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Synthesis of Poly[APMA]-DOTA-64Cu conjugates for interventional radionuclide therapy of prostate cancer: assessment of intratumoral retention by micro-positron emission tomography.

Abstract
To develop new radiopharmaceuticals for interventional radionuclide therapy of locally recurrent prostate cancer, poly[N-(3-aminopropyl)methacrylamide] [poly(APMA)] polymers were synthesized by free radical precipitation polymerization in acetone-dimethylsulfoxide using N,N'-azobis(isobutyronitrile) as the initiator. The polymers were characterized with nuclear magnetic resonance, size exclusion chromatography, and dynamic light scattering (M(n) = 2.40 x 10(4), M(w)/M(n) = 1.87). Subsequently, poly[APMA] was coupled with 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) using 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride as an activator, followed by conjugation with (64)Cu radionuclide. Prolonged retention of poly[APMA]-DOTA-(64)Cu conjugates within the tumor tissues was demonstrated by micro-positron emission tomography at 24 hours following intra-tumoral injection of the conjugates to human prostate xenografts in mice. The data suggest that the poly[APMA]-DOTA-(64)Cu conjugates might be useful for interventional radionuclide therapy of locally recurrent prostate cancer in humans.
AuthorsJianchao Yuan, Yezi You, Xin Lu, Otto Muzik, David Oupicky, Fangyu Peng
JournalMolecular imaging (Mol Imaging) 2007 Jan-Feb Vol. 6 Issue 1 Pg. 10-7 ISSN: 1535-3508 [Print] England
PMID17311761 (Publication Type: Journal Article, Research Support, N.I.H., Extramural, Research Support, Non-U.S. Gov't)
Chemical References
  • Acrylic Resins
  • Heterocyclic Compounds, 1-Ring
  • Nitriles
  • Organometallic Compounds
  • Radiopharmaceuticals
  • poly(N-(3-aminopropyl)methacrylamide)-DOTA-64Cu conjugate
  • 1,4,7,10-tetraazacyclododecane- 1,4,7,10-tetraacetic acid
  • azobis(isobutyronitrile)
Topics
  • Acrylic Resins (analysis, chemical synthesis, pharmacokinetics)
  • Animals
  • Heterocyclic Compounds, 1-Ring (chemistry)
  • Humans
  • Light
  • Magnetic Resonance Spectroscopy
  • Male
  • Mice
  • Mice, Inbred Strains
  • Nitriles (chemistry)
  • Organometallic Compounds (analysis, chemical synthesis, pharmacokinetics)
  • Positron-Emission Tomography
  • Prostatic Neoplasms (chemistry, metabolism, radiotherapy)
  • Radiopharmaceuticals (analysis, chemical synthesis, pharmacokinetics)
  • Scattering, Radiation
  • Xenograft Model Antitumor Assays

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