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Synthesis of 99mTc-DOTMP and its preclinical evaluation as a multidentate imaging agent for skeletal metastases.

Authors
  • Datta, Anupama
  • Panwar, Puja
  • Chuttani, Krishna
  • Mishra, Anil Kumar
Type
Published Article
Journal
Cancer Biotherapy & Radiopharmaceuticals
Publisher
Mary Ann Liebert
Publication Date
February 2009
Volume
24
Issue
1
Pages
123–128
Identifiers
DOI: 10.1089/cbr.2008.0536
PMID: 19243254
Source
Medline
License
Unknown

Abstract

The convenient synthetic methodology and in vivo stability of the bone-seeking gamma-radiation-emitting compound, (99m)Tc-DOTMP are described in this paper. The radiolabeling efficiency was found to be >97%, and the stability in serum indicated that (99m)Tc remained bound to the chelate, DOTMP, for up to 24 hours. Blood clearance showed a quick washout from the circulation, and biologic half-life was found to be t(1/2)(F) = 25 min; t(1/2)(S) = 6 hours 5 minutes. The LD(50) was found to be 70 mg/kg, as determined by toxicity studies in BALB/c mice. Biodistribution characteristics of (99m)Tc-DOTMP were examined in BALB/c mice. The drug was excreted mainly through renal routes and the accumulation of (99m)Tc-DOTMP in bone was 9.06 +/- 0.75 percent injected dose per gram at 1 hour. Visual image analysis of (99m)Tc-DOTMP was clinically comparable to the interpretation of imaging studies with conventional (99m)Tc-MDP and other phosphonate derivatives. (99m)Tc-DOTMP injected into Balb/c mice showed prominent bone localization and rapid clearance from blood and other organs, thereby making it a promising candidate as a diagnostic pharmaceutical of bone metastases.

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