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PubMed1993

Indium-111-labelled cationic complexes of aminothiols: structure-activity correlation.

In the present work a series of NxS2 ligands were synthesized, investigated for the formation of cationic, indium chelates and evaluated comparatively in experimental animals. The compounds under study formed indium complexes which were stable in vitro and presented myocardial uptake. Animal studies showed that the chemical structure of the ligand plays an important role in biodistribution. A system of one six-membered and two five-membered rings, formed by the metal and the donor atoms of the ligand, may constitute a basic structure for the development of new indium tracers with myocardial affinity.

Animals↗

PubMed1991

Monoclonal antibody BW431/26 labelled with technetium 99m and indium 111: an investigation of the biodistribution and the dosimetry in patients.

As a competitive diagnostic tool for the detection of malignant tumours and other pathological conditions, monoclonal antibodies have long been established. Herein we give the biokinetic data of the antibody BW 431/26 and the consequent radiation dose to patients. These parameters were recorded in 39 patients, using the antibody labelled either with technetium 99m or indium 111. Remarkable differences were observed between the two radionuclides. Whereas the indium-labelled one showed biexponential elimination kinetics, the technetium-labelled one is eliminated linearly over time. The distribution pattern of the two is identical, although the radiation dose varies quite a lot, being 20-fold higher with indium 111 when total body exposure is taken into account (for 111In the whole-body radiation exposure is 0.1 mGy/MBq; for 99mTc it is 0.0047 mGy/MBq). With respect to these results and considering the general availability of the technetium-labelled Ab, it is the best choice for diagnostic use.

Humans↗

PubMed1994

Immunoscintigraphy with a new indium-111-labeled monoclonal antibody (MAb 1A3) in patients with colorectal cancer.

PURPOSE: This study was designed to evaluate a new anticolorectal carcinoma monoclonal antibody (1A3), conjugated with the bifunctional chelating agent N,N'-bis(2-hydroxybenzyl)1(4-bromoacetamidobenzyl)1,2-ethylenediam ine-N,N'- diacetic acid and labeled with indium-111, in a Phase I/II study involving 38 patients with localized or advanced colorectal cancer. METHODS: Patients were injected with indium-111-N,N'-bis(2-hydroxybenzyl) 1(4-bromoacetamidobenzyl)1,2-ethylenediamine-N,N'-diacetic acid-monoclonal antibody 1A3 (1-50 mg, 1-5 mCi) and imaged at two or three sessions one to five days later. Scintigraphic findings were compared with radiologic, pathologic, surgical, and other clinical findings to assess the accuracy of radioimmunoscintigraphy. RESULTS: At least one known tumor site was clearly defined by planar scintigraphy in 29 (76 percent) patients. Increased radioactivity was seen in 40 of 63 known tumor sites (37/43 abdominal-pelvic, 3/15 hepatic, and 0/5 pulmonary sites) without any apparent dose-related effects. Nineteen previously undetected sites were considered positive by imaging, and, of these, six were biopsy-proven tumor sites, four were probable tumor sites, three were definitely false positive sites, and six were probable false positive sites. Radioimmunoscintigraphy detected proven tumor in 15 of 16 patients with negative or equivocal computed tomography results. Of of the 28 patients with rectosigmoid cancer, 25 (89 percent) had positive studies with 34 of 47 tumor sites showing definite uptake on the scintigrams. This included 3 of 9 hepatic metastases. The only adverse reaction occurred in one patient who developed transient hives. Human anti-mouse antibody responses occurred in approximately one-half of the patients injected with doses of 10 or 50 mg. CONCLUSION: This study shows that radioimmunoscintigraphy with this indium-111-labeled monoclonal antibody is safe, it can detect most nonhepatic abdominal-pelvic tumors with a positive predictive value of 83 (44/53) percent, and it should prove to be useful, particularly in the diagnosis of recurrent rectal carcinoma.

Adenocarcinoma↗

PubMed1989

Predictive value of indium-111 antimyosin uptake for improvement of left ventricular wall motion after thrombolysis in acute myocardial infarction.

