Development of a stable radioiodinating reagent to label monoclonal antibodies for radiotherapy of cancer
- NeoRx Corporation, Seattle, WA (USA)
A method of radioiodinating monoclonal antibodies such that the labeled antibodies do not undergo in vivo deiodination has been studied. The method utilizes conjugation of succinimidyl para-iodobenzoate to the antibody. The iodobenzoate was radiolabeled by using an organometallic intermediate to facilitate the reaction. Thus, succinimidyl para-tri-n-butylstannylbenzoate was radiolabeled in 60-90% radiochemical yield and subsequently conjugated to the antibody in 80-90% yield. Animal biodistribution studies were carried out with two separate anti-melanoma antibodies (9.2.27 and NR-M1-05) labeled by this method, and examined in nude mice bearing human melanoma tumor xenografts. Very large differences in the localization of radioactivity were observed in the thyroids and stomachs of mice when the iodobenzoyl-labeled antibodies were compared with the same antibodies labeled using the chloramine-T method of radioiodination. Few other significant differences in the tissue distribution of the radioiodinated antibodies were seen.
- OSTI ID:
- 5402219
- Journal Information:
- Journal of Nuclear Medicine; (USA), Vol. 30:2; ISSN 0161-5505
- Country of Publication:
- United States
- Language:
- English
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Related Subjects
MELANOMAS
RADIOIMMUNOTHERAPY
MONOCLONAL ANTIBODIES
LABELLING
RADIOPHARMACEUTICALS
CHEMICAL PREPARATION
EXPERIMENTAL NEOPLASMS
IODINE ISOTOPES
MICE
ORGANOMETALLIC COMPOUNDS
REAGENTS
TISSUE DISTRIBUTION
ANIMALS
ANTIBODIES
DISEASES
DISTRIBUTION
DRUGS
IMMUNOLOGY
IMMUNOTHERAPY
ISOTOPES
LABELLED COMPOUNDS
MAMMALS
MEDICINE
NEOPLASMS
NUCLEAR MEDICINE
ORGANIC COMPOUNDS
RADIOIMMUNOLOGY
RADIOLOGY
RADIOTHERAPY
RODENTS
SYNTHESIS
THERAPY
VERTEBRATES
550604* - Medicine- Unsealed Radionuclides in Therapy- (1980-)