Comparative evaluation of 68Ga-labelled TATEs: the impact of chelators on imaging

被引:11
作者
Xia, Yuxiao [1 ,2 ]
Zeng, Chengrun [1 ,2 ]
Zhao, Yanhong [1 ,2 ]
Zhang, Xinyi [1 ,2 ]
Li, Zibo [3 ,4 ]
Chen, Yue [1 ,2 ]
机构
[1] Southwest Med Univ, Affiliated Hosp, Dept Nucl Med, 25 Taiping St, Luzhou 646000, Sichuan, Peoples R China
[2] Nucl Med & Mol Imaging Key Lab Sichuan Prov, 25 Taiping St, Luzhou 646000, Sichuan, Peoples R China
[3] Univ N Carolina, Dept Radiol, Biomed Res Imaging Ctr, Chapel Hill, NC 27514 USA
[4] Univ N Carolina, Lineberger Comprehens Canc Ctr, Chapel Hill, NC 27514 USA
关键词
Ga-68-NOTA-TATE; Ga-68-DOTA-TATE; Bifunctional chelating agent; Neuroendocrine tumour; AR42J tumour-bearing mouse; Pharmacokinetics; Positron emission tomography; Micro-PET; CT; Healthy human imaging; Maximum standardized uptake values; SOMATOSTATIN RECEPTOR ANTAGONISTS; GA-68-DOTATATE; MANAGEMENT; PET/CT; GA-68; TOMOGRAPHY; DIAGNOSIS; TUMOR; DOTA;
D O I
10.1186/s13550-020-00620-6
中图分类号
R8 [特种医学]; R445 [影像诊断学];
学科分类号
1002 ; 100207 ; 1009 ;
摘要
Background Ga-68-labelled peptides targeting somatostatin receptor 2 (SSTR2) have demonstrated encouraging results in managing patients with neuroendocrine tumours (NETs). In addition to metal chelation, bifunctional chelators have also been found to impact imaging outcomes due to their differences in stability, charge, hydrophilicity, etc. In the present work, a comparative pharmacokinetic evaluation and imaging characteristics were performed between Ga-68-labelled somatostatin analogues (TATE) using NOTA (1,4,7-triazacyclononane-1,4,7-triacetic acid) and DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid) as bifunctional chelating agents (BFCAs). Results Both Ga-68-NOTA-TATE and Ga-68-DOTA-TATE were obtained with high radiochemical purity. Ga-68-NOTA-TATE demonstrated higher in vitro stability (>= 99%) than Ga-68-DOTA-TATE (>= 95%) after 3 h of incubation. The water solubilities (partition coefficients, - 1.76 +/- 0.06 vs. - 2.72 +/- 0.16) and plasma protein binding rates (12.12% vs. 30.6%) were lower for Ga-68-NOTA-TATE than for Ga-68-DOTA-TATE. Differential pharmacokinetics and comparable tumour affinities (within 1 h) were observed in AR42J tumour-bearing mice. Healthy volunteer imaging studies showed comparable distribution patterns of these two imaging agents. However, the maximum standardized uptake values (SUVmax) of the two tracers varied in each organ. The two PET agents demonstrated almost identical SUVmax values in the kidneys. Ga-68-NOTA-TATE did have a lower SUVmax in most other organs compared with Ga-68-DOTA-TATE, including the liver (4.2 vs. 10.1), potentially due to the lower protein binding rate. Conclusion Ga-68-NOTA-TATE and Ga-68-DOTA-TATE demonstrated comparable tumour uptake in an AR42J mouse model. An initial clinical study revealed that Ga-68-NOTA-TATE may have reduced background uptake in the major organs such as the liver. Although the subject numbers were limited, further investigation of Ga-68-NOTA-TATE is warranted for detecting SSTR2-positive neuroendocrine tumours.