In 21 patients treated with thrombolysis for acute myocardial infarction (AMI), the degree of myocardial uptake of indium-111 monoclonal antimyosin antibodies injected within 24 hours after onset of AMI was compared with the degree and extent of regional asynergy on admission and discharge, as assessed by 2-dimensional echocardiography. On the first day of AMI, 80 MBq of indium-111 antimyosin was injected and planar images were made 24 hours later. Indium-111 antimyosin uptake was evaluated for count density index (count density of infarct zone/left lung count density) in the left anterior oblique projection, in which the infarction zone was well displayed in all patients. Using 2-dimensional echocardiography, the left ventricle was divided into 13 segments and evaluated for regional asynergy, which was considered severe (akinesia or dyskinesia) or mild (hypokinesia). The extent of regional asynergy was measured by the number of asynergic segments. All 21 patients had severe regional asynergy on admission. Nine of 21 showed only mild regional asynergy on discharge and 12 of 21 had persistent severe regional asynergy in at least 1 segment. The count density index was significantly lower in patients with mild regional asynergy on discharge compared with patients with severe regional asynergy (1.63 +/- 0.27 vs 2.50 +/- 0.42, p less than 0.01).(ABSTRACT TRUNCATED AT 250 WORDS)

Aged↗

PubMed1994

Postoperative cardiothoracic infection: diagnostic value of indium-111 white blood cell imaging.

During a 6.5-year period, 50 indium 111-labeled white blood cell scans were obtained in 49 selected patients who had undergone sternotomy. Retrospectively, six sternal wounds and eight cardiovascular prostheses were found to be infected in 13 patients. For cardiothoracic surgical sites, the sensitivity, specificity, and accuracy of indium-111-labeled white blood cell scintigraphy were 86%, 97%, and 95%, respectively. Whole-body imaging identified the presence of major extramediastinal sites of infection in 10 patients. In patients with complicated cardiothoracic conditions, indium-111-labeled white blood cell imaging provides valuable diagnostic information regarding a variety of postoperative infections.

Adolescent↗

PubMed1983

Labelling of lymphocytes with indium 111 oxine: effect on cell surface phenotype and antibody-dependent cellular cytotoxicity.

Indium 111 oxine is currently used to label peripheral lymphocytes in order to study the kinetics of these cells in vivo. Since the quantity of radioisotope for labelling is still a matter of controversy, we have investigated in vitro the effect of increasing the concentration of indium 111 oxine on the lymphocyte surface phenotype and the antibody-dependent cellular cytotoxicity (ADCC) using lymphocytes from normal subjects. The cell surface phenotype, as evaluated by 2 monoclonal antibodies, was not affected whereas ADCC, at any of the doses used, was significantly reduced compared to the baseline value. The implications of these results for the use of indium 111 oxine for the in vivo studies are discussed.

Adult↗

PubMed2005

In vitro effect of free and complexed indium(III) against Mycobacterium tuberculosis.

In mycobacteria, the study of inhibition by metal ions has been limited by the absence of suitable molecular vectors. Recently, we reported on the inhibitory activity of a family of chelators, macrocyclic compounds (MCC), against Mycobacterium tuberculosis. In this study equimolar concentrations of the free cations vanadium(IV), arsenic(III), iron(III), indium(III) and bismuth(III), and as 1:1 complexes with the MCC 1,4,8,11-tetraazacyclotetradecane-1,4,8,11-tetra-acetic acid (TETA) were tested in vitro against M. tuberculosis using the Bactec 460 TB radiometric technology (Becton-Dickinson, MD, USA). Radiometric inhibition above 80% was obtained with free indium(III) and bismuth(III), and ranged from 80% to 99%, with the complexes of TETA with vanadium(IV), bismuth(III) and indium(III), in the order of increasing activity. The highest radiometric inhibition levels were obtained with the [In(TETA)]- complex, which caused drops of up to 4 log units in cellular viability. The minimal inhibitory concentration of this compound was evaluated at 3 microM.

Anti-Bacterial Agents↗

PubMed2004

Toxicity of indium arsenide, gallium arsenide, and aluminium gallium arsenide.

