Rational Design and Systemic Appraisal of an EGFR-Targeting Antibody-Drug Conjugate LR-DM1 for Pancreatic Cancer

J Med Chem. 2022 May 26;65(10):7141-7153. doi: 10.1021/acs.jmedchem.1c01920. Epub 2022 May 6.

Abstract

By harnessing the payload DM1 and a monoclonal antibody LR004 through a noncleavable linker succinimidyl-4-(N-maleimidomethyl)-cyclohexane-1-carboxylate, we designed and evaluated an antibody-drug conjugate LR-DM1 with an appropriate drug-antibody ratio of 3.6. LR-DM1, which was targeted toward the epidermal growth factor receptor for pancreatic cancer, exhibited potent antiproliferation activity in vitro with a half-maximal inhibitory concentration value of 7.03 nM for Capan-2 cells. Particularly, it displayed prominent tumor growth inhibition in vivo under 20 mg/kg LR-DM1 dosage in a single administration or multiple administrations without apparent abnormality of pathological observation. Moreover, LR-DM1 possessed a relatively broad therapeutic index with a half-lethal dose above 300 mg/kg, which was over 15-fold higher than the highest administration dosage of 20 mg/kg. This initial study on LR-DM1 holds promise for further development of a new antibody drug conjugate that is transformative for treatment of patients concerned.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antibodies, Monoclonal / pharmacology
  • Antibodies, Monoclonal / therapeutic use
  • Breast Neoplasms* / drug therapy
  • Cell Line, Tumor
  • ErbB Receptors / metabolism
  • Female
  • Humans
  • Immunoconjugates* / pharmacology
  • Immunoconjugates* / therapeutic use
  • Maytansine* / pharmacology
  • Maytansine* / therapeutic use
  • Pancreatic Neoplasms* / drug therapy
  • Receptor, ErbB-2
  • Trastuzumab

Substances

  • Antibodies, Monoclonal
  • Immunoconjugates
  • Maytansine
  • EGFR protein, human
  • ErbB Receptors
  • Receptor, ErbB-2
  • Trastuzumab