<Superscript>99m</Superscript>Tc-tetrofosmin or <Superscript>99m</Superscript>Tc-sestamibi for double-phase parathyroid scintigraphy?

Several years ago technetium-99m tetrofosmin was reported to localise parathyroid adenomas. The aim of this study was to compare the sensitivity of this radiopharmaceutical with that of (99m)Tc-sestamibi using a double-phase parathyroid scintigraphy protocol. Scans of 12 patients were evaluated visually and lesion to thyroid ratios were calculated. Nine of the patients were subsequently operated on; a total of eight parathyroid adenomas or hyperplastic glands were histologically confirmed in seven of the patients, while in one patient a parathyroid carcinoma was histologically proven. All of these patients had positive (99m)Tc-sestamibi scintigrams, whereas only two (99m)Tc-tetrofosmin scintigrams were positive. With (99m)Tc-sestamibi there was a significant increase in the lesion to thyroid ratio from 10 min to 90 min and 150 min p.i. which was not seen on scintigraphy with (99m)Tc-tetrofosmin. This makes (99m)Tc-tetrofosmin less suitable for double-phase parathyroid scintigraphy.     

Dopamine transporter SPECT using fast kinetic ligands: <Superscript>123</Superscript>I-FP-β-CIT versus <Superscript>99m</Superscript>Tc-TRODAT-1

A comparative study was carried out on two promising presynaptic dopamine transporter single-photon emission tomography (SPECT) radioligands with a fast pharmacokinetic profile, ¹²³I-FP--CIT (FP) and ^99mTc-TRODAT-1 (TR), in order to assess their differential diagnostic power in early parkinsonism and their sensitivity for detection of disease progression. This cross-sectional study was conducted on 96 patients with early-stage parkinsonism referred in a tertiary clinical setting. Mean disease duration was 2.0±1.3 years, and patients had a modified Hoehn and Yahr (H&Y) stage of 1–2 (average 1.2). Forty-seven patients received TR, and 49 received FP. In both groups, ten patients with normal presynaptic function were included as a control population; all other patients were clinically diagnosed as having idiopathic Parkinsons disease. Groups were matched for gender, age, disease duration and modified H&Y stage. Triple-head gamma camera SPECT was analysed using a semiquantitative index of transporter binding (BI). Discriminant analysis with cross-validation resulted in a maximal classification accuracy for FP of 93% (sensitivity 95% and specificity 86%) for the contralateral putamen BI. For TR, the corresponding values were 87% accuracy, 92% sensitivity and 70% specificity. For FP, disease duration was correlated with both the putamen BI (–8.8%/year, =–0.41, P=0.025) and the putamen/caudate ratio (–7.4%/year, =–0.51, P=0.004), but for TR no significant correlation was found (all P values >0.5). In conclusion, both FP and TR show high sensitivity in a clinically relevant setting, but FP has superior accuracy for early differential diagnosis of idiopathic parkinsonism and non-degenerative extrapyramidal disorders, as well as better sensitivity for disease follow-up.     

Could <Superscript>99m</Superscript>Tc-glucarate be used to evaluate tumour necrosis?

PURPOSE: The aim of this study was to determine whether (99m)Tc-glucarate ((99m)Tc-GLA) is a powerful and discriminant tumour necrosis marker. MATERIALS AND METHODS: The induction of apoptosis and secondary necrosis (by a chemotherapeutic agent) and necrosis (by intense hyperthermia) was studied on an in vitro and in vivo leukaemic cell line model (U937). The percentage of apoptosis/necrosis in vitro was determined by flow cytometry after staining cells with annexin-V-fluorescein/propidium iodide. The uptake of (99m)Tc-GLA was studied after treatments that produce an optimal of necrosis cells or apoptotic cells. Three populations of interest: viable, apoptotic and necrotic cells were sorted by flow cytometry. The uptake and the intracellular distribution of (99m)Tc-GLA on each population have been studied. We also investigated the influence of necrosis on (99m)Tc-GLA uptake in a model of U937 xenografts in nude mice. RESULTS: The accumulation of (99m)Tc-GLA in untreated and apoptotic cells was lower than in necrotic cells. Cell sorting discriminated each cellular population and showed a 14% accumulation in necrotic cells and no more than a 3% in apoptotic cells. In apoptotic and viable cells, (99m)Tc-GLA is distributed between the cytosolic/membrane and the nucleus fractions. In necrotic cells, (99m)Tc-GLA is mainly found in the nucleus fraction. In vivo investigations showed a higher (99m)Tc-GLA uptake in necrotic tumour than in apoptotic and control ones. CONCLUSIONS: (99m)Tc-GLA may be a useful agent to specifically evaluate tumour necrosis and may be helpful for the follow-up of patients with cancer.     

