Biodistribution pharmacokinetics and radiation dosimetry of Tc-99m D-glucaric acid in humans
- Univ. of Pisa (Italy)
Previous experimental studies have shown the high targeting potential of Tc-99m-labeled D-glucaric acid (TcGLA, a six-carbon dicarboxylic acid partly competing in vitro with fructose/glucose uptake) in animal models of acute ischemia/early necrosis of the heart or brain, and in human tumor xenografts. This study evaluated the biodistribution pharmacokinetics and radiation dosimetry of TcGLA in cancer patients. TcGLA (900 MBq) was injected i.v. as a bolus into 12 patients with breast (n=9) or colon (n=3) cancer. Whole-body scans were recorded at 0.5, 1,2,4,6, 10,24,32,46 hr while blood samples were taken at frequent intervals and urines were collected at 6-hr intervals. The MIRD approach was employed for radiation dosimetry estimates. No early or delayed adverse reactions of any type were observed. TcGLA showed an important, early and persistent accumulation in the kidneys (plateau at about 8-10% I.D.), combined with a slow hepatobiliary clearance. The TcGLA plasma disappearance curve was three-exponential, with average T {sub 1 2} values equal to 36.8, 1.4 and 0.4 hr, respectively. Urinary excretion was 45.8 {plus_minus} 7.4% I.D. from 0-6 hr, with a cumulative plateau of about 57% I.D. at 46 hr. while the cumulative extra-renal excretion was 15-30% I.D. The initial and total distribution volumes (12.5 {plus_minus} 0.9 and 47.9 {plus_minus} 81) corresponded to the extracellular and, respectively, the total body water. The main radiation dosimetry estimates (expressed as Gy/MBq) were 0.037 (kidneys), 0.065 (bladder), 0.002 (liver), 0.0035 (red marrow), 0.007 (ovaries) 0.005 (testes) and 0.003 (whole body). The favourable pharmacokinetic pattern and very low radiation dosimetry estimates obtained in this study enable further investigations on the imaging potential of TcGLA in various disease conditions.
- OSTI ID:
- 441638
- Report Number(s):
- CONF-950603-; ISSN 0161-5505; TRN: 96:002093-0063
- Journal Information:
- Journal of Nuclear Medicine, Vol. 36, Issue Suppl.5; Conference: 42. annual meeting of the Society of Nuclear Medicine, Minneapolis, MN (United States), 12-15 Jun 1995; Other Information: PBD: May 1995
- Country of Publication:
- United States
- Language:
- English
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