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Journal articles on the topic '177Lu'

Author: Grafiati

Published: 4 June 2021

Last updated: 26 July 2025

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1

Дьячков, А. Б., А. А. Горкунов, А. В. Лабозин та ін. "Исследование кинетических параметров схемы лазерной фотоионизации лютеция". Журнал технической физики 128, № 3 (2020): 301. http://dx.doi.org/10.21883/os.2020.03.49055.277-19.

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Разработка лазерного фотоионизационного метода получения радионуклида 177Lu для применения в медицине требует знания интенсивностей светового насыщения по каждой ступени схемы фотоионизации лютеция (5d6s2 2D3/2-5d6s6p 4Fo5/2-5d6s7s 4D3/2-(53375 сm-1)o1/2) с учетом используемых компонент сверхтонкой структуры переходов. В работе экспериментально определены эффективные сечения возбуждения различных сверхтонких компонент переходов для изотопов 175Lu, 176Lu, 177Lu и 177mLu излучением импульсных перестраиваемых по длине волны лазеров на красителях, накачиваемых лазерами на парах меди. Ключевые слов

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2

Riskiana, Dewi Nur, Mukhtar Effendi, Ariyawan Sunardi, Mochamad Imron, and Abdul Aziz Rohman Hakim. "PERHITUNGAN PRODUKSI 177Lu BERDASARKAN VARIASI WAKTU IRADIASI DI REAKTOR RSG-GAS MENGGUNAKAN PROGRAM ORIGEN 2.1." Reaktor : Buletin Pengelolaan Reaktor Nuklir 18, no. 1 (2021): 27. http://dx.doi.org/10.17146/bprn.2021.18.1.6281.

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Telah dilakukan perhitungan radioaktivitas 177Lu (Lutetium-177) dengan variasi waktu iradiasi di Reaktor RSG-GAS. 177Lu merupakan radioisotop golongan lantanida yang sekarang banyak digunakan sebagai agen radioterapi kanker. Perhitungan ini menggunakan paket program ORIGEN 2.1 dengan memasukkan data inputan seperti fluks neutron (1 x 104 n/m2 s), massa lutetium oksida (3 miligram) dan lama iradiasi (4 hari,8 hari, dan 12 hari). Dalam penentuan massa lutetium dibedakan menjadi dua komponen yaitu massa 176Lu dan 175Lu yang berturut-turut sebesar 2 miligram dan 0,6 miligram. Perhitungan tersebut

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3

Gurin, Andrey, Yelena Chakrova, Ilona Matveyeva, and Patrick Riss. "Optimization of Reaction Parameters for the Synthesis of 177Lu-DOTAELA." Revista de Chimie 71, no. 8 (2020): 55–62. http://dx.doi.org/10.37358/rc.20.8.8278.

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The article provides a comparison of the theoretically calculated and experimentally determined yield of the reaction 176Lu (n, �A)177Lu. Also, it provides the results of the studies on lutetium-177 labeling of a non-peptide antagonist of gonadotropin-releasing hormone (GnRH) elagolix (ELA) associated with a chelating DOTA (DOTAELA). The synthesized DOTAELA complex was labeled with the 177Lu isotope.177Lu was produced by the reaction (n, �A) using the enriched LuCl3 target at the reactor WWR�CK. Production of 177Lu by the (n, �A) reaction from the enriched 176Lu target achieved by irradiation

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4

Nguyen, Ngoc Tuan, Van Dong Duong, Van Cuong Bui, Thanh Minh Pham, and Thi Hang Nguyen. "Study on the production of ¹⁷⁷Lu for medical purposes at the Dalat Research Reactor. Part 1. Study on production of ¹⁷⁷Lu at the Dalat Research Reactor." Nuclear Science and Technology 5, no. 1 (2015): 18–25. http://dx.doi.org/10.53747/jnst.v5i1.181.

