Toward realization of 'mix-and-use' approach in ⁶⁸Ga radiopharmacy: preparation, evaluation and preliminary clinical utilization of ⁶⁸Ga-labeled NODAGA-coupled RGD peptide derivative.

Abstract:

INTRODUCTION:The present article demonstrates a 'mix-and-use' approach for radiolabeling RGD peptide derivative with (68)Ga, which is easily adaptable in hospital radiopharmacy practice. The radiotracer thus formulated was successfully used for positron emission tomography (PET) imaging of breast cancer in human patients. METHODS:The conditions for radiolabeling NODAGA-coupled dimeric cyclic RGD peptide derivative [NODAGA-(RGD)2] with (68)Ga were optimized using (68)Ga obtained from a (68)Ge/(68)Ga generator developed in-house with CeO2-PAN composite sorbent as well as from a commercial (68)Ge/(68)Ga generator obtained from ITG, Germany. Preclinical studies were carried out in C57BL/6 mice bearing melanoma tumors. The radiotracer was prepared in a hospital radiopharmacy using (68)Ga obtained from ITG generator and used for monitoring breast cancer patients by positron emission tomography (PET) imaging. RESULTS:(68)Ga-NODAGA-(RGD)2 could be prepared with high radiolabeling yield (>98%) and specific activity (~50 GBq/μmol) within 10 min at room temperature by mixing (68)Ga with the solution of the peptide conjugate. In vivo biodistribution studies showed significant uptake (5.24±0.39% ID/g) in melanoma tumor at 30 min post-injection, with high tumor-to-background contrast. The integrin αvβ3 specificity of the tracer was corroborated by blocking study. Preliminary clinical studies in locally advanced breast cancer (LABC) patients indicated specifically high tumor uptake (SUVmax 10-15) with good contrast. CONCLUSIONS:This is one of the very few reports which presents preliminary clinical data on use of (68)Ga-NODAGA-(RGD)2 and the developed 'mix-and-use' holds tremendous prospect in clinical PET imaging using (68)Ga.

journal_name

Nucl Med Biol

authors

Chakraborty S,Chakravarty R,Vatsa R,Bhusari P,Sarma HD,Shukla J,Mittal BR,Dash A

doi

10.1016/j.nucmedbio.2015.09.010

subject

Has Abstract

pub_date

2016-01-01 00:00:00

pages

116-123

issue

1

eissn

0969-8051

issn

1872-9614

pii

S0969-8051(15)00169-9

journal_volume

43

pub_type

杂志文章
  • Preparation and pharmacokinetics of 11C labeled stavudine (d4T).

    abstract::Stavudine, a potent antiviral agent for treating human immunodeficiency virus (HIV) infections, was radiolabeled with (11)C by methylation of a specifically designed precursor, 5'-O-(2-tetrahydropyranyl)-5-bromo-2',3'-didehydro-3'-deoxythymidine, with (11)C H(3)I. The radiolabeled drug was isolated by reverse phase HP...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2003.11.006

    authors: Livni E,Berker M,Hillier S,Waller SC,Ogan MD,Discordia RP,Rienhart JK,Rubin RH,Fischman AJ

    更新日期:2004-07-01 00:00:00

  • Change of central cholinergic receptors following lesions of nucleus basalis magnocellularis in rats: search for an imaging index suitable for the early detection of Alzheimer's disease.

    abstract::Cholinergic system in the central nervous system is involved in the memory function. Thus, because the dysfunction of cholinergic system that project to the cerebral cortex from nucleus basalis of Meynert (nbM) would be implicated in the memory function deficits in Alzheimer's disease (AD), evaluating cholinergic func...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2005.06.013

    authors: Ogawa M,Iida Y,Nakagawa M,Kuge Y,Kawashima H,Tominaga A,Ueda M,Magata Y,Saji H

    更新日期:2006-02-01 00:00:00

  • True tracers: comparing FDG with glucose and FLT with thymidine.

    abstract::As PET metabolic imaging becomes routine in clinical practice, there is a tendency to make imaging and data analysis fast and simple, but interpretation of these pictures by visual inspection does not do justice to the power of PET technology. Tissue data and blood data can be analyzed mathematically to provide parame...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章,评审

    doi:10.1016/j.nucmedbio.2005.04.004

    authors: Krohn KA,Mankoff DA,Muzi M,Link JM,Spence AM

    更新日期:2005-10-01 00:00:00

  • 99Mo/(99m)Tc separation: an assessment of technology options.

