Monomethyl auristatin E (MMAE) is a synthetic antineoplastic agent. Because of its toxicity, it cannot be used as a drug itself; instead, it is linked to a monoclonal antibody (MAB) which directs it to the cancer cells.

2023年11月9日 · 抗体药物偶联物（antibody-drug conjugate，ADC）是一类用于治疗癌症的新兴靶向疗法，旨在将小分子化疗直接递送并杀伤肿瘤细胞，同时保留健康细胞。 自2000年MYLOTARG成功获批以来，抗体药物偶联物（ADC）已成为癌…

2023年11月3日 · MMAE作为有效载荷在ADC药物的开发中很普遍，已在14个批准的ADC中有5个使用了MMAE（表1）。 在识别和结合表达在癌细胞表面的靶抗原后，ADC通过 内吞作用 内化，然后通过蛋白降解/酸性裂解释放有效载荷，以实现准确的杀伤。 通过与 微管蛋白 的相互作用，MMAE抑制微管的形成，破坏有丝分裂纺锤体的组装，导致肿瘤细胞停滞在细胞周期的M期。 基于MMAE的ADC在改善各种癌症的整体治疗结果方面显示出显著的效果。 表1. 全球批准上市 …

2022年7月5日 · Monomethyl auristatin (MMAE) is the most common ADC warhead conjugated to an expanding array of antibodies in clinical development for oncologic applications. In...

2021年6月10日 · We also demonstrate that a homogeneous anti-HER2 ADC containing both MMAE and MMAF exerts remarkable therapeutic effect in two mouse models of refractory breast cancer with heterogeneous HER2...

2023年11月3日 · 缔码生物开发了适合ADC ELISA 测定开发的anti-MMAE抗体，它可用于定量测定测试样品中anti-MMAE-缀合物的水平， 可用于PK检测以及DAR值分析，加速ADC药物的研发进程。

Background: Monomethyl auristatin E (MMAE) has been used as a payload for several Food and Drug Administration (FDA) approved antibody-drug conjugates (ADCs). It is known that MMAE is released from the ADC following binding, internalisation and proteolytic degradation in …

Antibody–drug conjugates (ADCs) are a novel class of therapeutic agents consisting of a monoclonal antibody (mAb) covalently bound with a cytotoxic drug through a chemical linker. The mAb preferentially targets cell surface antigens overexpressed in tumor cells.

2022年11月3日 · Among the 15 marketed ADC drugs, there are six ADC drugs with payloads of MMAE or MMAF, including Adcetris, Polivy, Padcev, Blenrep, Tivdak, and Aidixi (RC48). Notably, at the beginning of 2022, the FDA granted breakthrough therapy designation to the novel ADC telisotuzumab vedotin based on the excellent data from its phase 2 LUMINOSITY study.

2025年2月5日 · Monomethyl auristatin E (MMAE) is a key payload in these ADCs due to its ability to disrupt microtubules and induce cell cycle arrest, making it an effective anti-cancer agent. Understanding MMAE’s chemistry, mechanism of action, and clinical insights is crucial for advancing ADC development.