Scintigraphy with J001 Macrophage Targeting Glycolipopeptide

Diot, P.; Lemarié, É.; Banlieu, Jean Louis; Pascal, Sophie; Vaillant, L.; Revillard, J P; Binz, Hans; Normier, G.; Pape, Alain Le

doi:10.1378/chest.102.3.670

Cited by 18 publications

(2 citation statements)

References 9 publications

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“…Scintigraphic imaging agents are a million times more sensitive than magnetic resonance imaging contrast agents, and their selectivity can be enhanced by targeting them to lesion‐specific cell markers (13). Indeed, the radioisotope 99m Tc has been delivered to arthritic tissues using nonspecific IgG (14, 15), anti‐CD4 antibodies (16), CD11b/CD14–glycolipopeptide ligands (17, 18), and E‐selectin–binding peptides (18). Preclinical studies with such radioimaging agents have clearly emphasized the value of imaging arthritic tissues in vivo; however, the selectivity of the current imaging agents is not yet optimal (13), and none of the present compounds is targeted exclusively to activated macrophages.…”

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confidence: 99%

Folate‐targeted imaging of activated macrophages in rats with adjuvant‐induced arthritis

Turk

Breur

Widmer

et al. 2002

Arthritis & Rheumatism

188

168

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Objective. To determine whether overexpression of the high-affinity folate receptor (FR) on activated macrophages can be exploited to selectively target imaging agents to sites of inflammation in rats with adjuvant-induced arthritis (AIA).Methods. Folic acid was conjugated to a 99m Tc chelator (the complex termed EC20), and its distribution was visualized using gamma scintigraphy in healthy rats, rats with AIA, and arthritic rats that had been depleted of macrophages. To confirm that uptake was mediated by the FR, excess folic acid competition studies were conducted, and tissue FR levels were quantitated using a radioligand binding assay. Flow cytometry was also used to investigate uptake of folate conjugates into macrophages of both arthritic and healthy rats.Results. EC20 concentrated in the arthritic extremities of diseased rats but not in the extremities of healthy rats. The intensity of images of affected tissues was greatly reduced in the presence of excess competing folic acid. The livers and spleens of arthritic animals also showed enhanced uptake of EC20 and increased levels of FR. Depletion of macrophages from arthritic animals reduced tissue FR content and concomitantly abolished uptake of EC20. In addition, macrophages isolated from livers of rats with AIA exhibited a significantly higher binding capacity for folate conjugates than did macrophages obtained from healthy rats.Conclusion. Although EC20 is currently undergoing clinical evaluation for use in the imaging of ovarian carcinomas, the present results suggest that it may also be useful for assaying the participation of activated macrophages in inflammatory processes such as rheumatoid arthritis.

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confidence: 99%

Folate‐targeted imaging of activated macrophages in rats with adjuvant‐induced arthritis

Turk

Breur

Widmer

et al. 2002

Arthritis & Rheumatism

188

168

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“…Therefore, we decided to directly label amphotericin B itself after reduction by stannous chloride, as previously described for albumin [14]. We recently applied this method to label a new scintigraphic tracer (J001) and pentamidine [15,16]. Quality of amphotericin B radiolabelling was demonstrated by reduced content of labelled colloids, similar chromatography pattern and retention volumes of labelled and unlabelled amphotericin B.…”

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confidence: 99%

Deposition of amphotericin B aerosols in pulmonary aspergilloma

Diot

Rivoire²,

Pape³

et al. 1995

Eur Respir J

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D De ep po os si it ti io on n o of f a am mp ph ho ot te er ri ic ci in n B B a ae er ro os so ol ls s i in n p pu ul lm mo on na ar ry y a as sp pe er rg gi il ll lo om ma a ABSTRACT: The aim of the present study was to characterize amphotericin B aerosols nebulized by ultrasonic and jet nebulizers and to study their deposition and pharmacokinetics in patients with pulmonary mycetoma. The aerodynamic behaviour and pulmonary deposition of amphotericin B particles were measured using a direct isotopic method based on stable labelling of the drug with 99m Tc. Each nebulizer was bench tested for inhaled mass and particle size distribution. Three patients suffering from pulmonary aspergilloma were enrolled for a 4 week clinical study. They received 5 mg of amphotericin B daily delivered by either Fisoneb® or DP100® (ultrasonic) or Respirgard II® (jet) nebulizers. Deposition of radiolabelled amphotericin B was measured once with each nebulizer using a gamma-camera. In two patients, amphotericin B serum concentration was monitored over a 330 min period after the nebulization had been completed.Inhaled masses of the three nebulizers, assessed as % of labelled drug caught in inspiratory filter in duplicate experiments, were: 5.8 and 3.6% for Respirgard II®; 26.5 and 28.3% with Fisoneb®; 5.9 and 6.3% for DP100®. Mass median aerodynamic diameter (mean±SD) results were: 0.28±0.04 µm with Respirgard II®; 4.82±0.78 µm with Fisoneb®; and 2.27±1.14 µm with DP100®. Because of larger particles and significantly greater inhaled mass, Fisoneb® delivered more amphotericin B to the central airways, the lung periphery and in the mycetoma lung regions. Amphotericin B serum concentrations correlated with pulmonary deposition and remained below 25 ng·mL -1 . No untoward effects were reported by the patients during the 4 week trial.This study demonstrates that amphotericin B suspension can be accurately radiolabelled, is effectively nebulized by a variety of nebulizers, and is well-tolerated by human subjects.

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What Is Needed in Metabolic Research?

Elia¹,

Ward²

2000

Quality of the Body Cell Mass

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Scintigraphy with J001 Macrophage Targeting Glycolipopeptide

Cited by 18 publications

References 9 publications

Folate‐targeted imaging of activated macrophages in rats with adjuvant‐induced arthritis

Folate‐targeted imaging of activated macrophages in rats with adjuvant‐induced arthritis

Deposition of amphotericin B aerosols in pulmonary aspergilloma

What Is Needed in Metabolic Research?

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