A Chemical Technology to Generate Homogeneous Antibody-Drug-Conjugates (ADCs) and Bispecifics

生成均质抗体药物偶联物 (ADC) 和双特异性药物的化学技术

• 批准号: BB/L024349/1
• 负责人: James Baker
• 金额: $ 61.17万
• 依托单位: University College London
• 依托单位国家: 英国
• 项目类别: Research Grant
• 财政年份: 2014
• 资助国家: 英国
• 起止时间: 2014 至 无数据
• 项目状态: 已结题
• 来源: https://gtr.ukri.org/projects?ref=BB%2FL024349%2F1
• 关键词: Chemical; Technology; Generate; Homogeneous; Antibody

Using antibodies as therapeutics and diagnostics is one of the most promising areas of research into new healthcare products. Antibodies represent the fastest growing class of therapeutics, with over 20 approved for clinical use to date and over 150 in clinical development. It is estimated that the global market for antibody therapeutics is currently around $50 billion. Two particularly promising classes of antibody based therapeutics are antibody-drug-conjugates (ADCs) and bispecifics, commonly referred to as 'magic-bullet' therapies due to their ability to seek and destroy just diseased cells within the body (e.g. cancer cells). However, a major hindrance to the area is the lack of suitable chemical methods for the construction of homogeneous, well defined, antibody conjugates. Here we propose to exemplify a powerful new chemical technology that we have developed to overcome these limitations, to enable the design of superior next generation ADCs and bispecifics.

使用抗体作为治疗和诊断是研究新的医疗保健产品最有前途的领域之一。抗体是增长最快的一类治疗药物，迄今为止已有超过20种药物获批用于临床，超过150种药物正在临床开发中。据估计，全球抗体治疗市场目前约为500亿美元。基于抗体的治疗剂的两个特别有前途的类别是抗体-药物-缀合物（ADC）和双特异性，由于其仅寻找和破坏体内患病细胞（例如癌细胞）的能力，通常被称为“魔术子弹”疗法。然而，该领域的一个主要障碍是缺乏合适的化学方法来构建均匀的、明确定义的抗体缀合物。在这里，我们提出了一个强大的新的化学技术，我们已经开发克服这些限制，使设计的上级下一代ADC和双特异性。

项目成果

A platform for efficient, thiol-stable conjugation to albumin's native single accessible cysteine.

与白蛋白的原生单一可访问半胱氨酸的高效，硫代结合的平台。

• DOI: 10.1039/c5ob01205h
• 发表时间: 2015-08-07
• 期刊: Organic & biomolecular chemistry
• 影响因子: 3.2
• 作者: Smith ME;Caspersen MB;Robinson E;Morais M;Maruani A;Nunes JP;Nicholls K;Saxton MJ;Caddick S;Baker JR;Chudasama V
• 通讯作者: Chudasama V

Pyridazinediones deliver potent, stable, targeted and efficacious antibody-drug conjugates (ADCs) with a controlled loading of 4 drugs per antibody

• DOI: 10.1039/c7ra00788d
• 发表时间: 2017-01-01
• 期刊: RSC ADVANCES
• 影响因子: 3.9
• 作者: Robinson, Eifion;Nunes, Joao P. M.;Chudasama, Vijay
• 通讯作者: Chudasama, Vijay