Gallium arsenide (GaAs), indium arsenide (InAs), and aluminium gallium arsenide (AlGaAs) are semiconductor applications. Although the increased use of these materials has raised concerns about occupational exposure to them, there is little information regarding the adverse health effects to workers arising from exposure to these particles. However, available data indicate these semiconductor materials can be toxic in animals. Although acute and chronic toxicity of the lung, reproductive organs, and kidney are associated with exposure to these semiconductor materials, in particular, chronic toxicity should pay much attention owing to low solubility of these materials. Between InAs, GaAs, and AlGaAs, InAs was the most toxic material to the lung followed by GaAs and AlGaAs when given intratracheally. This was probably due to difference in the toxicity of the counter-element of arsenic in semiconductor materials, such as indium, gallium, or aluminium, and not arsenic itself. It appeared that indium, gallium, or aluminium was toxic when released from the particles, though the physical character of the particles also contributes to toxic effect. Although there is no evidence of the carcinogenicity of InAs or AlGaAs, GaAs and InP, which are semiconductor materials, showed the clear evidence of carcinogenic potential. It is necessary to pay much greater attention to the human exposure of semiconductor materials.

Aluminum Compounds↗

PubMed1983

Indium-111 tropolonate leucocyte scanning in the detection of intra-abdominal abscesses.

Indium-111 leucocyte scanning is established as an accurate method for localising intra-abdominal abscesses. With the currently available cell labelling techniques there is a variable and significant delay in localisation of abscesses which is a major disadvantage in comparison with ultrasound or computed tomography. We have examined the speed and accuracy of localisation of leucocytes labelled in plasma with a new chelating agent, indium-111 tropolonate, in 90 patients with suspected intra-abdominal abscess. In 50 patients a comparison with ultrasound was made. Nineteen patients had abscesses. The sensitivity and specificity of labelled leucocytes were 95% and 99%, respectively. Comparative results for ultrasound were 60% and 83%. In nine out of 10 patients with abscesses scanned sequentially from 40 min after return of the labelled cells, activity corresponding to the abscess was already visible on the 40 min scan. These results demonstrate that indium-111 plasma labelled leucocyte scanning is both rapid and an accurate method of detecting abscesses.

Abdomen↗

PubMed1997

Indium In-111 pentetreotide scintigraphy: application to carotid body tumors.

PURPOSE: This study was conducted to investigate and illustrate the use of Indium In-111 pentetreotide scintigraphy as it applies to carotid body tumors (CBT). Localization has relied primarily on ultrasonography, computed tomography, and magnetic resonance imaging with angiographic confirmation. These methods only assess the cervical bifurcation without providing an evaluation of metastasis in patients without symptoms or recurrence in patients after surgery. METHODS: Indium In-111 pentetreotide scintigraphy was used in five patients with a diagnosis of CBT. Four patients were evaluated after surgical excision for evidence of tumor recurrence. One patient was evaluated before excision for diagnostic confirmation. RESULTS: No evidence of tumor recurrence was demonstrated in the four patients who had undergone previous CBT excision. One of these patients had increased activity in the pituitary, later confirmed as an enlarged pituitary without evidence of an adenoma with computed tomography. The diagnosis of CBT was confirmed in the patient evaluated before surgery. This patient also had increased activity in the occipital region, confirmed as the site of previous ischemia on computed tomography. CONCLUSION: Indium In-111 pentetreotide scintigraphy is a new innovative method for viewing neuroendocrine tumors. Its potential lies not only in tumor localization but also in identification of recurrent tumor at the operative site and metastatic disease.

Carotid Body↗

PubMedDate not supplied

Carbohydrate-bearing 3-hydroxy-4-pyridinonato complexes of gallium(III) and indium(III).

Gallium and indium complexes with pendant carbohydrates have been prepared and examined for their potential as radiopharmaceuticals. Carbohydrate-bearing 3-hydroxy-4-pyridinone ligand precursors and their tris(ligand)gallium(III) and -indium(III) complexes were synthesized and characterized by mass spectrometry, elemental analysis, and (1)H and (13)C NMR spectroscopy, and in the case of one intermediate, by X-ray crystallography. With three equivalents of ligand, neutral complexes formed with the bidentate hydroxypyridinone moiety complexing the gallium(III) and indium(III) metal centers.

