Copper-67-labeled monoclonal antibody Lym-1, a potential radiopharmaceutical for cancer therapy: Labeling and biodistribution in RAJI tumored mice

S. V. Desphande, S. J. DeNardo, C. F. Meares, M. J. McCall, G. P. Adams, M. K. Moi, Gerald L Denardo

Research output: Contribution to journalArticle

103 Citations (Scopus)

Abstract

Copper-67 (67Cu) is one of the most compromising radiometals for radioimmunotherapy because of its 61.5 hr physical half-life, abundant beta particles, and gamma emmissions suitable for imaging. However, 67Cu is readily tranferred from the usual chelates of EDTA or DTPA to albumen. We developed a new macrocycle (6-p-nitrobenzyl-TETA) to chelate copper. Bifunctional chelating agent p-bromoacetamidobenzyl-TETA was conjugated to Lym-1, a monoclonal antibody against human B cell lymphoma, without significantly altering its immunoreactivity. This conjugate was stably labeled with 67Cu under conditions chosen to optimize the yield of a high specific activity radiopharmaceutical. The biodistribution in RAJI tumor bearing mice demonstrated significant tumor uptake (14.7% ID per gram) and extended residence time (120 hr) in contrast to normal organs. After 24 hr, radioactivity was continuously cleared from all tissues except the tumor. This study suggests 67Cu labeled Lym-1 to be a promising radiopharmaceutical for potential use for radioimmunotherapy of B cell lymphoma.

Original languageEnglish (US)
Pages (from-to)217-225
Number of pages9
JournalJournal of Nuclear Medicine
Volume29
Issue number2
StatePublished - 1988

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Radiopharmaceuticals
Radioimmunotherapy
Copper
B-Cell Lymphoma
Beta Particles
Neoplasms
Pentetic Acid
Chelating Agents
Edetic Acid
Radioactivity
Half-Life
Therapeutics
Lym-1 monoclonal antibody

ASJC Scopus subject areas

  • Radiological and Ultrasound Technology

Cite this

Copper-67-labeled monoclonal antibody Lym-1, a potential radiopharmaceutical for cancer therapy : Labeling and biodistribution in RAJI tumored mice. / Desphande, S. V.; DeNardo, S. J.; Meares, C. F.; McCall, M. J.; Adams, G. P.; Moi, M. K.; Denardo, Gerald L.

In: Journal of Nuclear Medicine, Vol. 29, No. 2, 1988, p. 217-225.

Research output: Contribution to journalArticle

Desphande, S. V. ; DeNardo, S. J. ; Meares, C. F. ; McCall, M. J. ; Adams, G. P. ; Moi, M. K. ; Denardo, Gerald L. / Copper-67-labeled monoclonal antibody Lym-1, a potential radiopharmaceutical for cancer therapy : Labeling and biodistribution in RAJI tumored mice. In: Journal of Nuclear Medicine. 1988 ; Vol. 29, No. 2. pp. 217-225.
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abstract = "Copper-67 (67Cu) is one of the most compromising radiometals for radioimmunotherapy because of its 61.5 hr physical half-life, abundant beta particles, and gamma emmissions suitable for imaging. However, 67Cu is readily tranferred from the usual chelates of EDTA or DTPA to albumen. We developed a new macrocycle (6-p-nitrobenzyl-TETA) to chelate copper. Bifunctional chelating agent p-bromoacetamidobenzyl-TETA was conjugated to Lym-1, a monoclonal antibody against human B cell lymphoma, without significantly altering its immunoreactivity. This conjugate was stably labeled with 67Cu under conditions chosen to optimize the yield of a high specific activity radiopharmaceutical. The biodistribution in RAJI tumor bearing mice demonstrated significant tumor uptake (14.7{\%} ID per gram) and extended residence time (120 hr) in contrast to normal organs. After 24 hr, radioactivity was continuously cleared from all tissues except the tumor. This study suggests 67Cu labeled Lym-1 to be a promising radiopharmaceutical for potential use for radioimmunotherapy of B cell lymphoma.",
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AU - Meares, C. F.

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AU - Denardo, Gerald L

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