Development of a stable radioiodinating reagent to label monoclonal antibodies for radiotherapy of cancer

Journal Article · Tue Jan 31 23:00:00 EST 1989 · Journal of Nuclear Medicine; (USA)

OSTI ID:5402219

Wilbur, D S; Hadley, S W; Hylarides, M D; Abrams, P G; Beaumier, P A; Morgan, A C; Reno, J M; Fritzberg, A R ^[1]

---

1. 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), Journal Name: Journal of Nuclear Medicine; (USA) Vol. 30:2; ISSN 0161-5505; ISSN JNMEA
• Country of Publication: United States
• Language: English

Related Subjects

550604* -- Medicine-- Unsealed Radionuclides in Therapy-- (1980-)
62 RADIOLOGY AND NUCLEAR MEDICINE
ANIMALS
ANTIBODIES
CHEMICAL PREPARATION
DISEASES
DISTRIBUTION
DRUGS
EXPERIMENTAL NEOPLASMS
IMMUNOLOGY
IMMUNOTHERAPY
IODINE ISOTOPES
ISOTOPES
LABELLED COMPOUNDS
LABELLING
MAMMALS
MEDICINE
MELANOMAS
MICE
MONOCLONAL ANTIBODIES
NEOPLASMS
NUCLEAR MEDICINE
ORGANIC COMPOUNDS
ORGANOMETALLIC COMPOUNDS
RADIOIMMUNOLOGY
RADIOIMMUNOTHERAPY
RADIOLOGY
RADIOPHARMACEUTICALS
RADIOTHERAPY
REAGENTS
RODENTS
SYNTHESIS
THERAPY
TISSUE DISTRIBUTION
VERTEBRATES