desired information. The aim of this review is to bridge over very simple or very complex information, compare the methods and inform the reader about modalities in cancer.

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Afatinib: An overview of its clinical development in non-small-cell lung cancer and other tumors

Cited by 30 publications

References 44 publications

Tumor-suppressive miR-218-5p inhibits cancer cell proliferation and migration via EGFR in non-small cell lung cancer

Tumor-suppressive miR-218-5p inhibits cancer cell proliferation and migration via EGFR in non-small cell lung cancer

Second-line treatment for advanced NSCLC without actionable mutations: is immunotherapy the ‘panacea’ for all patients?

Current Modalities in Treatment of Cancer

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