The study should evaluate the biological distribution of [99mTc]Tc(CO)3-(HE)3-Ec1 in patients with solid tumor
The primary objective are:
To assess the distribution of [99mTc]Tc(CO)3-(HE)3-Ec1 in normal tissues and tumors at different time intervals.
To evaluate dosimetry of [99mTc]Tc(CO)3-(HE)3-Ec1 .
To study the safety and tolerability of the drug [99mTc]Tc(CO)3-(HE)3-Ec1 after a single injection in a diagnostic dosage.
The secondary objective are:
1. To compare the obtained [99mTc]Tc(CO)3-(HE)3-Ec1 SPECT imaging results with the data of CT and/or MRI and/or ultrasound examination and immunohistochemical (IHC) studies in solid tumor patients.

开始日期2022-10-01

申办/合作机构

Tomsk National Research Medical Center of the Russian Academy of Sciences

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100 项与 [99mTc]Tc(CO)3-(HE)3-Ec1 相关的临床结果

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100 项与 [99mTc]Tc(CO)3-(HE)3-Ec1 相关的转化医学

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100 项与 [99mTc]Tc(CO)3-(HE)3-Ec1 相关的专利（医药）

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项与 [99mTc]Tc(CO)3-(HE)3-Ec1 相关的文献（医药）

2016-04-01·Cancer Biotherapy and Radiopharmaceuticals4区 · 医学

Exploring the Potential of ^99mTc(CO)₃-Labeled Triazolyl Peptides for Tumor Diagnosis

4区 · 医学

Article

作者: Sinha, Samarendu ; Debnath, Mita C. ; Dewanjee, Saikat ; Ganguly, Soumya ; Ganguly, Shantanu ; Baishya, Rinku ; Gupta, Amit ; Gaonkar, Raghuvir H.

In recent years the authors have reported on (99m)Tc(CO)3-labeled peptides that serve as carriers for biomolecules or radiopharmaceuticals to the tumors. In continuation of that work they report the synthesis of a pentapeptide (Met-Phe-Phe-Gly-His; pep-1), a hexapeptide (Met-Phe-Phe-Asp-Gly-His; pep-2), and a tetrapeptide (Asp-Gly-Arg-His; pep-3) and the attachment of 3-amino-1,2,4-triazole to the β carboxylic function of the aspartic acid unit of pep-2 and pep-3. The pharmacophores were radiolabeled in high yields with [(99m)Tc(CO)3(H2O)3](+) metal aqua ion, characterized for their stability in serum and saline, as well as in His solution, and found to be substantially stable. B16F10 cell line binding studies showed favorable uptake and internalization. In vivo behavior of the radiolabeled triazolyl peptides was assessed in mice bearing induced tumor. The (99m)Tc(CO)3-triazolyl pep-3 demonstrated rapid urinary clearance and comparatively better tumor uptake. Imaging studies showed visualization of the tumor using (99m)Tc(CO)3-triazolyl pep-3, but due to high abdominal background, low delineation occurred. Based on the results further experiments will be carried out for targeting tumor with triazolyl peptides.

2013-03-14·Journal of Medicinal Chemistry1区 · 医学

Influence of the Bifunctional Chelator on the Pharmacokinetic Properties of ^99mTc(CO)₃-Labeled Cyclic α-Melanocyte Stimulating Hormone Analog

1区 · 医学

Article

作者: Jiménez, Maria Angeles ; Correia, João D. G. ; Morais, Maurício ; Raposinho, Paula D. ; Santos, Isabel ; Oliveira, Bruno L. ; Oliveira, Maria Cristina

Aiming at the design of specific melanocortin-1 receptor (MC1R) targeted imaging probes, we report on the effect of different azolyl-ring substitution patterns (carboxylate at the 4-position and/or methyl groups at the 3,5 positions) of pyrazolyl-diamine bifunctional chelators (Pz(2)-Pz(4)) on the pharmacokinetic profile of the (99m)Tc(CO)3-labeled lactam bridge-cyclized α-melanocyte stimulating hormone derivative, βAlaNleCycMSH(hex). Three pyrazolyl-diamine-containing chelators were conjugated to βAlaNleCycMSHhex, with the resulting peptide conjugates displaying subnanomolar MC1R binding affinity. Biodistribution studies in B16F1 melanoma-bearing mice show that all radiopeptides present a good melanoma uptake. The introduction of a carboxylate group in the azolyl-ring leads to a remarkable reduction of the kidney (>89%) and liver (>91%) accumulation for (99m)Tc(CO)3-Pz(3)-βAlaNleCycMSH(hex) and (99m)Tc(CO)3-Pz(4)-βAlaNleCycMSH(hex) when compared to the radiopeptide (99m)Tc(CO)3-Pz(1)-βAlaNleCycMSH(hex), where that group is absent. The good tumor uptake and favorable tumor-to-nontarget-organs ratios of (99m)Tc(CO)3-Pz(3)-βAlaNleCycMSH(hex) and (99m)Tc(CO)3-Pz(4)-βAlaNleCycMSH(hex) highlights the potential of both compounds as melanoma imaging agents.

2010-12-01·Applied Radiation and Isotopes

Click chemistry for [99mTc(CO)3] labeling of Lys3-bombesin

Article

作者: Santos-Cuevas, C. L. ; Ordaz-Rosado, D. ; Garcia-Becerra, R. ; Ocampo-Garcia, B. E. ; Rivero, I. A. ; Arteaga de Murphy, C. ; Sarmiento, J. I. ; Ferro-Flores, G.

(99m)Tc-HYNIC labeled Lys(3)-bombesin has shown specific binding to gastrin-releasing peptide receptors (GRP-r) over-expressed in cancer cells. Click chemistry offers an innovative functionalization strategy for biomolecules such as bombesin. The aim of this research was to apply a click chemistry approach for [(99m)Tc(CO)(3)] labeling of Lys(3)-bombesin and to compare the in vitro MCF7 breast cancer cell uptake and biodistribution profile in mice with that of (99m)Tc-EDDA/HYNIC-Lys(3)-bombesin. The results suggest a higher lipophilicity for (99m)Tc(CO)(3)-triazole-Lys(3)-bombesin which explains its higher in vivo hepatobiliary elimination. Pancreas-to-blood ratio for (99m)Tc(CO)(3)-triazole-Lys(3)-bombesin was 4.46 at 3 h and both bombesin radiopharmaceuticals showed specific recognition for GRP receptors in MCF7 cancer cells. Click chemistry is a reliable approach for [(99m)Tc(CO)(3)] labeling of Lys(3)-bombesin.

100 项与 [99mTc]Tc(CO)3-(HE)3-Ec1 相关的药物交易

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