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Deferoxamine, A Promising Bifunctional Chelating Agent for Labeling Proteins with Gallium: Ga-67 DF-HSA: Concise Communication

Kyoto University, Kyoto, Japan

Correspondence: For reprints contact: Akira Yokoyama PhD, Faculty of Pharmaceutical Sciences, Kyoto University, Yoshida, Sakyo-ku, Kyoto 606, Japan.

ABSTRACT

A new efficient method has been developed for the labeling of various biologically important proteins with radiogallium, using deferoxamine (DF) as a bifunctional chelating agent. Human serum albumin (HSA) was chosen for studying the DF coupling reaction by a glutaraldehyde two-step method. The DF-HSA conjugate obtained was then easily labeled with Ga-67 with high efficiency and reproducibility. High stability of the Ga-67 DF-HSA was observed both in vitro and in vivo. In rats the half-time of blood clearance at the first phase was 234 min for the Ga-67 DF-HSA, whereas most conventional I-131 HSA gives 121 min. The excellent pharmacological and physiological properties were assessed by plasma clearance and plasma volume measurements in normal volunteers. Even at 2 hr after injection, (90.0 ± 3.0)% of Ga-67 DF-HSA was retained within the vascular space. The mean plasma volume per kilogram of body weight, measured with Ga-57 DF-HAS, was 46.6 ± 3.4 ml/kg, compared with 52.2 ± 2.4 ml/kg as determined with I-131 HSA in the same men.