Carbohydrates↗

PubMedDate not supplied

Evaluation of the in vivo biodistribution of indium-111 and yttrium-88 labeled dendrimer-1B4M-DTPA and its conjugation with anti-Tac monoclonal antibody.

We evaluated the in vivo biodistribution of indium- and yttrium-labeled second-generation polyamidoamine dendrimer (PAMAM) conjugated with 2-(p-isothiocyanatobenzyl)-6-methyl-diethylenetriaminepentaacetic acid (1B4M), a derivative of DTPA. In addition, we conjugated PAMAM-1B4M to humanized anti-Tac IgG (HuTac) and evaluated its in vitro and in vivo properties. PAMAM-1B4M was labeled with 111In at 37-48 MBq/mg (1.0-1.3 mCi/mg) or with 88Y at 3.7-4.8 MBq/mg (0.1-0. 13 mCi/mg), and an aliquot of radiolabeled conjugate was saturated with the corresponding stable yttrium or indium. Nontumor-bearing nude mice were injected intravenously with 55.5-66.6 kBq (1.5-1.8 microCi) of 88Y-labeled PAMAM-1B4M or with 185 kBq (5 microCi) of 111In-labeled PAMAM-1B4M. The mice were then sacrificed at 15 min, 90 min, 1 day, and 4 days postinjection. Then the PAMAM-1B4M was conjugated with HuTac and labeled with 111In at 111-259 MBq/mg (3-7 mCi/mg). Another preparation of 111In-labeled HuTac-PAMAM-1B4M was saturated with stable indium. Immunoreactivity of both preparations and biodistribution in normal mice 1 h after injection and in ATAC4 and A431 tumor-bearing mice 18 h after injection were evaluated and compared with those of 111In-labeled 1B4M-HuTac. We noted significantly higher accumulations (p < 0.05) of 111In-labeled and 88Y-labeled unsaturated PAMAM-1B4M than saturated preparations in the liver, kidney, spleen, and bone at most time points. The whole-body clearance times of unsaturated preparations were significantly slower than those of saturated preparations at all time points, with the exception of 168 h for 111In-labeled PAMAM-1B4M. The saturated preparation of 111In-labeled HuTac-PAMAM-1B4M showed lower hepatic uptake (27 +/- 2%ID/g) than the unsaturated (32 +/- 2%ID/g), but greater than the HuTac-1B4M control (10 +/- 0%ID/g). The splenic uptake showed 15 +/- 1, 38 +/- 5, and 8 +/- 1%ID/g for the saturated, unsaturated, and control, respectively. The biodistribution of the dendrimer conjugated HuTac in normal organs of tumor-bearing mice was similar to nontumor-bearing mice. Specific tumor (ATAC4) uptake was higher than that in nonspecific tumor (A431). In conclusion, we evaluated the biodistribution of radiolabeled PAMAM-1B4M. We noted high accumulation in the liver, kidney, and spleen, which significantly decreased when the chelates were saturated with the stable element. A similar phenomenon was observed between unsaturated and saturated 111In-labeled HuTac-PAMAM-1B4M, indicating that the PAMAM dendrimer had a detrimental effect on biodistribution.

Animals↗

PubMed1988

Assessment of severity of cardiac rejection in heterotopic heart transplantation using indium-111 antimyosin and magnetic resonance imaging.

Seven canine donor hearts in which atrial septal defect and tricuspid regurgitation had previously been produced were heterotopically transplanted into the recipients' chest cavities. Indium-111 antimyosin myocardial imaging of the excised heart was performed using a scinticamera. Magnetic resonance imaging was also performed and the T2 relaxation time calculated. Subsequently, these data were correlated with pathological findings, which indicated the degree of rejection. Indium-111 antimyosin uptake was high in moderate and severe rejection, but the T2 relaxation time was prolonged even in mild rejection. Thus indium-111 antimyosin uptake was specific, and the T2 relaxation time was sensitive, for detecting the severity and extent of cardiac rejection. Although ex vivo experimental results have been reported, these new methods allow characterisation and accurate evaluation of myocardial tissue undergoing cardiac rejection.

