摘要
抗体-药物偶联剂利用单克隆抗体的抗原特异性选择性地传递高度有效的细胞毒性药物到抗原表达的肿瘤细胞。最近批准的Adcetris™和Kadcyla™以及许多正在进行的临床试验的新数据强调了ADCs对癌症患者可作为一种新的治疗选择。 然而,传统的偶联方法通常会导致抗体-药物偶联剂的异质混合物,这可导致显著的治疗负债,并可能导致复杂的制造过程。从目前的抗体-药物偶联剂和位点特异性生物结合技术的临床调查中所增加的理解,使得科学家能够加速下一代ADCs的发现和开发,定义均相组合物。本稿件综述了新型ADCs的定点共轭方法研究和发展中的最新进展和发展趋势。
关键词: 抗体-药物偶联剂;ADCs;结合位点;DAR;均相抗体-药物偶联剂;位点特异性结合
Current Cancer Drug Targets
Title:Recent Advances in Site Specific Conjugations of Antibody Drug Conjugates (ADCs)
Volume: 16 Issue: 6
Author(s): Wenlong Gao, Jingxin Zhang, Jun Xiang, Lei Zhang, Chengbin Wu, Pradeep K. Dhal, Bo Chen
Affiliation:
关键词: 抗体-药物偶联剂;ADCs;结合位点;DAR;均相抗体-药物偶联剂;位点特异性结合
摘要: Antibody-drug conjugates (ADCs) take the advantage of antigen specificity of monoclonal antibodies to deliver highly potent cytotoxic drugs selectively to antigen-expressing tumor cells. The recent approval of Adcetris™ and Kadcyla™ as well as emerging data from numerous ongoing clinical trials underscore the role of ADCs as a new therapeutic option for cancer patients. However, conventional conjugation methods generally result in a heterogeneous mixture of ADCs, which can result in significant therapeutic liabilities and can lead to complicated manufacturing processes. The increased understanding from the clinical investigation of current ADCs and site-specific bioconjugation technologies has enabled scientists to accelerate the discovery and development of the next generation ADCs with defined and homogeneous composition. The present manuscript reviews the recent advances and trends in the research and development of novel ADCs obtained by site-specific conjugation method.
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Wenlong Gao, Jingxin Zhang, Jun Xiang, Lei Zhang, Chengbin Wu, Pradeep K. Dhal, Bo Chen , Recent Advances in Site Specific Conjugations of Antibody Drug Conjugates (ADCs), Current Cancer Drug Targets 2016; 16 (6) . https://dx.doi.org/10.2174/1568009616666160512144715
DOI https://dx.doi.org/10.2174/1568009616666160512144715 |
Print ISSN 1568-0096 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5576 |
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