Abstract:
OBJECTIVE:Pretargeting is the concept that combines optimal delivery of the antibody and rapid capture and elimination of the radioactivity. In this study, we evaluated the potential of antibody pretargeting to enable the tumor-targeting (212)Pb for in vivo generation of (212)Bi for alpha particle radiotherapy. METHODS:The (212)Pb/(212)Bi chelate of DOTA-biotin, as well as their gamma-emitting analogues, (203)Pb and (205)Bi, was prepared and characterized. The radiolabeled compounds were injected in animals for evaluation of tumor targeting and normal tissue uptake and retention. In the pretargeting protocol, injection of 400 microg of NR-LU-10 antibody-streptavidin conjugate was given at t = 0 h, then 100 microg of N-acetyl-galatosamine-biotin clearing agent was injected at t = 20-24 h; finally, 1 microg of (212)Pb/(212)Bi-DOTA-biotin was injected 6 h later. RESULTS:Both (203)Pb and (205)Bi-DOTA-biotin were stable for at least 4 days in the different challenging solutions including PBS, 10 mM DTPA and serum. Contrary to its gamma-emitting analogues, radiolabeled (212)Pb-DOTA-biotin was not stable. There was greater than 30% of free (212)Bi released 4 h after (212)Pb-labeled DOTA-biotin. The results of pretargeting protocol of (203)Pb and (205)Bi-DOTA-biotin showed that the tumor target reached 20% injected dose (ID)/g at 4 h postinjection and remained high for 5 days. The %ID/g in the whole blood and other nontarget organs was low after administration of labeled (203)Pb and (205)Bi-DOTA-biotin similar to the biodistribution of labeled DOTA-biotin alone. In the animals administered (212)Pb-DOTA-biotin, radioactivity in nontarget organs was low except the kidneys. The %ID/g in the kidney for (212)Bi was 14.5 at 2 h, higher than (212)Pb, but dropped to about 6% ID/g by 4 h. However, tumor uptake for (212)Pb and (212)Bi was >25% ID/g at 1 h postinjection and remained so through 24 h. CONCLUSIONS:Antibody pretargeting system with Mab-streptavidin, clearing agent and DOTA-biotin provides the potential of (212)Bi for solid tumor radiotherapy despite the release of (212)Bi after (212)Pb decay. Dosimetry calculations resulted in tumor dose at 93 rad/muCi and ratios of tumor to marrow and kidney at 386:1 and 12:1, respectively.
journal_name
Nucl Med Bioljournal_title
Nuclear medicine and biologyauthors
Su FM,Beaumier P,Axworthy D,Atcher R,Fritzberg Adoi
10.1016/j.nucmedbio.2005.06.009keywords:
subject
Has Abstractpub_date
2005-10-01 00:00:00pages
741-7issue
7eissn
0969-8051issn
1872-9614pii
S0969-8051(05)00188-5journal_volume
32pub_type
杂志文章abstract::The hepatic and renal retention of indium-111 (111In) from 111In-labeled polypeptides has been the subject of many investigations. Because the lysosome is a common intracellular destination for the degradation of polypeptides, we studied the lysosomal metabolism of 111In-DTPA-labeled glycoproteins targeted to cell sur...
journal_title:Nuclear medicine and biology
pub_type: 杂志文章
doi:10.1016/0969-8051(94)90174-0
更新日期:1994-11-01 00:00:00
abstract::[11C]Methamphetamine, a psychotropic agent, was synthesized by N-methylation of amphetamine with [11C]CH3 I in hopes that it could be applied in the near future to assist positron emission tomography (PET) in the imaging of its distribution in the human brain. The regional distribution of [11C]methamphetamine was inve...
journal_title:Nuclear medicine and biology
pub_type: 杂志文章
doi:10.1016/0969-8051(93)90080-e
更新日期:1993-05-01 00:00:00
abstract::The advent of antibody-based cancer therapeutics has led to the concomitant rise in the development of companion diagnostics for these therapies, particularly nuclear imaging agents. A number of radioisotopes have been employed for antibody-based PET and SPECT imaging, notably ⁶⁴Cu, ¹²⁴I, ¹¹¹In, and (99m)Tc; in recent...