Animals↗

PubMed1992

Gastrointestinal accumulation of indium-111 labelled granulocytes in reactive arthritis.

Six patients with reactive arthritis (ReA) were examined for gastrointestinal accumulation of Indium-111 labelled granulocytes. Abnormal scintigrams were found in three of six patients all of which showed early (less than 4 h) accumulation of indium-111 labelled granulocytes which may represent small intestinal inflammation. Our findings may indicate that the small intestine is involved in ReA, and that indium-111 granulocyte scintigraphy is a useful method for demonstrating inflammatory changes in the small intestine in reactive arthritis (ReA).

Adult↗

PubMed1988

Donor indium-111 leukocyte scan in a nonleukopenic patient.

Indium-III leukocytes are useful in localizing infection and abscess with excellent sensitivity and specificity. In this case report, heterologous Indium-III leukocytes provided the same diagnostic information as autologous leukocytes without adverse effects to the patient. A potential application of donor Indium-III leukocytes in the nonleukopenic patient is discussed.

Adult↗

PubMed1990

Indium-111 leukocyte scanning and fracture healing.

This study was undertaken to determine the specificity of indium-111 leukocyte scans for osteomyelitis when fractures are present. Midshaft tibial osteotomies were performed in 14 New Zealand white rabbits, seven of which were infected postoperatively with Staphylococcus aureus per Norden's protocol. All 14 rabbits were scanned following injection with 75 microCi of indium 111 at 72 h after osteotomy and at weekly intervals for 4 weeks. Before the rabbits were killed, the fracture sites were cultured to document the presence or absence of infection. The results of all infected osteotomy sites were positive, whereas no positive scans were found in the noninfected osteotomies. We concluded from this study that uncomplicated fracture healing does not result in a positive indium-111 leukocyte scan.

Animals↗

PubMed2004

Biological monitoring of exposures to aluminium, gallium, indium, arsenic, and antimony in optoelectronic industry workers.

The main objective of this study was to investigate aluminum, gallium, indium, arsenic, and antimony exposures on blood and urine levels in the optoelectronic workers. One hundred seventy subjects were enrolled in this cohort study. Whole blood and urine levels were determined by inductively coupled plasma-mass spectrometry. Blood indium and urine gallium and arsenic levels in the 103 workers were significantly higher than that in 67 controls during the follow-up period. In regression models, the significant risk factors of exposure were job title, preventive equipment, Quetelet's index, sex, and education level. The findings of this study suggest that gallium, indium, and arsenic exposure levels may affect their respective levels in blood and urine. The use of clean, preventive equipment is recommended when prioritizing the administration of safety and hygiene in optoelectronics industries.

Adult↗

PubMed1984

Left ventricular platelet deposition after acute myocardial infarction. An attempt at quantification using blood pool subtracted indium-111 platelet scintigraphy.

Since indium-111 platelet scintigraphy for the detection of left ventricular thrombosis often shows considerable non-specific blood pool activity a subtraction method using simultaneous technetium-99m blood pool scintigraphy was undertaken in 11 subjects with well documented remote myocardial infarction, who served as positive or negative controls, and in 18 consecutive patients with acute myocardial infarction. The results were compared with those of cross sectional echocardiography. Thirteen patients had transmural myocardial infarction and the calculated count per pixel in the left ventricle of the subtracted indium-111 platelet scintigram was (mean (SD)) 0.28(0.35), but five patients with subendocardial myocardial infarction had a mean count of 0.04(0.06). In seven patients with transmural myocardial infarction (two anterior and five inferior) left ventricular thrombosis was detected by indium-111 platelet scintigraphy but in only one of these by cross sectional echocardiography. None of the patients with subendocardial myocardial infarction had left ventricular thrombosis. Subtracted left ventricular counts correlated well with the visual results. It is concluded that left ventricular platelet sequestration after acute myocardial infarction may be quantified and precisely located and that quantitative longitudinal studies of the natural history and drug intervention are now possible.

Adult↗