    abstract::Several strategies for the effective separation of (99m)Tc from (99)Mo have been developed and validated. Due to the success of column chromatographic separation using acidic alumina coupled with high specific activity fission (99)Mo (F (99)Mo) for production of (99)Mo/(99m)Tc generators, however, most technologies un...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章,评审

    doi:10.1016/j.nucmedbio.2012.10.005

    authors: Dash A,Knapp FF Jr,Pillai MR

    更新日期:2013-02-01 00:00:00

  • Synthesis of an I-123 analog of A-85380 and preliminary SPECT imaging of nicotinic receptors in baboon.

    abstract::A radiosynthetic method to prepare the nicotinic acetylcholine receptor radioligand (S)-5-[123I]iodo-3-(2-azetidinylmethoxy)pyridine, 5-IA, has been developed. The two-step sequence produced [123I]-5-IA in high radiochemical yield (52%), high radiochemical purity (98%), and high specific radioactivities (> 8,500 mCi/m...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/s0969-8051(98)00101-2

    authors: Musachio JL,Villemagne VL,Scheffel UA,Dannals RF,Dogan AS,Yokoi F,Wong DF

    更新日期:1999-02-01 00:00:00

  • Application of image-derived and venous input functions in major depression using [carbonyl-(11)C]WAY-100635.

    abstract:INTRODUCTION:Image-derived input functions (IDIFs) represent a promising non-invasive alternative to arterial blood sampling for quantification in positron emission tomography (PET) studies. However, routine applications in patients and longitudinal designs are largely missing despite widespread attempts in healthy sub...

    journal_title:Nuclear medicine and biology

    pub_type: 临床试验,杂志文章

    doi:10.1016/j.nucmedbio.2012.12.011

    authors: Hahn A,Nics L,Baldinger P,Wadsak W,Savli M,Kraus C,Birkfellner W,Ungersboeck J,Haeusler D,Mitterhauser M,Karanikas G,Kasper S,Frey R,Lanzenberger R

    更新日期:2013-04-01 00:00:00

  • Comparison of (18)F-FET and (18)F-FDG PET in brain tumors.

    abstract:UNLABELLED:The purpose of this study was to compare the diagnostic value of positron emission tomography (PET) using [(18)F]-fluorodeoxyglucose ((18)F-FDG) and O-(2-[(18)F]fluoroethyl)-l-tyrosine ((18)F-FET) in patients with brain lesions suspicious of cerebral gliomas. METHODS:Fifty-two patients with suspicion of cer...

    journal_title:Nuclear medicine and biology

    pub_type: 临床试验,杂志文章

    doi:10.1016/j.nucmedbio.2009.05.005

    authors: Pauleit D,Stoffels G,Bachofner A,Floeth FW,Sabel M,Herzog H,Tellmann L,Jansen P,Reifenberger G,Hamacher K,Coenen HH,Langen KJ

    更新日期:2009-10-01 00:00:00

  • Synthesis of O-(2-[18F]fluoroethyl)-L-tyrosine based on a cartridge purification method.

    abstract:INTRODUCTION:O-(2-[(18)F]fluoroethyl)-L-tyrosine (FET) is widely used as a positron emission tomography tracer for brain tumors. Usually, a high-performance liquid chromatography (HPLC) purification at the end of the two-step synthesis is applied. In this work, we report an automatic radiosynthesis of FET with a purifi...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2011.01.006

    authors: Mueller D,Klette I,Kalb F,Baum RP

    更新日期:2011-07-01 00:00:00

  • A simplified method for the measurement of nonmetabolized 2-[18F]F-A-85380 in blood plasma using solid-phase extraction.

    abstract::Quantification of alpha(4)beta(2)* nicotinic acetylcholine receptors using 2-[(18)F]fluoro-3-(2(S)-azetidinylmethoxy)pyridine (2-[(18)F]FA) and positron emission tomography (PET) imaging requires measurement of nonmetabolized radioligand in blood plasma, which was previously accomplished using high-performance liquid ...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2006.12.001

    authors: Shumway DA,Pavlova OA,Mukhin AG

    更新日期:2007-02-01 00:00:00

  • Preclinical evaluation of (99m)Tc labeled chondroitin sulfate for monitoring of cartilage degeneration in osteoarthritis.

