A Mini-Review on EGFR-Tyrosine Kinase Inhibitors and their Resistance Mechanisms.

IF 2.6 4区 医学 Q2 PHARMACOLOGY & PHARMACY Current pharmaceutical design Pub Date : 2025-03-11 DOI:10.2174/0113816128349342250121053445
Mohd Javed Naim, Abdul Samad
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Abstract

Background: An essential component of cell development, proliferation, and survival is the transmembrane receptor known as the epidermal growth factor receptor (EGFR). Dysregulated EGFR signalling is an appealing pathway that has been linked to the genesis and progression of several cancer types. EGFR tyrosine kinase inhibitors (TKIs) are targeted drugs that show promise in the fight against cancer. EGFR tyrosine kinase inhibitors obstruct cancer growth and survival signalling pathways by blocking the receptor's tyrosine kinase domain. Patients with non-small cell lung cancer (NSCLC) that have EGFR mutations have shown increased progression-free survival and overall survival rates when treated with EGFR TKIs as compared to conventional chemotherapy, according to many clinical studies.

Objectives: This review is aimed to present the journey of EGFR-tyrosine kinase inhibitors, their signalling cascade, and various resistant mechanisms.

Methods: The literature search was carried out on electronic databases like PubMed, Medline, etc., by employing search keywords, such as EGFR, EGFR inhibitors, cancer, tyrosine kinase, etc., and data on EGFR signaling pathways and the types of potential inhibitors in a hierarchical manner, followed by various resistance mechanisms that have emerged, were collected.

Results: Drug resistance is still an issue in long-term therapy of patients, even though EGFR TKIs provide substantial therapeutic advantages. Common routes of resistance to EGFR TKIs include acquired resistance mechanisms, which include the development of secondary EGFR mutations and the activation of alternative signalling pathways. To improve the therapeutic effectiveness of EGFR TKIs, future research will center on searching indicators of response and resistance, finding ways to employ these medicines most effectively, and creating new treatment approaches.

Conclusion: This review provides insight into the use of EGFR kinase inhibitors for treating cancer patients and outlines potential advancements in current therapies to develop more effective molecules.

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表皮生长因子受体-酪氨酸激酶抑制剂及其耐药机制微型综述。
背景:表皮生长因子受体(EGFR)是细胞发育、增殖和存活的重要组成部分。表皮生长因子受体信号失调是一种具有吸引力的途径,与多种癌症类型的发生和发展有关。表皮生长因子受体酪氨酸激酶抑制剂(TKIs)是抗癌前景看好的靶向药物。表皮生长因子受体酪氨酸激酶抑制剂通过阻断受体的酪氨酸激酶结构域,阻碍癌症生长和生存信号通路。许多临床研究表明,与传统化疗相比,表皮生长因子受体酪氨酸激酶抑制剂可提高有表皮生长因子受体突变的非小细胞肺癌(NSCLC)患者的无进展生存期和总生存率:本综述旨在介绍表皮生长因子受体酪氨酸激酶抑制剂的发展历程、其信号级联以及各种耐药机制:方法:在PubMed、Medline等电子数据库中进行文献检索,采用表皮生长因子受体、表皮生长因子受体抑制剂、癌症、酪氨酸激酶等检索关键词,分层次收集表皮生长因子受体信号通路和潜在抑制剂类型的数据,然后收集已出现的各种耐药机制:结果:尽管表皮生长因子受体 TKIs 具有很大的治疗优势,但耐药性仍然是患者长期治疗中的一个问题。表皮生长因子受体 TKIs 常见的耐药途径包括获得性耐药机制,其中包括发生二次表皮生长因子受体突变和激活替代信号通路。为了提高表皮生长因子受体 TKIs 的治疗效果,未来的研究将集中在寻找反应和耐药性指标、找到最有效地使用这些药物的方法以及创造新的治疗方法:本综述深入探讨了表皮生长因子受体激酶抑制剂在治疗癌症患者中的应用,并概述了当前疗法的潜在进展,以开发更有效的分子。
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来源期刊
CiteScore
6.30
自引率
0.00%
发文量
302
审稿时长
2 months
期刊介绍: Current Pharmaceutical Design publishes timely in-depth reviews and research articles from leading pharmaceutical researchers in the field, covering all aspects of current research in rational drug design. Each issue is devoted to a single major therapeutic area guest edited by an acknowledged authority in the field. Each thematic issue of Current Pharmaceutical Design covers all subject areas of major importance to modern drug design including: medicinal chemistry, pharmacology, drug targets and disease mechanism.
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