NC100668, a New Tracer Tested for Imaging of Venous Thromboembolism: Pharmacokinetics and Metabolism in Humans

Toft, Kim Gunnar; Johnson, Judith A.; Oulie, Inger; Skotland, Tore

doi:10.1124/dmd.106.014126

Cited by 6 publications

(2 citation statements)

References 7 publications

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“…In one recent publication it was reported that the Tat peptide enters the cytosol under conditions where all known forms of endocytosis have been knocked down (50). However, the concentration used in this study was rather high, approximately 10 µg/ml, when compared with the expected human dose of 50-100 µg for SPECT imaging with targeting peptides (51,52). Even if these positively charged peptides turn out to be useful for other purposes, it is very unlikely that they will be useful for medical imaging of cytosolic targets.…”

Section: Cellular Uptake Of Positively Charged Moleculesmentioning

confidence: 88%

Molecular imaging: challenges of bringing imaging of intracellular targets into common clinical use

Skotland

2012

Contrast Media & Molecular

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Molecular imaging (MI) takes advantage of several new techniques to detect biomarkers or biochemical and cellular processes, with the goal of obtaining high sensitivity, specificity and signal-to-noise ratio imaging of disease. The imaging modalities bearing the most promise for MI are positron emission tomography (PET), single photon emission computer tomography (SPECT) and different optical imaging techniques with high sensitivity. Also magnetic resonance imaging (MRI) with contrast agents like ultra-small superparamagnetic iron oxide particles (USPIO), magnetic resonance spectroscopy and ultrasound imaging with contrast agents may be useful approaches. MI techniques have been used in the clinic for many years, i.e. PET imaging using (18) F-labeled fluorodeoxyglucose. Animal studies have during the last years revealed great potential for MI also with several other agents. The focus of the present article is the challenges of clinical imaging of intracellular targets following intravenous injection of the agents. Thus, the great challenge of getting enough contrast agent into the cytosol and at the same time obtaining a low signal from tissue just outside the diseased area is discussed.

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Section: Cellular Uptake Of Positively Charged Moleculesmentioning

confidence: 88%

Molecular imaging: challenges of bringing imaging of intracellular targets into common clinical use

Skotland

2012

Contrast Media & Molecular

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“…Much higher amounts have to be injected to obtain concentrations above 10 µM for more than a few seconds in blood and reach such concentrations in the diseased tissues. Thus, the dose needed to obtain the membrane-penetrating properties for such peptides is rather high, especially when compared to the expected human dose of 50–100 µg for two targeting peptides for SPECT imaging, with which one of the authors has been working [37,38].…”

Section: Binding Of Cpps To Cells and Uptake Via Endocytosismentioning

confidence: 99%

Cell-Penetrating Peptides: Possibilities and Challenges for Drug Delivery in Vitro and in Vivo

et al. 2015

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Abstract:In this review, we discuss how cell-penetrating peptides (CPPs) might get access to their intracellular targets. We specifically focus on the challenge of deciding whether the positively-charged CPPs are just bound to the negatively-charged cell surface and subsequently endocytosed or actually transported into the cytosol, either by direct plasma membrane penetration or after endocytosis. This discussion includes comments about pitfalls when using pharmacological inhibitors in such studies. The possibility of exploiting CPPs as carriers for the delivery of drugs of different sizes in vitro is discussed, as is the use of CPPs as carriers for therapeutic drugs or contrast agents in vivo. We conclude that in many cases, more studies are needed to demonstrate conclusively whether increased delivery of a substance attached to CPPs is due to a membrane-penetrating property or whether the increase is a consequence of just changing the charge of the substance to be delivered. Finally, the expected dose needed for the use of such conjugates in vivo is discussed, including aspects to consider in order to bring potential products into clinical use.

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Human urinary excretion of NC100692, an RGD-peptide for imaging angiogenesis

Roed

Oulie

McParland³

et al. 2009

European Journal of Pharmaceutical Sciences

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NC100668, a New Tracer Tested for Imaging of Venous Thromboembolism: Pharmacokinetics and Metabolism in Humans

Abstract: ABSTRACT:The 99m Tc-complex of NC100668 [Acetyl-Asn-Gln-Glu-Gln-Val-SerPro-Tyr(3-iodo)-Thr-Leu-Leu-Lys-Gly-NC100194] is a new tracer tested for nuclear medical imaging of venous thromboembolism. NC100668 is a 13-amino acid peptide with a Tc-binding chelator

Cited by 6 publications

References 7 publications

Molecular imaging: challenges of bringing imaging of intracellular targets into common clinical use

Molecular imaging: challenges of bringing imaging of intracellular targets into common clinical use

Cell-Penetrating Peptides: Possibilities and Challenges for Drug Delivery in Vitro and in Vivo

Human urinary excretion of NC100692, an RGD-peptide for imaging angiogenesis

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