贝伐单抗:开发,药理学和应用于脑肿瘤的综述

H. Newton
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引用次数: 5

摘要

贝伐单抗是一种针对血管内皮生长因子(VEGF)的人源化单克隆抗体。VEGF是VEGF受体(VEGFR)的配体,对包括恶性胶质瘤在内的高级别实体瘤的血管生成表型的发展和维持至关重要。血管生成,VEGF, VEGFR和贝伐单抗药理学的概述将被提出。贝伐单抗在神经胶质瘤组织培养和异种移植物模型的临床前测试中很活跃。在临床中,与伊立替康和其他化疗药物联合使用,在多形性胶质母细胞瘤(GBM)和其他脑肿瘤患者中显示出显著的活性。在30%-60%的报告病例中注意到神经影像学的客观反应。许多报告也建议延长无进展生存期和总生存期。贝伐单抗的治疗与潜在的副作用相关,包括血栓栓塞性疾病、疲劳、颅内出血、蛋白尿、高血压和肠穿孔。
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Bevacizumab: Review of Development, Pharmacology, and Application to Brain Tumors
Bevacizumab is a humanised monoclonal antibody targeted to the vascular endothelial growth factor (VEGF). VEGF is the ligand for VEGF receptors (VEGFR), which are important for the development and maintenance of the angiogenic phenotype in high-grade solid tumors, including malignant gliomas. An overview of angiogenesis, VEGF, VEGFR, and the pharmacology of bevacizumab will be presented. Bevacizumab is active in pre-clinical testing against glioma tissue cultures and xenograft models. In the clinical setting, in combination with irinotecan and other chemotherapy agents, it has shown significant activity in patients with glioblastoma multiforme (GBM) and other brain tumors. Objective responses on neuro-imaging have been noted in 30%–60% of reported cases. Prolongation of progression-free survival and overall survival have also been suggested in many reports. Treatment of bevacizumab is associated with potential side effects, including thromboembolic disorders, fatigue, intracranial hemorrhage, proteinuria, hypertension, and bowel perforation.
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