trastuzumab-auristatin ADC

Trastuzumab-auristatin ADC refers to a class of antibody-drug conjugates (ADCs) consisting of the humanized anti-HER2 monoclonal antibody trastuzumab conjugated to an auristatin-based cytotoxic payload (such as monomethyl auristatin E [MMAE], monomethyl auristatin F [MMAF], monomethyl auristatin U [MMAU], or Aur0101) via a chemical linker. This platform targets cells expressing human epidermal growth factor receptor 2 (HER2/ERBB2). Upon binding to HER2, the ADC is internalized via receptor-mediated endocytosis, and the auristatin payload is released (either through lysosomal degradation of the antibody or enzymatic cleavage of the linker). The released auristatin binds to tubulin, disrupting microtubule dynamics and inducing cell cycle arrest and apoptosis. Various developers, including Pfizer and Shanghai Miracogen, have investigated trastuzumab-auristatin ADCs (such as PF-06804103 and MRG002) for the treatment of HER2-positive and HER2-low breast, gastric, and other solid tumors.

Other names

trastuzumab-MMAEtrastuzumab-MMAFtrastuzumab-MMAUtrastuzumab-auristatin antibody-drug conjugatetrastuzumab-auristatin conjugatetrastuzumab-vedotin