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Lutetium-177 (177Lu) radioisotope used for medical purposes has been produced at the Dalat Nuclear Research Reactor during 2012-2014. The product was synthezed by the activation reaction 176Lu (n,γ) 177Lu. The target was Lutetium oxide with an abundance of 176Lu being 2.59% and the irradiation was conducted with a neutron flux of 2.1013 n cm-2 s-1. The activity of the 177Lu product was 39,59 Ci g-1 after 108 hous of the irradiation. The yield of this method was much higher compared to those of the reaction 176Yb(n, γ)177Yb → 177Lu + β- which for the same time could be 15mCi/50mg only. Because

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5

Widyaningrum, Triani, Mr Triyanto, Endang Sarmini, Umi Nur Sholikhah, and Sunarhadijoso Soenarjo. "KARAKTERISTIK PEMISAHAN RADIOLUTESIUM-177/177mLu DAN RADIOITERBIUM-169/175Yb PADA KOLOM RESIN LN-EICHROM." Jurnal Sains dan Teknologi Nuklir Indonesia 16, no. 1 (2015): 1. http://dx.doi.org/10.17146/jstni.2015.16.1.2353.

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ABSTRAK KARAKTERISTIK PEMISAHAN RADIOLUTESIUM- 177/177mLu DAN RADIOITERBIUM-169/175Yb PADA KOLOM RESIN LN-EICHROM. Radiolutesium-177Lu keradioaktifan jenis tinggi merupakan salah satu radiolantanida yang banyak digunakan untuk menangani berbagai kasus kanker, namun di Indonesia penggunaan radiofarmaka bertanda 177Lu belum dapat dijanjikan karena teknik produksi radioisotop primernya belum dikuasai. Prospek produksi 177Lu melalui reaksi inti 176Yb (n,g) 177Yb* à 177Lu* + β– dipelajari melalui metode pemisahan matrik 177/177mLu-169/175Yb/176Yb dalam sistem kromatografi kolom resin LN-Eichrom. Pr

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6

Rosmayani, Lena, Anis Rohanda, and Raden Farzand Abdullatif. "A SIMULATION OF IRRADIATION CALCULATIONS ON LUTETIUM-177 PRODUCTION IN RSG-GAS USING U3SI2-AL AND U9MO-AL FUELS." JURNAL TEKNOLOGI REAKTOR NUKLIR TRI DASA MEGA 25, no. 2 (2023): 45. http://dx.doi.org/10.55981/tdm.2023.6793.

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This research is a simulation of irradiation calculations on the production of the radioisotope Lutetium-177 (177Lu) in the G.A Siwabessy Reactor (RSG-GAS). This study aims to analyze the comparative calculation of 177Lu activity and its purity. One of the production methods of 177Lu in RSG-GAS is carried out by irradiating Lu2O3 targets. This Lu2O3 target irradiation produced the radioisotope 177Lu along with 177mLu as an impurity. For Medical treatment using radioisotopes, the minimum activity for 177Lu is 20 GBq/mg, and the impurity should not exceed 0.1%. Calculations were carried out with

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7

Kazakov, Andrey G., Taisya Y. Ekatova, Julia S. Babenya, et al. "Recovery of 177Lu from Irradiated HfO2 Targets for Nuclear Medicine Purposes." Molecules 27, no. 10 (2022): 3179. http://dx.doi.org/10.3390/molecules27103179.

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A new method of production of one of the most widely used isotopes in nuclear medicine, 177Lu, with high chemical purity was developed; this method includes irradiation of the HfO2 target with bremsstrahlung photons. The irradiated target was dissolved in HF and then diluted and placed onto a column filled with LN resin. Quantitative sorption of 177Lu could be observed during this process. The column later was rinsed with the mixture of 0.1 M HF and 1 M HNO3 and then 2 M HNO3 to remove impurities. Quantitative desorption of 177Lu was achieved by using 6 M HNO3. The developed method of 177Lu pr

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8

Дьячков, А. Б., А. А. Горкунов, А. В. Лабозин та ін. "Исследование схемы селективной фотоионизации -=SUP=-177-=/SUP=-Lu". Журнал технической физики 126, № 2 (2019): 103. http://dx.doi.org/10.21883/os.2019.02.47189.212-18.

