A fully automated synthesis for the preparation of 68Ga-labelled peptides

Somatostatin receptor scintigraphy is an accurate imaging modality for the diagnosis of neuroendocrine tumor. Because detection of distant metastases has a major impact on treatment, early diagnosis of metastatic spread is of great importance. So far, no standard procedure has become established for the early diagnosis of bone metastases from neuroendocrine tumor. We compared the diagnostic value of CT with that of the novel somatostatin analog 68 Ga-1,4,7,10-tetraazacyclododecane-N,N9,N$,N999-tetraacetic acid-D-Phe 1 -Tyr 3 -octreotide ( 68 Ga-DOTATOC) in the detection of such metastases. Methods: Fifty-one patients (22 women and 29 men; age range, 32-87 y) with histologically verified neuroendocrine tumor were included in this study. PET scans were fused with CT scans using a vacuum fixation device. 18 F-NaF or 99m Tc-dicarboxypropane diphosphonate bone scans or clinical follow-up served as the reference standard. Results: Twelve of the 51 patients had no evidence of bone metastases on any of the available imaging modalities, and 37 patients had 68 Ga-DOTATOC PET results true-positive for bone metastases. 68 Ga-DOTATOC PET results were true-negative for 12 patients, false-positive for one, and false-negative for another, resulting in a sensitivity of 97% and a specificity of 92%. 68 Ga-DOTATOC PET detected bone metastases at a significantly higher rate than did CT (P , 0.001). Furthermore, conventional bone scans confirmed the results of somatostatin receptor PET but did not reveal additional tumors in any patients. Conclusion: 68 Ga-DOTATOC PET is a reliable, novel method for the early detection of bone metastases in patients with neuroendocrine tumor. Our results show that CT and conventional bone scintigraphy are less accurate than 68 Ga-DOTATOC PET in the primary staging or restaging of neuroendocrine tumor.

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“…68 Ga-DOTATOC PET Preparation of 68 Ga-DOTATOC was based on a fully automated synthesis, as described previously (17).…”

Section: Patientsmentioning

confidence: 99%

Bone Metastases in Patients with Neuroendocrine Tumor: ⁶⁸Ga-DOTA-Tyr³-Octreotide PET in Comparison to CT and Bone Scintigraphy

Putzer¹,

Gabriel²,

Henninger³

et al. 2009

J Nucl Med

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189

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“…The radionuclide purity (RNP, expressed as the activities of 68 Ge over 68 Ga) of 68 Ge was found nearly 10 -2 %. In the labeling step, solid phase extraction by C 18 reversed phase provides an extra ''safety net'' for clinical applications since it reduces 68 Ge and RNP alters to a level of 10 -4 % [18].…”

Section: Resultsmentioning

confidence: 99%

Speciation of no-carrier-added 68Ga prior to its labeling for PET imaging

Sen

Breeman

Wolterbeek

2011

J Radioanal Nucl Chem

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The present article describes the probable speciation of 68 Ga radionuclide just before labeling to DOTA peptides for PET imaging. The 68 Ga eluted from an anion exchange column after its purification was analyzed for its elemental composition and pH at several stages. Neutron activation analysis of the eluted fractions yields the concentrations of Na and Cl, pH measurements indicate the concentration of free H ? ions in the medium and specific activity calculations indicate the concentration of 68 Ga in the solution. Using all these information we get the idea of speciation of no carrier added Ga in the eluted fractions from CHEAQS programme. The estimations indicate that Ga is mostly present as GaCl 2? in the total MiliQ eluate. However, just before labeling of DOTA the pH of the Ga-containing eluate is adjusted to *3.5 using HEPES buffer and at that condition Ga remains as Ga 3? species which is responsible for a successful and efficient labeling. The MilliQ eluate collected before actual labeling was estimated for trace elements using inductively coupled plasma atomic emission spectrometry was found to contain a few ppb of Al, Co, Pd and Pt that did not interfere in the actual labeling. A clear idea about the prerequisite of 68 Ga species before labeling to a peptide might be of special interest for its judicious application as a radiopharmaceutical.

