Divinylpyrimidine reagents generate antibody-drug conjugates with excellent in vivo efficacy and tolerability

Chem Commun (Camb). 2022 Feb 8;58(12):1962-1965. doi: 10.1039/d1cc06766d.

Abstract

The development of divinylpyrimidine (DVP) reagents for the synthesis of antibody-drug conjugates (ADCs) with in vivo efficacy and tolerability is reported. Detailed structural characterisation of the synthesised ADCs was first conducted followed by in vitro and in vivo evaluation of the ADCs' ability to safely and selectively eradicate target-positive tumours.

MeSH terms

  • Animals
  • Antineoplastic Agents, Immunological / adverse effects
  • Antineoplastic Agents, Immunological / pharmacology*
  • Cell Line, Tumor
  • Humans
  • Immunoconjugates / adverse effects
  • Immunoconjugates / chemistry*
  • Indicators and Reagents / chemistry*
  • Mice
  • Proof of Concept Study
  • Pyrimidines / chemistry*
  • Trastuzumab / adverse effects
  • Trastuzumab / pharmacology
  • Xenograft Model Antitumor Assays

Substances

  • Antineoplastic Agents, Immunological
  • Immunoconjugates
  • Indicators and Reagents
  • Pyrimidines
  • Trastuzumab