Comparison of <Superscript>99m</Superscript>Tc-annexin A5 with <Superscript>18</Superscript>F-FDG for the detection of atherosclerosis in ApoE−/− mice

Purpose ^99mTc-annexin A5, a marker of ongoing apoptosis, and ¹⁸F-FDG, a marker of the increased metabolism of inflammatory cells, are supposed to be useful in the detection of metabolically active atheroma. This study reports a comparison of the intralesional distribution of these tracers in relation to lesion development in ApoE−/− mice. Methods Male ApoE−/− mice (n = 12–14/group) were maintained on a Western-type diet after the age of 5 weeks. At 25 weeks, ^99mTc-annexin A5 or ¹⁸F-FDG was injected and the aortas were harvested for autoradiography (ARG) and Oil Red O staining. Regional radioactivity accumulation was compared in relation to the Oil Red O staining score (ranging from 0 to 3, a semiquantitative parameter for evaluating lesion development). Results Both ^99mTc-annexin A5 and ¹⁸F-FDG showed preferential uptake into atherosclerotic lesions, with higher uptake levels for ¹⁸F-FDG (mean, 56.07 %ID×kg/m²) than for ^99mTc-annexin A5 (mean, 10.38 %ID×kg/m²). The regional uptake levels of each tracer correlated with the Oil Red O staining score (r = 0.65, p < 0.05 for ^99mTc-annexin A5; r = 0.56, p < 0.05 for ¹⁸F-FDG). The uptake ratios of advanced lesions (score >0.5) to early lesions (score <0.5) were significantly higher for ^99mTc-annexin A5 than for ¹⁸F-FDG (f = 4.73, p = 0.03). Conclusion Both ^99mTc-annexin A5 and ¹⁸F-FDG accumulate in atherosclerotic lesions and correlate with the severity of each lesion. The higher absolute uptake levels of ¹⁸F-FDG may be advantageous for lesion detection, whereas the preferential uptake of ^99mTc-annexin A5 in advanced lesions may be a useful indicator of late-stage lesions or vulnerable plaque transformation.     

The clinical utility of 99<Superscript>m</Superscript>Tc-HMPAO SPECT in Fahr’s disease

Fahr's disease is a rare neurodegenerative syndrome, characterized by massive symmetrical intracerebral calcifications of the basal ganglia, dentate nuclei of the cerebellum, and the adjacent parenchyma. Computerized tomography (CT) is considerably more sensitive to detect these intracranial calcifications than other imaging modalities. The clinical, CT scan, and 99(m)Tc-D,L-hexamethylpropylene amine oxime (99(m)Tc-HMPAO) brain perfusion single-photon emission computerized tomography (SPECT) findings in a 42-year-old woman with Fahr's disease are reported, and the clinical utility of 99(m)Tc-HMPAO SPECT findings in Fahr's disease is discussed in this article. In conclusion, 99(m)Tc-HMPAO brain perfusion SPECT seems to be useful in the clinical approach to Fahr's disease, and may provide more specific and clinically relevant information when compared with anatomical imaging.     

Diagnosis and staging of children’s lymphoma using the technetium-labelled somatostatin analogue, <Superscript>99m</Superscript>Tc-depreotide

Somatostatin receptor scintigraphy (SRS) is useful in diagnosing tumours with increased expression of somatostatin receptors. Lymphoma cells are known to express somatostatin receptors; however, the application of indium-labelled analogues in children is limited. The aim of this study was to investigate whether the technetium-labelled somatostatin analogue, depreotide, may be useful in diagnosing and staging malignant lymphoma in children. Fifteen children (mean age 13.8 years) with malignant lymphoma were studied (eight with Hodgkins lymphoma and seven with non-Hodgkins lymphoma). All children were investigated for verification of staging established by other modalities. Imaging was performed 3–5 h after administration of 300–550 MBq ^99mTc-depreotide. All patients underwent whole-body scan and single-photon emission tomography of the chest and/or abdomen. Images were assessed visually. In all patients, foci of increased tracer uptake were found. The neck and thorax were the most frequent lesion localisations. Abdominal lesions were found in four patients, and bone lesions in three. In two patients, diffusely increased uptake was observed throughout the skeleton (verified as representing bone marrow involvement). In 11 patients, the number of abnormal sites detected by SRS was greater than that detected by CT. Based on radionuclide examination, three children were upstaged and none were downstaged. It is concluded that ^99mTc-depreotide shows increased accumulation in pathological sites in malignant lymphoma in children. SRS with ^99mTc-depreotide provides a single-day imaging method with high sensitivity in lymphoma and with all the advantages of a technetium-labelled compound. Further studies are required on the specificity and the possible value of ^99mTc-depreotide in the follow-up of these patients.     