journal_title:Nuclear medicine and biology
pub_type: 杂志文章,评审
doi:10.1016/j.nucmedbio.2012.08.004
更新日期:2013-01-01 00:00:00
abstract::We have synthesized N-(6-18F-fluorohexyl)-N-methylpropargylamine (18F-FHMP) as a positron emission tomography (PET) radiotracer for monoamine oxidase B (MAO-B). The radiosynthesis was carried out by a fluorine-for-bromine substitution in 30-40% radiochemical yield in specific activities of 1-2 Ci/micromol. Selectivity...
journal_title:Nuclear medicine and biology
pub_type: 杂志文章
doi:10.1016/s0969-8051(98)00061-4
更新日期:1999-01-01 00:00:00
abstract:INTRODUCTION:The pyruvaldehyde bis(N(4)-methylthiosemicarbazonato)copper(II) (Cu-PTSM) and diacetyl bis(N(4)-methylthiosemicarbazonato)copper(II) (Cu-ATSM) radiopharmaceuticals exhibit strong, species-dependent binding to the IIA site of human serum albumin (HSA), while the related ethylglyoxal bis(thiosemicarbazonato)...
journal_title:Nuclear medicine and biology
pub_type: 杂志文章
doi:10.1016/j.nucmedbio.2009.02.006
更新日期:2009-07-01 00:00:00
abstract:INTRODUCTION:The α(V)β(3) integrin is a well-known transmembrane receptor involved in tumor invasion, angiogenesis and metastasis. Our aim was to evaluate a novel positron emission tomography (PET) probe, (64)Cu-cyclam-RAFT-c(-RGDfK-)(4), for noninvasive visualization and quantification of α(V)β(3) integrin expression....
journal_title:Nuclear medicine and biology
pub_type: 杂志文章
doi:10.1016/j.nucmedbio.2010.11.008
更新日期:2011-05-01 00:00:00
abstract::The in vitro stability and animal pharmacokinetics of 99mTc bound to Sandoz and C110 IgG antibodies via a modified MAG3 has been compared with the hydrazino nicotinamide (SHNH) moiety as standard. For both antibodies, the stabilities of the label to challenge at up to 50:1 cysteine: IgG molar ratio were comparable, bu...
journal_title:Nuclear medicine and biology
pub_type: 杂志文章
doi:10.1016/s0969-8051(96)00131-x
更新日期:1996-10-01 00:00:00
abstract:INTRODUCTION:Tetradentate acyclic and macrocyclic diphosphine ligands (P(2)N(2) and P(2)S(2)) have been synthesized and characterized as potential chelates for Rh(III). METHODS:The coordination complexes [RhCl(2)(L1)]Cl, trans-[RhCl(2)(L2)]PF(6), [Ni(L2)](PF(6))(2), [Ni(L3)](PF(6))(2), [RhCl(2)(L4)]PF(6) and [RhCl(2)(...
journal_title:Nuclear medicine and biology
pub_type: 杂志文章
doi:10.1016/j.nucmedbio.2010.06.013
更新日期:2011-01-01 00:00:00
abstract:OBJECTIVES:To evaluate the effectiveness of PET in differentiating malignant from benign pancreatic cystic tumors. METHODS:Between 2009 and 2010, all patients with pancreatic cystic tumors who had PET, triple phase contrast computed tomography (CT) and endoscopic ultrasound (EUS) were reviewed. Clinicopathological cha...
journal_title:Nuclear medicine and biology
pub_type: 杂志文章
doi:10.1016/j.nucmedbio.2012.03.005
更新日期:2012-10-01 00:00:00
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
更新日期:2005-10-01 00:00:00
abstract:OBJECTIVES:Positron emission tomography (PET) using O-(2-[(18)F]fluoroethyl)-l-tyrosine (FET) has been successfully employed in the diagnostic workup of brain tumors. Knowledge on the mechanisms of the uptake of radiolabeled amino acids into thyroidal tissues and well-differentiated thyroid carcinomas is limited. We th...
journal_title:Nuclear medicine and biology
pub_type: 杂志文章
doi:10.1016/j.nucmedbio.2006.12.007
更新日期:2007-04-01 00:00:00
abstract:INTRODUCTION:Ultrasound (US) contrast agents based on microbubbles (MBs) are being investigated as platforms for drug and gene delivery. A methodology for determining the distribution and fate of modified MBs quantitatively in vivo can be achieved by tagging MBs directly with (99m)Tc. This creates the opportunity to em...