引用
收藏
页数:11
相关论文
共 50 条
  • [21] The diagnostic value of PET/CT imaging with the 68Ga-labelled PSMA ligand HBED-CC in the diagnosis of recurrent prostate cancer
    Ali Afshar-Oromieh
    Eleni Avtzi
    Frederik L. Giesel
    Tim Holland-Letz
    Heinz G. Linhart
    Matthias Eder
    Michael Eisenhut
    Silvan Boxler
    Boris A. Hadaschik
    Clemens Kratochwil
    Wilko Weichert
    Klaus Kopka
    Jürgen Debus
    Uwe Haberkorn
    European Journal of Nuclear Medicine and Molecular Imaging, 2015, 42 : 197 - 209
  • [22] 68Ga-labelled PSMA ligand HBED-CC PET/CT imaging in patients with recurrent prostate cancer
    Elif Neslihan Akdemir
    Murat Tuncel
    Fadıl Akyol
    Cenk Yucel Bilen
    Dilek Ertoy Baydar
    Erdem Karabulut
    Haluk Ozen
    Meltem Caglar
    World Journal of Urology, 2019, 37 : 813 - 821
  • [23] Comparison of DOTA and NODAGA as chelates for 68Ga-labelled CDP1 as novel infection PET imaging agents
    A. H. Mdlophane
    T. Ebenhan
    B. Marjanovic-Painter
    T. Govender
    M. M. Sathekge
    J. R. Zeevaart
    Journal of Radioanalytical and Nuclear Chemistry, 2019, 322 : 629 - 638
  • [24] Comparison of DOTA and NODAGA as chelates for 68Ga-labelled CDP1 as novel infection PET imaging agents
    Mdlophane, A. H.
    Ebenhan, T.
    Marjanovic-Painter, B.
    Govender, T.
    Sathekge, M. M.
    Zeevaart, J. R.
    JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY, 2019, 322 (02) : 629 - 638
  • [25] Comparison of 68Ga-labelled PSMA-11 and 11C-choline in the detection of prostate cancer metastases by PET/CT
    Schwenck, Johannes
    Rempp, Hansjoerg
    Reischl, Gerald
    Kruck, Stephan
    Stenzl, Arnulf
    Nikolaou, Konstantin
    Pfannenberg, Christina
    la Fougere, Christian
    EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING, 2017, 44 (01) : 92 - 101
  • [26] Pharmacokinetic Properties of 68Ga-labelled Folic Acid Conjugates: Improvement Using HEHE Tag
    Larenkov, Anton
    Rakhimov, Marat
    Lunyova, Kristina
    Klementyeva, Olga
    Maruk, Alesya
    Machulkin, Aleksei
    MOLECULES, 2020, 25 (11):
  • [27] Comparison of PET imaging with a 68Ga-labelled PSMA ligand and 18F-choline-based PET/CT for the diagnosis of recurrent prostate cancer
    Afshar-Oromieh, Ali
    Zechmann, Christian M.
    Malcher, Anna
    Eder, Matthias
    Eisenhut, Michael
    Linhart, Heinz G.
    Holland-Letz, Tim
    Hadaschik, Boris A.
    Giesel, Frederik L.
    Debus, Juergen
    Haberkorn, Uwe
    EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING, 2014, 41 (01) : 11 - 20
  • [28] Comparison of PET imaging with a 68Ga-labelled PSMA ligand and 18F-choline-based PET/CT for the diagnosis of recurrent prostate cancer
    Ali Afshar-Oromieh
    Christian M. Zechmann
    Anna Malcher
    Matthias Eder
    Michael Eisenhut
    Heinz G. Linhart
    Tim Holland-Letz
    Boris A. Hadaschik
    Frederik L. Giesel
    Jürgen Debus
    Uwe Haberkorn
    European Journal of Nuclear Medicine and Molecular Imaging, 2014, 41 : 11 - 20
  • [29] Synthesis, in vitro and in vivo characterization of two novel 68Ga-labelled 5-nitroimidazole derivatives as potential agents for imaging hypoxia
    Fernandez, Soledad
    Dematteis, Sylvia
    Giglio, Javier
    Cerecetto, Hugo
    Rey, Ana
    NUCLEAR MEDICINE AND BIOLOGY, 2013, 40 (02) : 273 - 279
  • [30] PET imaging of αvβ3 integrin expression in tumours with 68Ga-labelled mono-, di- and tetrameric RGD peptides
    Ingrid Dijkgraaf
    Cheng-Bin Yim
    Gerben M. Franssen
    Robert C. Schuit
    Gert Luurtsema
    Shuang Liu
    Wim J. G. Oyen
    Otto C. Boerman
    European Journal of Nuclear Medicine and Molecular Imaging, 2011, 38 : 128 - 137