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雷莫芦单抗:临床前研究与临床开发。

Ramucirumab: preclinical research and clinical development.

机构信息

Department of Oncology, University Hospital of Udine, Udine, Italy.

Lung Cancer Unit, National Cancer Institut "San Martino", Genoa, Italy.

出版信息

Onco Targets Ther. 2014 Oct 29;7:1997-2006. doi: 10.2147/OTT.S61132. eCollection 2014.

Abstract

Ramucirumab (IMC-1121B, LY3009806), a fully humanized monoclonal antibody directed against the extracellular domain of vascular endothelial growth factor receptor 2 (VEGFR-2), is a new therapeutic option that selectively inhibits the human VEGFR-2 with a much greater affinity than its natural ligands. Based on the promising results of both preclinical and early clinical studies, ramucirumab has been tested in different tumor types either alone or in combination with chemotherapy. While it has recently been granted its first US Food and Drug Administration approval for use as a single agent in patients with advanced or metastatic gastric cancer or gastroesophageal junction carcinoma, its role for metastatic breast cancer or advanced non-small-cell lung cancer is still debated. The aims of this review are to recall and discuss the most significant preclinical and clinical studies that led to the development of ramucirumab and to present the results of the randomized clinical trials that have tested its efficacy in different malignancies, including gastric and lung cancer.

摘要

雷莫芦单抗(IMC-1121B,LY3009806)是一种针对血管内皮生长因子受体 2(VEGFR-2)胞外结构域的全人源化单克隆抗体,是一种新型治疗药物,可选择性抑制人 VEGFR-2,亲和力比其天然配体高得多。基于临床前和早期临床研究的良好结果,雷莫芦单抗已在不同的肿瘤类型中进行了单独或联合化疗的测试。尽管最近它已被美国食品和药物管理局首次批准作为晚期或转移性胃癌或胃食管交界处癌患者的单一药物使用,但它在转移性乳腺癌或晚期非小细胞肺癌中的作用仍存在争议。本文旨在回顾和讨论导致雷莫芦单抗开发的最重要的临床前和临床研究,并介绍在不同恶性肿瘤中测试其疗效的随机临床试验结果,包括胃癌和肺癌。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/82b9/4218907/972da14bc91a/ott-7-1997Fig1.jpg

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