Labeling of monoclonal antibodies with radionuclides

Journal Article · Sat Jul 01 00:00:00 EDT 1989 · Seminars in Nuclear Medicine; (USA)

DOI:https://doi.org/10.1016/S0001-2998(89)80013-3· OSTI ID:5226494

Bhargava, K K; Acharya, S A ^[1]

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1. Albert Einstein College of Medicine-Montefiore Medical Center, Bronx, NY (USA)

Antibodies, specifically monoclonal antibodies, are potentially very useful and powerful carriers of therapeutic agents to target tissues and diagnostic agents. The loading or charging of antibodies with agents, especially radiotracers, is reviewed here. The choice of radioisotope for immunodetection and/or immunotherapy is based on its availability, half-life, nature of the radiation emitted, and the metabolic pathways of the radionuclide in the body. Most important of all are the derivatization techniques available for labeling the antibody with the given radionuclide. Isotopes of iodine and divalent metal ions are the most commonly used radionuclides. Antibodies labeled with iodine at tyrosine residues are metabolized rapidly in vivo. This leads to the incorporation of metabolized radioactive iodine into various tissues, mainly the thyroid gland and stomach, and to the accumulation of high levels of circulating iodine in the blood, which masks tumor uptake considerably. To overcome these limitations, the use of iodohippurate as an iodine-anchoring molecule to the protein should be considered. When divalent or multivalent metal ions are used as the preferred radionuclide, bifunctional chelating reagents such as EDTA or DTPA are first coupled to the protein or antibody. These chelating molecules are attached to the protein by formation of an isopeptide linkage between the carboxylate of the chelating reagent and the amino group of the protein. Several procedures are available to generate the isopeptide linkage. When the anchoring of the chelating agent through isopeptide linkage results in the inactivation of the antibody, periodate oxidation of the carbohydrate moiety of the antibody, followed by reductive coupling of chelator, could be considered as an alternative. There is still a need for better, simpler, and more direct methods for labeling antibodies with radionuclides. 78 references.

• OSTI ID: 5226494
• Journal Information: Seminars in Nuclear Medicine; (USA), Vol. 19:3; ISSN 0001-2998
• Country of Publication: United States
• Language: English

Related Subjects

62 RADIOLOGY AND NUCLEAR MEDICINE
MONOCLONAL ANTIBODIES
LABELLING
NUCLEAR MEDICINE
BIOLOGICAL HALF-LIFE
DTPA
EDTA
INDIUM ISOTOPES
IODINE ISOTOPES
METABOLISM
RADIOIMMUNOSCINTIGRAPHY
RADIOIMMUNOTHERAPY
REVIEWS
AMINO ACIDS
ANTIBODIES
CARBOXYLIC ACIDS
CHELATING AGENTS
COUNTING TECHNIQUES
DIAGNOSTIC TECHNIQUES
DOCUMENT TYPES
DRUGS
IMMUNOLOGY
IMMUNOTHERAPY
ISOTOPE APPLICATIONS
ISOTOPES
MEDICINE
ORGANIC ACIDS
ORGANIC COMPOUNDS
RADIOIMMUNODETECTION
RADIOIMMUNOLOGY
RADIOISOTOPE SCANNING
RADIOLOGY
RADIOPROTECTIVE SUBSTANCES
RADIOTHERAPY
SCINTISCANNING
THERAPY
TRACER TECHNIQUES
550601* - Medicine- Unsealed Radionuclides in Diagnostics
550604 - Medicine- Unsealed Radionuclides in Therapy- (1980-)