MI130004, a Novel Antibody–Drug Conjugate Combining Trastuzumab with a Molecule of Marine Origin, Shows Outstanding In Vivo Activity against HER2-Expressing Tumors

@article{Avils2018MI130004AN,
  title={MI130004, a Novel Antibody–Drug Conjugate Combining Trastuzumab with a Molecule of Marine Origin, Shows Outstanding In Vivo Activity against HER2-Expressing Tumors},
  author={P. Avil{\'e}s and J. Domínguez and M. Guill{\'e}n and M. Mu{\~n}oz-Alonso and C. Mateo and R. Rodr{\'i}guez-Acebes and J. M. Molina-Guijarro and A. Francesch and J. F. Mart{\'i}nez-Leal and S. Munt and C. Galmarini and C. Cuevas},
  journal={Molecular Cancer Therapeutics},
  year={2018},
  volume={17},
  pages={786 - 794}
}
In the search for novel payloads to design new antibody–drug conjugates (ADC), marine compounds represent an interesting opportunity given their unique chemical features. PM050489 is a marine compound that binds β-tubulin at a new site and disrupts the microtubule network, hence leading to mitotic aberrations and cell death. PM050489 has been conjugated to trastuzumab via Cys residues through a noncleavable linker, and the resulting ADC, named MI130004, has been studied. Analysis of MI130004… Expand
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