    abstract:PURPOSE:In previous in-vitro and ex-vivo studies we proved the specific uptake of (99m)Tc radiolabeled chondroitin sulfate (CS) in human articular cartilage. As a logical next step for the clinical use for imaging osteoarthritis we investigated in-vivo uptake of (99m)TcCS in dogs. PROCEDURES:The radiolabeling of CS Co...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2016.02.009

    authors: Sobal G,Velusamy K,Kosik S,Menzel J,Hacker M,Pagitz M

    更新日期:2016-06-01 00:00:00

  • Influence of different chelators on the radiochemical properties of a 68-Gallium labelled bombesin analogue.

    abstract:UNLABELLED:The radiolabelled bombesin analogue AMBA shows high potential for diagnosis and treatment of prostate and breast cancer, but the influence of different chelators, which differ in terms of radiochemical reactivity and stability, have not been explored so far. In order to find the best suitable chelator for la...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2013.08.010

    authors: Asti M,Iori M,Capponi PC,Atti G,Rubagotti S,Martin R,Brennauer A,Müller M,Bergmann R,Erba PA,Versari A

    更新日期:2014-01-01 00:00:00

  • Evaluation of [11C]KB631 as a PET tracer for in vivo visualisation of HDAC6 in B16.F10 melanoma.

    abstract:INTRODUCTION:HDAC6, a structural and functional distinct member of the HDAC-family, shows great promise as a target to treat several cancers and neurodegenerative diseases. Several clinical trials are evaluating HDAC6 inhibitors in solid tumours and haematological malignancies, but so far no HDAC6 inhibitor has receive...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2019.05.004

    authors: Vermeulen K,Ahamed M,Luyten K,Bormans G

    更新日期:2019-01-01 00:00:00

  • Clinical 68Ga-PET: Is radiosynthesis module an absolute necessity?

    abstract:INTRODUCTION:The commercially available 68Ge/68Ga generators are generally used in clinical context in conjunction with automated or semi-automated modules for the syntheses of 68Ga radiopharmaceuticals. It is desirable to develop strategies for the formulation of 68Ga-radiopharmaceuticals without use of such expensive...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2016.11.006

    authors: Chakravarty R,Chakraborty S,Radhakrishnan ER,Kamaleshwaran K,Shinto A,Dash A

    更新日期:2017-03-01 00:00:00

  • An original radio-biomimetic approach to synthesize radiometabolites for PET imaging.

    abstract::To fully exploit the potential of positron emission tomography (PET) imaging to assess drug distribution and pharmacokinetics in the central nervous system, the contribution of radiometabolites to the PET signal has to be determined for correct interpretation of data. However, radiosynthesis and extensive study of rad...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2020.08.001

    authors: Auvity S,Breuil L,Goislard M,Bottlaender M,Kuhnast B,Tournier N,Caillé F

    更新日期:2020-01-01 00:00:00

  • Sigma1 and dopamine D2 receptor occupancy in the mouse brain after a single administration of haloperidol and two dopamine D2-like receptor ligands.

    abstract::We investigated sigma(1) and dopamine D(2) receptor occupancy in mouse brain after a single injection of haloperidol, nemonapride, or spiperone using [(11)C]SA4503 and [(11)C]raclopride, respectively. Co-injection of the three compounds significantly blocked the uptake of each radioligand. Six hours later, only halope...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/s0969-8051(03)00003-9

    authors: Ishiwata K,Kawamura K,Kobayashi T,Matsuno K

    更新日期:2003-05-01 00:00:00

  • Repeated administration of D-amphetamine induces loss of [123I]FP-CIT binding to striatal dopamine transporters in rat brain: a validation study.

    abstract:UNLABELLED:In recent years, several PET and SPECT studies have shown loss of striatal dopamine transporter (DAT) binding in amphetamine (AMPH) users. However, the use of DAT SPECT tracers to detect AMPH-induced changes in DAT binding has not been validated. We therefore examined if repeated administration of D-AMPH or ...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2005.12.007

    authors: Booij J,de Bruin K,Gunning WB

    更新日期:2006-04-01 00:00:00

  • Radio-copper-labeled Cu-ATSM: an indicator of quiescent but clonogenic cells under mild hypoxia in a Lewis lung carcinoma model.

    abstract:UNLABELLED:The purpose of this study is to reveal characteristics of (64)Cu-labeled diacetyl-bis(N(4)-methylthiosemicarbazone) ([(64)Cu]Cu-ATSM) during cell proliferation and hypoxia by autoradiography imaging and immunohistochemical staining. METHODS:The intratumoral distributions of [(64)Cu]Cu-ATSM and [(18)F]-2-flu...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2009.01.016

    authors: Oh M,Tanaka T,Kobayashi M,Furukawa T,Mori T,Kudo T,Fujieda S,Fujibayashi Y

