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Site-specific conjugation improves therapeutic index of antibody drug conjugates with high drug loading

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Figure 1: Efficacy and pharmacokinetics of ADCs with different loading.
Figure 2: Clustering of hydrophobic payloads on higher-loaded ADCs and their corresponding pharmacokinetics in rat.

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Acknowledgements

We thank D. McDonough and C. Samain for their help with PK experiments, G. Bolton for technical assistance and T. Kuo and O.-K. Wong for reading the manuscript.

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Author notes

  1. Pavel Strop, Kathy Delaria and Davide Foletti: These authors contributed equally to this work.

Authors and Affiliations

  1. Rinat Laboratories, Pfizer Inc., South San Francisco, California, USA

    Pavel Strop, Kathy Delaria, Davide Foletti, Jody Melton Witt, Adela Hasa-Moreno, Kris Poulsen, Meritxell Galindo Casas, Magdalena Dorywalska, Santiago Farias, Ariel Pios, Victor Lui, Thomas-Toan Tran, Janette Sutton, Kevin C Lindquist, Shu-Hui Liu, David L Shelton, Jaume Pons & Arvind Rajpal

  2. Worldwide Medicinal Chemistry, Pfizer Inc., Groton, Connecticut, USA

    Russell Dushin, Dahui Zhou & Thayalan Navaratnam

  3. Drug Safety Research and Development, Pfizer Inc., San Diego, California, USA

    Bora Han

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  1. Pavel Strop
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  2. Kathy Delaria
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  19. Shu-Hui Liu
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Corresponding authors

Correspondence to Pavel Strop or Arvind Rajpal.

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Competing interests

All authors are employees of Pfizer, Inc.

Supplementary information

Supplementary Text and Figures

Supplementary Figures 1–8, and Supplementary Tables 1–3, and Supplemental Experimental Procedures (PDF 5728 kb)

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Strop, P., Delaria, K., Foletti, D. et al. Site-specific conjugation improves therapeutic index of antibody drug conjugates with high drug loading. Nat Biotechnol 33, 694–696 (2015). https://doi.org/10.1038/nbt.3274

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