A new biotin derivative-DOTA conjugate as a candidate for pretargeted diagnosis and therapy of tumors

J Med Chem. 2003 Jul 3;46(14):3170-3. doi: 10.1021/jm030789z.

Abstract

The synthesis of a new biotin derivative, the (CO) reduced N-aminohexyl biotinamido derivative, designed to be serum biotinidase resistant, and its conjugation to the chelator DOTA through an amide bond at one of the four carboxymethyl chains are described. The (90)Y-labeled conjugate was able to bind avidin at different Av/conjugate molar ratios with good results. The preclinical results indicate that this new biotin-DOTA conjugate is a good candidate for pretargeted diagnosis and therapy of tumors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / chemistry
  • Avidin / chemistry
  • Biotin / analogs & derivatives*
  • Biotin / chemical synthesis*
  • Biotin / chemistry
  • Chelating Agents / chemical synthesis
  • Chelating Agents / chemistry
  • Drug Stability
  • Heterocyclic Compounds, 1-Ring / chemical synthesis*
  • Heterocyclic Compounds, 1-Ring / chemistry
  • Humans
  • Isotope Labeling
  • Neoplasms / diagnosis
  • Protein Binding
  • Radiopharmaceuticals / chemical synthesis*
  • Radiopharmaceuticals / chemistry
  • Yttrium

Substances

  • Antineoplastic Agents
  • Chelating Agents
  • Heterocyclic Compounds, 1-Ring
  • Radiopharmaceuticals
  • Avidin
  • 1,4,7,10-tetraazacyclododecane- 1,4,7,10-tetraacetic acid
  • Yttrium
  • Biotin