    更新日期:2009-05-01 00:00:00

  • Fluorine-18 labeled diphenyl sulfide derivatives for imaging serotonin transporter (SERT) in the brain.

    abstract:OBJECTIVES:Serotonin transporters (SERT) play an important role in controlling serotonin concentration in the synaptic cleft and in managing postsynaptic signal transduction. Inhibitors of SERT binding are well known as selective serotonin reuptake inhibitors (SSRIs) such as fluoxetine, sertraline, paroxetine, and esci...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2018.06.008

    authors: Zhang Y,Liu F,Xiao H,Yao X,Li G,Choi SR,Ploessl K,Zha Z,Zhu L,Kung HF

    更新日期:2018-11-01 00:00:00

  • Investigation of four (99m)Tc-labeled bacteriophages for infection-specific imaging.

    abstract:INTRODUCTION:This study investigated radiolabeled bacteriophages for specific detection of infection through gamma imaging. Previously, a (99m)Tc-labeled M13 phage demonstrated specific binding for its host Escherichia coli in vitro and in mice through imaging. METHODS:This study was extended to phages P22, E79, VD-13...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2008.02.011

    authors: Rusckowski M,Gupta S,Liu G,Dou S,Hnatowich DJ

    更新日期:2008-05-01 00:00:00

  • Synthesis and fluorine-18 radiolabeling of a phospholipid as a PET imaging agent for prostate cancer.

    abstract:INTRODUCTION:Altered lipid metabolism and subsequent changes in cellular lipid composition have been observed in prostate cancer cells, are associated with poor clinical outcome, and are promising targets for metabolic therapies. This study reports for the first time on the synthesis of a phospholipid radiotracer based...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2020.11.007

    authors: Kwan KH,Burvenich IJG,Centenera MM,Goh YW,Rigopoulos A,Dehairs J,Swinnen JV,Raj GV,Hoy AJ,Butler LM,Scott AM,White JM,Ackermann U

    更新日期:2020-11-28 00:00:00

  • A new approach to labeling cells with technetium-99m, Part II. Evaluation of radiolabeled human-lymphocyte immune functions.

    abstract::Technetium-99m-modified polylysine (MPL) is a mild and efficient method for cell labeling that is easily applicable to human lymphocytes. 99mTc-MPL uptake is maximal in 40 min at room temperature. Cell labeling efficiency (from 60 to 80%) increases with rising concentrations of cells and labeling agent. In vitro stabi...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/0969-8051(95)02011-x

    authors: Delmon-Moingeon LI,Mahmood A,Davison A,Jones AG

    更新日期:1996-01-01 00:00:00

  • Optimization, biological evaluation and microPET imaging of copper-64-labeled bombesin agonists, [64Cu-NO2A-(X)-BBN(7-14)NH2], in a prostate tumor xenografted mouse model.

    abstract:UNLABELLED:Gastrin-releasing peptide receptors (GRPr) are a member of the bombesin (BBN) receptor family. GRPr are expressed in high numbers on specific human cancers, including human prostate cancer. Therefore, copper-64 ((64)Cu) radiolabeled BBN(7-14)NH(2) conjugates could have potential for diagnosis of human prosta...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2010.04.016

    authors: Lane SR,Nanda P,Rold TL,Sieckman GL,Figueroa SD,Hoffman TJ,Jurisson SS,Smith CJ

    更新日期:2010-10-01 00:00:00

  • Binding properties of the cerebral alpha4beta2 nicotinic acetylcholine receptor ligand 2-[18F]fluoro-A-85380 to plasma proteins.

    abstract:INTRODUCTION:To determine the availability of nicotinic acetylcholine receptors in different human brain regions using the positron emission tomography (PET) radioligand 2-[18F]fluoro-A-85380 (2-[18F]FA) and invasive approaches for quantification, it is important to correct the arterial input function as well for plasm...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2006.07.012

    authors: Sorger D,Becker GA,Hauber K,Schildan A,Patt M,Birkenmeier G,Otto A,Meyer P,Kluge M,Schliebs R,Sabri O

    更新日期:2006-10-01 00:00:00

  • Synthesis of [18F]RGD-K5 by catalyzed [3 + 2] cycloaddition for imaging integrin αvβ3 expression in vivo.