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“…pořád obsahuje poměrně zásadní množ-ství matečného germania-68 [62][63][64][65]. Nutnost dodatečného zpracování eluátu z generátoru může u koncového uživa-tele -nemocnice -zvyklého na jednoduché zacházení s Tc generátory znamenat zásadní problém i z hlediska potřebného personálu a vybavení nutného k dodržení správné praxe při produkci fi nální lékové formy.…”

Section: S133unclassified

Current Trends in Using PET Radiopharmaceuticals for Dia gnostics in Oncology

Adam¹,

Kaderavek²,

Kužel³

et al. 2014

Klin Onkol

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1 Regionální centrum aplikované molekulární onkologie, Masarykův onkologický ústav, Brno 2 ÚJV Řež, a. s., Husinec-Řež 3 Oddělení nukleární medicíny, Masarykův onkologický ústav, Brno SouhrnNukleární medicína je důležitým oborem moderní medicíny, zejména díky své roli v in vivo zobrazování důležitých procesů v lidském organizmu. Toto je možné prostřednictvím využití radiofarmak, specifi ckých látek značených radioaktivním nuklidem, jejichž distribuci v těle lze vizualizovat pomocí speciálních skenerů a na základě fyziologických zákonitostí interpretovat dia gnózu. Pozitronová emisní tomografi e (PET) je moderní a v mnoha směrech nepostradatelná metoda nukleární medicíny. Spektrum radiofarmak pro tuto metodu dostupných se v posledních letech zvyšuje díky koordinované snaze výrobců syntézních zařízení, chemiků i potenciálních uživatelů -lékařů. Článek se formou přehledového článku zabývá vývojem na poli PET radiofarmak v posledních pěti letech s ohledem na onkologické aplikace PET. Klíčová slovanukleární lékařství -pozitronová emisní tomografi e -radiofarmaka -gallium-68 -uhlík-11 -fl uor-18 -zirkonium-89 SummaryNuclear medicine is an important fi eld of modern medicine, particularly thanks to its role in in vivo imaging of important processes in human organism. This is possible thanks to the use of radiopharmaceuticals, specifi c substances labeled by radioactive nuclide, its distribution in the body can be visualized by specialized scanners and, based on the knowledge of physiological patterns, dia gnosis can be determined. Positron emission tomography (PET) is a modern and in many ways indispensable method of nuclear medicine. The spectrum of radiopharmaceuticals available in recent years is broadening thanks to a coordinated eff ort of manufacturers of synthesis equipment, chemists and potential users -physicians. This review focuses on the development in the PET radiopharmaceutical fi eld in the last fi ve years, with an emphasis on oncological applications of PET.

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A fully automated synthesis for the preparation of 68Ga-labelled peptides

Abstract: The system described allows the fully automated, efficient and rapid preparation of Ga-DOTA-derivatized peptides. It has been used successfully and reliably for routine preparations in clinical studies.

Cited by 102 publications

References 7 publications

Bone Metastases in Patients with Neuroendocrine Tumor: ⁶⁸Ga-DOTA-Tyr³-Octreotide PET in Comparison to CT and Bone Scintigraphy

Bone Metastases in Patients with Neuroendocrine Tumor: ⁶⁸Ga-DOTA-Tyr³-Octreotide PET in Comparison to CT and Bone Scintigraphy

Speciation of no-carrier-added 68Ga prior to its labeling for PET imaging

Current Trends in Using PET Radiopharmaceuticals for Dia gnostics in Oncology

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A fully automated synthesis for the preparation of 68Ga-labelled peptides

Abstract: The system described allows the fully automated, efficient and rapid preparation of Ga-DOTA-derivatized peptides. It has been used successfully and reliably for routine preparations in clinical studies.

Cited by 102 publications

References 7 publications

Bone Metastases in Patients with Neuroendocrine Tumor: 68Ga-DOTA-Tyr3-Octreotide PET in Comparison to CT and Bone Scintigraphy

Bone Metastases in Patients with Neuroendocrine Tumor: 68Ga-DOTA-Tyr3-Octreotide PET in Comparison to CT and Bone Scintigraphy

Speciation of no-carrier-added 68Ga prior to its labeling for PET imaging

Current Trends in Using PET Radiopharmaceuticals for Dia gnostics in Oncology

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Product

Resources

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Bone Metastases in Patients with Neuroendocrine Tumor: ⁶⁸Ga-DOTA-Tyr³-Octreotide PET in Comparison to CT and Bone Scintigraphy

Bone Metastases in Patients with Neuroendocrine Tumor: ⁶⁸Ga-DOTA-Tyr³-Octreotide PET in Comparison to CT and Bone Scintigraphy