Synthesis of poly[APMA]-DOTA-64Cu conjugates for interventional radionuclide therapy of prostate cancer

Assessment of intratumoral retention by micro-positron emission tomography

Jianchao Yuan, Yezi You, Xin Lu, Otto Muzik, David Oupicky, Fangyu Peng

Research output: Contribution to journalArticle

14 Citations (Scopus)

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 acetonedimethylsulfoxide using N,N-azobis(isobutyronitrile) as the initiator. The polymers were characterized with nuclear magnetic resonance, size exclusion chromatography, and dynamic light scattering (Mn = 2.40 × 104, Mw/Mn = 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 64Cu radionuclide. Prolonged retention of poly[APMA]-DOTA-64Cu 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-64Cu conjugates might be useful for interventional radionuclide therapy of locally recurrent prostate cancer in humans.

Original languageEnglish (US)
Pages (from-to)10-17
Number of pages8
JournalMolecular Imaging
Volume6
Issue number1
DOIs
StatePublished - Jan 2007

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Positron emission tomography
Radioisotopes
Positron-Emission Tomography
Prostatic Neoplasms
Acids
Polymers
Size exclusion chromatography
Ethyldimethylaminopropyl Carbodiimide
Dynamic light scattering
Free radicals
Radiopharmaceuticals
Tumors
Therapeutics
Polymerization
Heterografts
Nuclear magnetic resonance
Tissue
Free Radicals
Gel Chromatography
Prostate

ASJC Scopus subject areas

  • Engineering(all)

Cite this

Synthesis of poly[APMA]-DOTA-64Cu conjugates for interventional radionuclide therapy of prostate cancer : Assessment of intratumoral retention by micro-positron emission tomography. / Yuan, Jianchao; You, Yezi; Lu, Xin; Muzik, Otto; Oupicky, David; Peng, Fangyu.

In: Molecular Imaging, Vol. 6, No. 1, 01.2007, p. 10-17.

Research output: Contribution to journalArticle

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