    abstract::In the last few years click chemistry reactions, and in particular copper-catalyzed cycloadditions have been used extensively for the preparation of new bioconjugated molecules such as (18)F-radiolabeled radiopharmaceuticals for positron emission tomography (PET). This study is focused on the synthesis of the Siemens ...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2013.04.003

    authors: Mirfeizi L,Walsh J,Kolb H,Campbell-Verduyn L,Dierckx RA,Feringa BL,Elsinga PH,de Groot T,Sannen I,Bormans G,Celen S

    更新日期:2013-07-01 00:00:00

  • Measuring tumor blood flow with H(2)(15)O: practical considerations.

    abstract::The ability to measure blood flow to tumors non-invasively may be of importance in monitoring tumor therapies, assessing drug delivery, and understanding tumor physiology. Of all the radiotracer methods that have been proposed to measure tumor blood flow, the method based on labeled water-H(2)(15)O-may be the most app...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章,评审

    doi:10.1016/s0969-8051(00)00136-0

    authors: Bacharach SL,Libutti SK,Carrasquillo JA

    更新日期:2000-10-01 00:00:00

  • Radiosynthesis and biological evaluation of alpha-[F-18]fluoromethyl phenylalanine for brain tumor imaging.

    abstract:OBJECTIVES:Radiolabeled amino acids have proven utility for imaging brain tumors in humans, particularly those that target system L amino acid transport. We have prepared the novel phenylalanine analogue, (FMePhe, 9), as part of an effort to develop new system L tracers that can be prepared in high radiochemical yield ...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2012.12.013

    authors: Huang C,Yuan L,Rich KM,McConathy J

    更新日期:2013-05-01 00:00:00

  • Radiolabelling and evaluation of a novel sulfoxide as a PET imaging agent for tumor hypoxia.

    abstract::[¹⁸F]FMISO is the most widely validated PET radiotracer for imaging hypoxic tissue. However, as a result of the pharmacokinetics of [¹⁸F]FMISO a 2h wait between tracer administration and patient scanning is required for optimal image acquisition. In order to develop hypoxia imaging agents with faster kinetics, we have...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2014.03.001

    authors: Laurens E,Yeoh SD,Rigopoulos A,Cao D,Cartwright GA,O'Keefe GJ,Tochon-Danguy HJ,White JM,Scott AM,Ackermann U

    更新日期:2014-05-01 00:00:00

  • Kinetic parameters of 3-[(123)I]iodo-L-alpha-methyl tyrosine ([(123)I]IMT) transport in human GOS3 glioma cells.

    abstract::The radiolabelled amino acid 3-[(123)I]iodo-L-alpha-methyl tyrosine ([(123)I]IMT) is a promising tool for the diagnosis and monitoring of brain tumors using single-photon emission tomography (SPECT). However, little is known about the precise kinetics of [(123)I]IMT uptake in human glioma cells. The kinetic analysis o...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/s0969-8051(01)00191-3

    authors: Riemann B,Kopka K,Stögbauer F,Halfter H,Ketteler S,Phan TQ,Franzius C,Weckesser M,Ringelstein EB,Schober O

    更新日期:2001-04-01 00:00:00

  • Fluorine-18-labeled fluorine gas for synthesis of tracer molecules.

    abstract::The aim of this work was to develop a method to produce 18F-labeled fluorine gas ([18F]F2) with high specific radioactivity (SA, radioactivity/mass-ratio). 18F-Labeled methyl fluoride ([18F]CH3F) was synthesized from [18F]F-aq and mixed with carrier F2 in an inert neon matrix. The constituents were atomized in an elec...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/s0969-8051(97)00078-4

    authors: Bergman J,Solin O

    更新日期:1997-10-01 00:00:00

  • Labeling and preliminary in vivo assessment of niobium-labeled radioactive species: A proof-of-concept study.

    abstract::The application of radionuclide-labeled biomolecules such as monoclonal antibodies or antibody fragments for imaging purposes is called immunoscintigraphy. More specifically, when the nuclides used are positron emitters, such as zirconium-89, the technique is referred to as immuno-PET. Currently, there is an urgent ne...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2016.02.003

    authors: Radchenko V,Bouziotis P,Tsotakos T,Paravatou-Petsotas M,la Fuente Ad,Loudos G,Harris AL,Xanthopoulos S,Filosofov D,Hauser H,Eisenhut M,Ponsard B,Roesch F

    更新日期:2016-05-01 00:00:00