SIDEBAR 6.3Antibody/Peptide Radiopharmaceutical Chemistry Needs

A central issue in the advancement of targeted radionuclide therapy lies in the design and development of labeled antibodies and peptides that target the tumor and spare healthy tissues. Chemistry plays a major role in this process, and the research priorities identified by the committee with input from experts are as follows:

  • To better understand how the chelating agent,a radionuclide, and conjugation method contribute to behavior in vivo;
  • To design radiolabeled ligands with better in vivo properties (faster blood clearance, cleavable linkers for renal clearance);
  • To retain the desired targeting properties of the parent compound after labeling;
  • To develop smaller, less polar,b kinetically stable radiometal ligand complexes that are readily available;
  • To develop processing and purification methods to reliably produce high-specific-activity radionuclides;
  • To synthesize more probes with higher affinity for targeting and capture, and smaller capture agents bearing the radionuclide that attach to the carrier for pre-targeting;
  • To advance radiopharmaceutical applications of the germanium-68/gallium-68 generator to take advantage of the availability of this generator and PET; and
  • To develop methods to produce clinical and commercial quantities of therapeutic radionuclides and to increase the availability of radionuclides approved by the Food and Drug Administration.
a

Chelation is a chemical process whereby a chelating agent binds to a metal ion, forming a metal complex known as a chelate.

b

A chemical compound is made up of one or more chemical bonds between atoms. How the bonds share electrons between the bonds will determine a compound’s polarity. In a polar compound, such as water, there is unequal sharing of the electrons creating a slightly positively charged end and a slightly negatively charged end.

Chelation is a chemical process whereby a chelating agent binds to a metal ion, forming a metal complex known as a chelate.

A chemical compound is made up of one or more chemical bonds between atoms. How the bonds share electrons between the bonds will determine a compound’s polarity. In a polar compound, such as water, there is unequal sharing of the electrons creating a slightly positively charged end and a slightly negatively charged end.

From: 6, Radiotracer and Radiopharmaceutical Chemistry

Cover of Advancing Nuclear Medicine Through Innovation
Advancing Nuclear Medicine Through Innovation.
National Research Council (US) and Institute of Medicine (US) Committee on State of the Science of Nuclear Medicine.
Washington (DC): National Academies Press (US); 2007.
Copyright © 2007, National Academy of Sciences.

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