In vivo imaging of tumour angiogenesis in mice with the α<Subscript>v</Subscript>β<Subscript>3</Subscript> integrin-targeted tracer <Superscript>99m</Superscript>Tc-RAFT-RGD

Purpose The molecular imaging of tumour neoangiogenesis currently represents a major field of research for the diagnostic and treatment strategy of solid tumours. Endothelial cells from tumour neovessels overexpress the α_vβ₃ integrin, which selectively binds to Arg-Gly-Asp (RGD)-containing peptides. We evaluated the potential of the novel radiotracer ^99mTc-RAFT-RGD for the non-invasive molecular imaging of α_vβ₃ integrin expression in mice models of tumour development. Methods ^99mTc-RAFT-RGD, ^99mTc-cRGD (specific control) and ^99mTc-RAFT-RAD (non-specific control) were injected intravenously to mice bearing B16F0 or TS/A-pc tumours. In vivo whole-body tomographic imaging and post-mortem biodistribution studies were performed 60 min following tracer injection. Adjacent tumour slices were used to compare the localisation of neovessels from immunostaining and the pattern of ^99mTc-RAFT-RGD uptake from autoradiographic ex vivo imaging. Results Biodistribution studies indicated that ^99mTc-RAFT-RGD tumour uptake was significantly higher than that of ^99mTc-RAFT-RAD in B16F0 (2.4±0.5 vs 1.0±0.1%ID/g, respectively) and in TS/A-pc tumours (2.7±0.8 vs 0.7±0.1%ID/g, respectively). Immunohistochemical and autoradiographic studies indicated that ^99mTc-RAFT-RGD intratumoural uptake preferentially occurred in angiogenic areas. Tomographic imaging allowed tumour visualisation following injection of ^99mTc-RAFT-RGD and ^99mTc-cRGD with similar tumour-to-contralateral muscle (T/CM) ratios in B16F0 and in TS/A-pc tumours whereas ^99mTc-RAFT-RAD T/CM ratios did not allow tumour imaging. In accordance with the higher level of α_vβ₃ integrin expression on TS/A-pc tumours than on B16F0 tumours as determined from western blot and immunoprecipitation analyses, the ^99mTc-RAFT-RGD T/CM ratio was significantly higher in TS/A-pc than in B16F0 tumours. Conclusion ^99mTc-RAFT-RGD allowed the in vivo imaging of α_vβ₃ integrin tumour expression.     

Usefulness of brain <Superscript>99m</Superscript>Tc-TRODAT-1 SPET for the evaluation of Parkinson’s disease

Nigral dopaminergic projections to the striatum are targeted in Parkinsons disease (PD). The extent of the degeneration of the dopaminergic system in PD can be visualised by dopamine transporter imaging using single-photon emission tomography (SPET). In this study in 188 patients with PD, we analysed the image patterns and compared them with the clinical features in order to verify the usefulness of technetium-99m TRODAT-1 brain SPET in the evaluation of patients with PD. Two independent readers visually assessed SPET slices from three brain axes according to a fine visual scale; results were also grouped according to a rough visual scale. Results of both visual and semi-quantitative analyses were compared among patients with different stages of PD and healthy controls. There was good agreement between the readers in the interpretation of the image patterns [kappa statistic ()=0.85 for the presence of PD; =0.88 for the rough scale and 0.81 for the fine scale]. Good concordance was obtained when visual interpretation was used to evaluate the presence of PD (sensitivity =98%, specificity =86%, =0.85). Semi-quantitative analyses revealed significant negative correlations between both striatal and putaminal uptake and disease severity as assessed using the Hoehn and Yahr scale (=–0.89 and –0.93 respectively). An apparent decrease in striatal uptake in early PD, hardly discernible from the uptake level in advanced PD, was commonly found in visual analyses. The results suggest that both visual and semi-quantitative analyses of ^99mTc-TRODAT-1 SPET images reflect neurodegeneration in PD, and that ^99mTc-TRODAT-1 SPET represents an adequate means for evaluation of the status of patients with PD.     

