Disulfide re-bridging reagents for single-payload antibody-drug conjugates

Chem Commun (Camb). 2023 Aug 10;59(65):9868-9871. doi: 10.1039/d3cc02980h.

Abstract

Numerous antibody-drug conjugate (ADC) linker technologies exist for the synthesis of ADCs with drug-to-antibody ratios (DARs) being an even integer (typically 2, 4 or 8). However, ADCs with odd-integer DARs are significantly harder to synthesise. Here, we report the synthesis of ADCs loaded with a single warhead, using TetraDVP linkers which simultaneously re-bridge all four interchain disulfides of an IgG1 antibody.

MeSH terms

  • Antineoplastic Agents*
  • Disulfides
  • Immunoconjugates*
  • Indicators and Reagents

Substances

  • Immunoconjugates
  • Indicators and Reagents
  • Disulfides
  • Antineoplastic Agents