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ZD1839(“易瑞沙”)作为一种抗癌药物。

ZD1839 ('Iressa') as an anticancer agent.

作者信息

Baselga J, Averbuch S D

机构信息

Medical Oncology Service, Vail d'Hebron University Hospital, Barcelona, Spain.

出版信息

Drugs. 2000;60 Suppl 1:33-40; discussion 41-2. doi: 10.2165/00003495-200060001-00004.

Abstract

ZD1839 ('Iressa') is an orally active, selective epidermal growth factor receptor-tyrosine kinase inhibitor which blocks signal transduction pathways implicated in the proliferation and survival of cancer cells and other host-dependent processes promoting cancer growth. In preclinical studies, ZD1839 produced reversible growth inhibition and growth delay in a wide range of tumour cell lines and human tumour xenografts. Moreover, this activity was enhanced when ZD1839 was coadministered with cytotoxic agents. Preliminary results from phase I trials in patients with advanced disease and a wide variety of tumour types suggest that ZD1839 has an acceptable tolerability profile and promising clinical efficacy, particularly in non-small cell lung cancer (NSCLC). ZD1839 is currently in phase III clinical development for the treatment of advanced NSCLC. In addition, further trials are ongoing or planned in a number of other tumour types.

摘要

ZD1839(“易瑞沙”)是一种口服活性、选择性表皮生长因子受体酪氨酸激酶抑制剂,它可阻断与癌细胞增殖和存活以及促进癌症生长的其他宿主依赖性过程相关的信号转导途径。在临床前研究中,ZD1839在多种肿瘤细胞系和人肿瘤异种移植模型中产生了可逆的生长抑制和生长延迟。此外,当ZD1839与细胞毒性药物联合使用时,这种活性会增强。对患有晚期疾病和多种肿瘤类型的患者进行的I期试验的初步结果表明,ZD1839具有可接受的耐受性和有前景的临床疗效,尤其是在非小细胞肺癌(NSCLC)中。ZD1839目前正处于治疗晚期NSCLC的III期临床开发阶段。此外,针对其他多种肿瘤类型的进一步试验正在进行或计划中。

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