Do androgens control the uptake of <Superscript>18</Superscript>F-FDG, <Superscript>11</Superscript>C-choline and <Superscript>11</Superscript>C-acetate in human prostate cancer cell lines?

Purpose  

The aim of this study was to evaluate the impact of androgen ablation therapy in different prostate cancer (PCa) cell lines—reflecting different stages of the disease—on ¹⁸F-fluorodeoxyglucose (FDG), ¹¹C-choline and ¹¹C-acetate uptake.     

Comparison of <Superscript>99m</Superscript>Tc-labeled PR81 and its F(ab′)<Subscript>2</Subscript> fragments as radioimmunoscintigraphy agents for breast cancer imaging

Objective  

We digested anti-MUC1 monoclonal antibody PR81 to produce F(ab′)₂ fragments. A comparison was performed between the two radiolabeled PR81 and F(ab′)₂ fragments for breast tumor imaging in a mouse model.     

Development of “super rapid dynamic SPECT,” and analysis of retention process of<Superscript>99m</Superscript>Tc-ECD in ischemie lesions: Comparative study with<Superscript>133</Superscript>Xe SPECT

To analyze the retention process of technetium-99m ethyl cysteinate dimer (99mTc-ECD) in normal and ischemic lesions, we developed a super rapid dynamic SPECT system based on the CERASPECT (DSI, Inc., Waltham, MA, USA). The system made it possible to take a SPECT series every 2 seconds. Each SPECT series contains a maximum of 16 slices (6.6 mm slice interval) in a matrix size of 32 x 32. The sensitivity of this system is 175 kcps/MBq/ml/cm slice thickness, and resolution is 12 mm FWHM at the center of a 20 cm(phi) water phantom. Using the super rapid SPECT system, the kinetic behavior of the 99mTc-ECD during retention in normal and ischemic lesions was analyzed. Twenty patients with ischemic lesions that were clearly demonstrated by 133Xe-rCBF (regional cerebral blood flow) SPECT but unclear on static 99mTc-ECD SPECT were examined. For the dynamic SPECT, 700 MBq of 99mTc-ECD was injected intravenously, and dynamic SPECT data were acquired every 2 seconds during a 90-second period. The serial dynamic SPECT and time-activity curves at some lesions with reduced rCBF and at the contralateral normal brain were analyzed. These dynamic SPECT data were compared with conventional static 99mTc-ECD SPECT and quantitative 133Xe-rCBF SPECT. All of mildly or moderately reduced rCBF lesions on the 133Xe-rCBF SPECT were recognized as low activity regions only at the early phase (during about 2-20 sec or less), with the lesions then gradually vanishing. These lesions were not recognized on the conventional static SPECT taken after the dynamic study. The time-activity curve at the reduced rCBF lesion was lower than that of contralateral normal brain at the early phase, and overtook the activity in the normal region with a gradual increase. The early phase images of 99mTc-ECD SPECT within 20 seconds by the super rapid dynamic SPECT were very useful to the same extent as the 133Xe-rCBF SPECT for detecting mild or moderate ischemic lesions. This study suggests that esterase activity, participating in the ECD retention mechanism, may be tolerable to mild or moderate ischemia. This tolerance may be the main cause of the nonlinear relationship between ECD accumulation and cerebral blood flow.     

Assessment of alveolar epithelial permeability in Behçet’s disease with <Superscript>99m</Superscript>Tc-DTPA aerosol scintigraphy

Objective

Behçet’s disease (BD) is a multisystem disorder characterized by vasculitis, and consists of a triad of recurrent ulcers of the oral and genital mucosa with relapsing uveitis. The prevalance of pulmonary involvement varies in the range of 1–10% in various studies and its complications are severe and life threatening. In this study, we investigated the changes of pulmonary epithelial permeability of patients with BD using technetium-99m diethylene triamine penta-acetic acid (^99mTc-DTPA) aerosol scintigraphy, so as to begin the therapy regimen as soon as possible.