journal_title:Nuclear medicine and biology
pub_type: 杂志文章
doi:10.1016/j.nucmedbio.2011.04.008
更新日期:2011-11-01 00:00:00
abstract::Quantitative imaging of glucose metabolism of human brain tumors with PET utilizes 2-[(18)F]-fluorodeoxy-D-glucose (FDG) and a conversion factor called the lumped constant (LC), which relates the metabolic rate of FDG to glucose. Since tumors have greater uptake of FDG than would be predicted by the metabolism of nati...
journal_title:Nuclear medicine and biology
pub_type: 杂志文章
doi:10.1016/s0969-8051(00)00201-8
更新日期:2001-02-01 00:00:00
abstract::We present a method for estimating 99mTc-MAG3 clearance from both a single injection and two blood samples that is valid for both adults and children. It was obtained by fitting a scaled two-compartment model (having only two adjustable parameters) to adult and pediatric data from multiple centers. ...
journal_title:Nuclear medicine and biology
pub_type: 杂志文章
doi:10.1016/0969-8051(94)00076-v
更新日期:1995-01-01 00:00:00
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
更新日期:2009-10-01 00:00:00
abstract:INTRODUCTION:Sepantronium bromide (YM155) is an antitumor drug in development and is a first-in-class chemical entity, which is a survivin suppressant. We developed a radiosynthesis of [(11)C]YM155 to non-invasively evaluate its tissue and tumor distribution in mice bearing human prostate tumor xenografts. METHODS:Met...
journal_title:Nuclear medicine and biology
pub_type: 杂志文章
doi:10.1016/j.nucmedbio.2012.10.002
更新日期:2013-02-01 00:00:00
abstract:INTRODUCTION:Several 11C and 18F labeled 3,4-dihydroxy-l-phenylalanine (l-DOPA) analogues have been used for neurologic and oncologic diseases, especially for brain tumors and neuroendocrine tumors PET imaging. However, 18F-labeled N-substituted l-DOPA analogues have not been reported so far. In the current study, radi...
journal_title:Nuclear medicine and biology
pub_type: 杂志文章
doi:10.1016/j.nucmedbio.2017.04.002
更新日期:2017-07-01 00:00:00
abstract:INTRODUCTION:Telmisartan, a nonpeptide angiotensin II AT1 receptor antagonist used as an antihypertensive drug, is specifically taken up by the liver through the OATP1B3. PET imaging with [(11)C]telmisartan is expected to provide information about the whole body pharmacokinetics of telmisartan as well as its transport ...
journal_title:Nuclear medicine and biology
pub_type: 临床试验,杂志文章
doi:10.1016/j.nucmedbio.2012.01.008
更新日期:2012-08-01 00:00:00
abstract::6-Hydrazinopyridine-3-carboxylic acid (HYNIC) is a representative agent used to prepare technetium-99m ((99m)Tc)-labeled polypeptides with tricine as a coligand. However, (99m)Tc-HYNIC-labeled polypeptides show delayed elimination rates of the radioactivity not only from the blood but also from nontarget tissues such ...
journal_title:Nuclear medicine and biology
pub_type: 杂志文章
doi:10.1016/s0969-8051(00)00210-9
更新日期:2001-04-01 00:00:00
abstract::Antimicrobial peptides have been proposed as new agents to distinguish between bacterial infections and sterile inflammatory processes. (99m)Tc-UBI labeled by a direct method has shown high in vitro and in vivo stability, specific uptake at the site of infection, rapid background clearance, minimal accumulation in non...
journal_title:Nuclear medicine and biology
pub_type: 临床试验,杂志文章
doi:10.1016/j.nucmedbio.2003.10.005
更新日期:2004-04-01 00:00:00
abstract::Radiolabeled derivatives of WAY-100635 have been shown to be important for imaging in vivo because of their antagonist properties and their specificity for the 5-hydroxytryptamine(1A) (5-HT(1A)) receptor. Our goal is to prepare a series of radiofluorinated derivatives of WAY-100635 that, in the rat, range in pharmacok...