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AbstractThe hyperfine structure of transitions in the three-step scheme 5 d 6 s ^22 D _3/2–5 d 6 s 6 p ^4 F $$_{{5/2}}^{^\circ }$$ –5 d 6 s 7 s ^4 D _3/2– (53 375 cm^–1) $$_{{1/2}}^{^\circ }$$ of lutetium ionization is studied for ^175Lu, ^176Lu, and ^177Lu isotopes using the photoionization laser spectroscopy method. Values of the magnetic dipole ( A ) and electric quadrupole ( B ) interaction constants are determined, as well as the energies, the isotope shifts, and the radiative lifetimes for the 5 d 6 s 7 s ^4 D _3/2 and (53 375 cm^–1) $$_{{1/2}}^{^\circ }$$ levels.

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9

Bhardwaj, Rupali, Hubert T. Wolterbeek, Antonia G. Denkova, and Pablo Serra-Crespo. "Modelling of the 177mLu/177Lu radionuclide generator." Applied Radiation and Isotopes 166 (December 2020): 109261. http://dx.doi.org/10.1016/j.apradiso.2020.109261.

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10

Mizukoshi, Yoshihide, Shota Tsuchida, Hiroko Inaba, et al. "Abstract 6024: A novel carbonic anhydrase IX targeting radiopeptide, 64Cu-PD-32766 and 177Lu-PD-32766, exhibit promising theranostic potential in ccRCC tumors." Cancer Research 84, no. 6_Supplement (2024): 6024. http://dx.doi.org/10.1158/1538-7445.am2024-6024.

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Abstract Introduction: Carbonic Anhydrase IX (CA9) is a zinc metalloenzyme that regulates the pH for cell growth. CA9 is considered an attractive target and is upregulated in a variety of cancers, especially, in 95% of clear cell renal cell carcinoma (ccRCC) where there remains a large clinical unmet need despite the availability of several newly approved medicines. PeptiDream has identified PD-32766, a novel macrocyclic peptide, targeting CA9 and can be labeled with radionuclides such as copper (64Cu) and lutetium (177Lu), which enables tumor-specific PET bioimaging and radiotherapy. Here we

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11

Nir-El, Y. "Production of 177Lu by neutron activation of 176Lu." Journal of Radioanalytical and Nuclear Chemistry 262, no. 3 (2004): 563–67. http://dx.doi.org/10.1007/s10967-004-0476-9.

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12

Nir-El, Y. "Production of 177Lu by neutron activation of 176Lu." Journal of Radioanalytical and Nuclear Chemistry 262, no. 3 (2005): 563–67. http://dx.doi.org/10.1007/s10967-005-0476-4.

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13

Zhernosekov, K. P., R. C. Perego, Z. Dvorakova, R. Henkelmann та A. Türler. "Target burn-up corrected specific activity of 177Lu produced via 176Lu(n, γ) 177Lu nuclear reactions". Applied Radiation and Isotopes 66, № 9 (2008): 1218–20. http://dx.doi.org/10.1016/j.apradiso.2008.02.058.

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14

Mansi, Rosalba, Pascale Plas, Georges Vauquelin, and Melpomeni Fani. "Distinct In Vitro Binding Profile of the Somatostatin Receptor Subtype 2 Antagonist [177Lu]Lu-OPS201 Compared to the Agonist [177Lu]Lu-DOTA-TATE." Pharmaceuticals 14, no. 12 (2021): 1265. http://dx.doi.org/10.3390/ph14121265.

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Treatment of neuroendocrine tumours with the radiolabelled somatostatin receptor subtype 2 (SST2) peptide agonist [177Lu]Lu-DOTA-TATE is effective and well-established. Recent studies suggest improved therapeutic efficacy using the SST2 peptide antagonist [177Lu]Lu-OPS201. However, little is known about the cellular mechanisms that lead to the observed differences. In the present in vitro study, we compared kinetic binding, saturation binding, competition binding, cellular uptake and release of [177Lu]Lu-OPS201 versus [177Lu]Lu-DOTA-TATE using HEK cells stably transfected with the human SST2.

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15

Дьячков, А. Б., А. А. Горкунов, А. В. Лабозин та ін. "Исследование лазерной фотоионизации ядерного изомера -=SUP=-177m-=/SUP=-Lu". Журнал технической физики 128, № 1 (2020): 10. http://dx.doi.org/10.21883/os.2020.01.48832.251-19.