Methods

Twenty-one nonsmoking patients with BD (8 women, 13 men; mean age 38.67 ± 8.86 years) and 15 healthy volunteer nonsmoking controls (8 women, 7 men; mean age 50.87 ± 12.45 years) underwent ^99mTc-DTPA aerosol inhalation scintigraphy and pulmonary function tests (PFTs). Subjects inhaled 1480 MBq of ^99mTc-DTPA for 4 min in the supine position. Scintigraphic data were recorded dynamically (1 frame/min) in the posterior projection on a 64 × 64 matrix for a 30-min period using a double-headed gamma camera (Infinia, GE, Tirat Hacarmel, Israel) equipped with a low-energy all-purpose parallel hole collimator. Half time of ^99mTc-DTPA clearance (T _1/2) was calculated by placing a mono-exponential fit on the curves. Penetration index (PI) was also calculated by dividing the peripheral total counts by the sum of the peripheral and central total counts on the first minute image, in order to quantify the distribution of the inhaled aerosol.

Results

The clearance half time of ^99mTc-DTPA radioaerosols in the BD patients (24.81 ± 6.22 min) was faster than in the normal control group (46.53 ± 22.41 min) (P = 0.004). There was also a significant difference between PI of the patients with BD (0.15 ± 0.03) and that of the controls (0.21 ± 0.06) (P = 0.002). No correlation was found between the mean T _1/2 values of ^99mTc-DTPA clearance or the spirometric measurements in the BD patients. Penetration indices were not correlated with PFT in the BD patients.

Conclusions

Lung epithelial permeability of the patients with BD was significantly higher than that of the normal subjects. The results of this study demonstrated that the assessment of lung epithelial permeability using ^99mTc-DTPA aerosol scintigraphy could predict the presence of lung involvement in the early stages of BD.

     

Imaging α<Subscript>v</Subscript>β<Subscript>3</Subscript> integrin expression in skeletal metastases with <Superscript>99m</Superscript>Tc-maraciclatide single-photon emission computed tomography: detection and therapy response assessment

Purpose

Osteoclast activity is an important factor in the pathogenesis of skeletal metastases and is a potential therapeutic target. This study aimed to determine if selective uptake of ^99mTc-maraciclatide, a radiopharmaceutical targeting α_vβ₃ integrin, occurs in prostate cancer (PCa) bone metastases and to observe the changes following systemic therapy.

Methods

The study group comprised 17 men with bone-predominant metastatic PCa who underwent whole-body planar and single-photon emission computed tomography/computed tomography (SPECT/CT) imaging with ^99mTc-maraciclatide before (n?=?17) and 12 weeks after (n?=?11) starting treatment with abiraterone. Tumour to normal bone (T:N) ratios, tumour to muscle (T:M) ratios and CT Hounsfield units (HU) were measured in up to five target metastases in each subject. An oncologist blinded to study scans assessed clinical responses up to 24 weeks using conventional criteria.

Results

Before treatment, metastases showed specific ^99mTc-maraciclatide accumulation (mean planar T:N and T:M ratios 1.43 and 3.06; SPECT T:N?and T:M ratios 3.1 and 5.19, respectively). Baseline sclerotic lesions (389–740 HU) showed lower T:M ratios (4.22 vs. 7.04, p?=?0.02) than less sclerotic/lytic lesions (46–381 HU). Patients with progressive disease (PD; n?=?5) showed increased planar T:N and T:M ratios (0.29 and 12.1%, respectively) and SPECT T:N and T:M ratios (11.9 and 20.2%, respectively). Patients without progression showed decreased planar T:N and T:M ratios (0.27 and ?8.0%, p?=?1.0 and 0.044, respectively) and SPECT T:N and T:M ratios (?21.9, and ?27.2%, p?=?0.3 and 0.036, respectively). The percentage change in CT HU was inversely correlated with the percentage change in SPECT T:M ratios (r?=??0.59, p?=?0.006).

Conclusions

^99mTc-maraciclatide accumulates in PCa bone metastases in keeping with increased α_vβ₃ integrin expression. Greater activity in metastases with lower CT density suggests that uptake is related to osteoclast activity. Changes in planar and SPECT T:M ratios after 12 weeks of treatment differed between patients with and without PD and ^99mTc-maraciclatide imaging may be a potential method for assessing early response.

