Genetic alteration of a bispecific ligand-directed toxin targeting human CD19 and CD22 receptors resulting in improved efficacy against systemic B cell malignancy

Leuk Res. 2009 Sep;33(9):1233-42. doi: 10.1016/j.leukres.2009.02.006. Epub 2009 Mar 26.

Abstract

A bispecific ligand-directed toxin (BLT) called DT2219ARL consisting of two scFv ligands recognizing CD19 and CD22 and catalytic DT390 was genetically enhanced for superior in vivo anti-leukemia activity. Genetic alterations included reverse orienting VH-VL domains and adding aggregation reducing/stabilizing linkers. In vivo, these improvements resulted in previously unseen long-term tumor-free survivors measured in a bioluminescent xenograft imaging model in which the progression of human Raji Burkitt's lymphoma could be tracked in real time and in a Daudi model as well. Studies showed DT2219ARL was potent (IC50s 0.06-0.2 nM range) and selectively blockable. Imaging studies indicated the highly invasive nature of this B cell malignancy model and showed it likely induced pre-terminal hind limb paralysis because of metastasis to spinal regions prevented by DT2219ARL. DT2219ARL represents a new class of bispecific biological that can be continually improved by genetic mutation.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Antigens, CD19 / drug effects*
  • Burkitt Lymphoma / pathology*
  • Cell Line, Tumor
  • Drug Delivery Systems
  • Female
  • Flow Cytometry
  • Humans
  • Immunotoxins / pharmacology*
  • Ligands
  • Mice
  • Mice, SCID
  • Sialic Acid Binding Ig-like Lectin 2 / drug effects*

Substances

  • Antigens, CD19
  • Immunotoxins
  • Ligands
  • Sialic Acid Binding Ig-like Lectin 2