Deferoxamine, a promising bifunctional chelating agent for labeling proteins with gallium: Ga-67 DF-HSA: concise...

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-67 DF-HSA, 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.