     

<Superscript>99m</Superscript>Tc-Demotate 1: first data in tumour patients—results of a pilot/phase I study

Somatostatin receptor (SSTR) scintigraphy with indium-111 DTPA-octreotide has become a routine diagnostic procedure in oncology. However, it suffers some drawbacks concerning the limited availability, suboptimal imaging properties and elevated radiation burden of ¹¹¹In. We have recently been involved in the development of a new tetraamine-functionalised [Tyr³]octreotate derivative (Demotate 1) that can be easily labelled with technetium-99m at high specific activities. ^99mTc-Demotate 1 showed promising properties in preclinical studies. In this study we report on the first experience with ^99mTc-Demotate 1 in patients. Six patients (mean age 56 years) with carcinoid tumours (n=2) or endocrine pancreatic tumours (n=4) with previously positive SSTR scintigraphy were enrolled in the study. Patients were injected with 500–600 MBq ^99mTc-Demotate 1. Clinical and laboratory parameters were controlled up to 3 months p.i. Blood samples were taken at various time points up to 24 h p.i., and urine was collected up to 24 h. Whole-body images were acquired at 15–30 min, 1–2 h, 4 h and 24 h p.i. with additional single-photon emission tomography imaging at 1–4 h. Blood excretion was very rapid, with <2%ID in plasma after 1 h, and urinary excretion <20% ID after 6 h. Two patients complained of mild gastrointestinal problems and paraesthesia, but no other adverse reactions were observed. SSTR-positive tumours were rapidly visualised as early as 15 min p.i., with maximum tumour uptake (up to 19% ID) and tumour/organ ratios as early as 1 h p.i. Organs of predominant physiological uptake were the spleen and the kidneys, with no intestinal excretion detectable up to 24 h. ^99mTc-Demotate 1 detected 11 lesions while In-Oct detected ten; differences in uptake behaviour were observed in three patients. This study shows for the first time that peptides derivatised with a tetraamine ligand for labelling with ^99mTc show suitable properties for receptor imaging in patients. ^99mTc-Demotate 1 is a promising agent for the visualisation of SSTR-positive lesions in patients, allowing rapid imaging as early as 1 h p.i.; some differences are observed in pharmacokinetic behaviour compared with ¹¹¹In-DTPA-octreotide.     

<Superscript>68</Superscript>Ga- and <Superscript>111</Superscript>In-labelled DOTA-RGD peptides for imaging of αvβ3 integrin expression

PURPOSE: alphavbeta3 integrins are important cell adhesion receptors involved in angiogenic processes. Recently, we demonstrated using [(18)F]Galacto-RGD that monitoring of alphavbeta3 expression is feasible. Here, we introduce (68)Ga- and (111)In-labelled derivatives and compare them with [(18)F]Galacto-RGD. METHODS: For radiolabelling, cyclo(RGDfK(DOTA)) was synthesised using SPPS. For in vitro characterisation determination of partition coefficients, protein binding, metabolic stability, alphavbeta3 affinity and cell uptake and for in vivo characterization, biodistribution studies and micro positron emission tomography (PET) imaging were carried out. For in vivo and in vitro studies, human melanoma M21 (alphavbeta3 positive) and M21-L (alphavbeta3 negative) cells were used. RESULTS: Both tracers can be synthesised straightforward. The compounds showed hydrophilic properties and high metabolic stability. Up to 23% protein-bound activity for [(68)Ga]DOTA-RGD and only up to 1.4% for [(111)In]DOTA-RGD was found. Cell uptake studies indicate receptor-specific accumulation. This is confirmed by the biodistribution data. One hour p.i. accumulation in alphavbeta3-positive tumours was 2.9 +/- 0.3%ID/g and in alphavbeta3-negative tumours 0.8 +/- 0.1%ID/g for [(68)Ga]DOTA-RGD ([(111)In]DOTA-RGD: 1.9 +/- 0.3%ID/g and 0.5 +/- 0.2%ID/g; [(18)F]Galacto-RGD: 1.6 +/- 0.2%ID/g and 0.4 +/- 0.1%ID/g). Thus, tumour uptake ratios were comparable. Due to approx. 3-fold higher blood pool activities for [(68)Ga]DOTA-RGD, tumour/blood ratios were higher for [(111)In]DOTA-RGD and [(18)F]Galacto-RGD. However, microPET studies demonstrated that visualisation of alphavbeta3-positive tumours using [(68)Ga]DOTA-RGD is possible. CONCLUSIONS: Our data indicate that [(68)Ga]DOTA-RGD allows monitoring of alphavbeta3 expression. Especially, the much easier radiosynthesis compared to [(18)F]Galacto-RGD would make it an attractive alternative. However, due to higher blood pool activity, [(18)F]Galacto-RGD remains superior for imaging alphavbeta3 expression. Introduction of alternative chelator systems may overcome the disadvantages.