journal_title:Nuclear medicine and biology
pub_type: 杂志文章,评审
doi:10.1016/s0969-8051(00)00111-6
更新日期:2000-07-01 00:00:00
abstract::In developing radioiodinated agents for pancreatic and brain tumor imaging by single photon emission tomography (SPET), we prepared p-amino-3-[123I]iodo-l-phenylalanine (IAPA), p-[123I]iodo-l-phenylalanine (IPA), L-8-[123I]iodo-1,2,3,4-tetrahydro-7-hydroxyisoquinoline-3-carboxylic acid (ITIC) and L-3-[123I]iodo-alpha-...
journal_title:Nuclear medicine and biology
pub_type: 杂志文章
doi:10.1016/s0969-8051(00)00176-1
更新日期:2001-01-01 00:00:00
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
更新日期:1996-01-01 00:00:00
abstract::To improve standardization in analytical reagents we investigated Chloramine-T radioiodination (125I) of several biomolecules based on the use of a single amount of the oxidizing agent Chloramine-T as the limiting reagent being exhausted during the course of the reaction. Whenever the labeling yield resulted in less t...
journal_title:Nuclear medicine and biology
pub_type: 杂志文章
doi:10.1016/s0969-8051(01)00261-x
更新日期:2001-11-01 00:00:00
abstract:INTRODUCTION:Targeted α-radionuclide therapy has attracted attention as a promising therapy for refractory cancers. However, the application is limited to certain types of cancer. Since L-type amino acid transporter 1 (LAT1) is highly expressed in various human cancers, we prepared an LAT1-selective α-radionuclide-labe...
journal_title:Nuclear medicine and biology
pub_type: 杂志文章
doi:10.1016/j.nucmedbio.2020.08.003
更新日期:2020-01-01 00:00:00
abstract::The imaging of the distribution of beta-amyloid (Abeta) plaques in the brain is becoming an important diagnostic modality in Alzheimer's disease (AD). Here, we synthesized novel benzothiophene derivatives and labeled them with (18)F for the potential diagnostic imaging of AD patients using positron emission tomography...
journal_title:Nuclear medicine and biology
pub_type: 杂志文章
doi:10.1016/j.nucmedbio.2006.06.006
更新日期:2006-08-01 00:00:00
abstract::Two photolabile heterobifunctional O-nitrobenzyl reagents were used to modify B72.3 monoclonal antibody followed by immobilization on a solid support. Antibody was labeled with 99mTc and then cleaved from the resin on irradiation with light of peak intensity at 365 nm. The antibody was restored unmodified after cleava...
journal_title:Nuclear medicine and biology
pub_type: 杂志文章
doi:10.1016/0969-8051(94)00147-c
更新日期:1995-07-01 00:00:00
abstract::L-2,4-Diamino[4-11C]butyric acid (DAB) was synthesized by an enzyme catalysed carrier added (0.1 micromol KCN) reaction of hydrogen [11C]cyanide with O-acetyl-L-serine followed by reduction. L-[11C]DAB was obtained with a radiochemical purity higher than 96% and with a decay corrected radiochemical yield of 30-40% wit...
journal_title:Nuclear medicine and biology
pub_type: 杂志文章
doi:10.1016/s0969-8051(97)00032-2
更新日期:1997-08-01 00:00:00
abstract:INTRODUCTION:Thermal neutron activation of 152Sm [152Sm(n,γ)153Sm] using natural or isotopically enriched (by 152Sm) samarium target is the established route for production of 153Sm used for preparation of 153Sm-EDTMP for pain palliation in cancer patients with disseminated bone metastases. However, some long-lived rad...
journal_title:Nuclear medicine and biology
pub_type: 杂志文章
doi:10.1016/j.nucmedbio.2017.11.010
更新日期:2018-03-01 00:00:00
abstract::Dithiocarboxylate ligands were synthesized and characterised. New nitrido 99m-technetium complexes were obtained with these ligands and identified by thin layer chromatography. The nitrido complexes were tested in vitro in whole blood for leucocyte labelling and the design of the ligand was optimized. Best results wer...
journal_title:Nuclear medicine and biology
pub_type: 杂志文章
doi:10.1016/s0969-8051(97)00025-5
更新日期:1997-07-01 00:00:00