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Впервые методом лазерной резонансной фотоионизационной спектроскопии исследована сверхтонкая структура переходов трехступенчатой схемы фотоионизации лютеция 5d6s2 2D3/2--5d6s6p4Fo5/2-- 5d6s7s4D3/2--(53375 cm-1)o1/2 для ядерного изомера 177mLu. В результате определены константы сверхтонкого расщепления и энергии уровней, а также магнитный дипольный и электрический квадрупольный моменты ядра 177mLu. Исследованы изотопические сдвиги спектральных линий изомера по отношению к природным изотопам и 177Lu. Ключевые слова: изотопический сдвиг, сверхтонкая структура, квадрупольный момент.

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16

García-Infantes, F., J. Praena, A. Casanovas, et al. "First high resolution measurement of neutron capture resonances in ¹⁷⁶Yb at the n_TOF CERN facility." EPJ Web of Conferences 284 (2023): 09001. http://dx.doi.org/10.1051/epjconf/202328409001.

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Several international agencies recommend the study of new routes and new facilities for producing radioisotopes with application to nuclear medicine. 177Lu is a versatile radioisotope used for therapy and diagnosis (theranostics) of cancer with good success in neuroendocrine tumours that is being studied to be applied to a wider range of tumours. 177Lu is produced in few nuclear reactors mainly by the neutron capture on 176Lu. However, it could be produced at high-intensity celeratorbased neutron facilities. The energy of the neutrons in accelerator-based neutron facilities is higher than in t

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17

ДЬЯЧКОВ, А. Б., та А. А. ГОРКУНОВ. "ИССЛЕДОВАНИЕ ЛАЗЕРНОЙ СЕЛЕКТИВНОЙ ФОТОИОНИЗАЦИИ ИЗОМЕРА 177MLU ДЛЯ СОЗДАНИЯ ГЕНЕРАТОРА 177MLU/177LU". РАДИОХИМИЯ 64, № 1 (2022): 65–69. http://dx.doi.org/10.31857/s0033831122010063.

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18

de Souza Caldeira Filho, José. "177Lu-DOTATATE: comparative study between 177Lu NRG/Netherlands and 177Lu ORNL/USA." Nuclear Medicine and Biology 37, no. 6 (2010): 691–92. http://dx.doi.org/10.1016/j.nucmedbio.2010.04.030.

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Boinapally, Srikanth, Suresh Alati, Zirui Jiang, et al. "Preclinical Evaluation of a New Series of Albumin-Binding 177Lu-Labeled PSMA-Based Low-Molecular-Weight Radiotherapeutics." Molecules 28, no. 16 (2023): 6158. http://dx.doi.org/10.3390/molecules28166158.

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Prostate-specific membrane antigen (PSMA)-based low-molecular-weight agents using beta(β)-particle-emitting radiopharmaceuticals is a new treatment paradigm for patients with metastatic castration-resistant prostate cancer. Although results have been encouraging, there is a need to improve the tumor residence time of current PSMA-based radiotherapeutics. Albumin-binding moieties have been used strategically to enhance the tumor uptake and retention of existing PSMA-based investigational agents. Previously, we developed a series of PSMA-based, β-particle-emitting, low-molecular-weight compounds

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20

Crudo, José L., José Luis Crudo, Noemí Nevares, and Ana Lopez Bularte. "Experimental production of MSA 177Lu from highly enriched 176Lu." Nuclear Medicine and Biology 37, no. 6 (2010): 717. http://dx.doi.org/10.1016/j.nucmedbio.2010.04.083.

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21

Lin, Min-Ying, Hsin-Hua Hsieh, Jyh-Cheng Chen, et al. "Brachytherapy Approach Using 177Lu Conjugated Gold Nanostars and Evaluation of Biodistribution, Tumor Retention, Dosimetry and Therapeutic Efficacy in Head and Neck Tumor Model." Pharmaceutics 13, no. 11 (2021): 1903. http://dx.doi.org/10.3390/pharmaceutics13111903.

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Brachytherapy can provide sufficient doses to head and neck squamous cell carcinoma (HNSCC) with minimal damage to nearby normal tissues. In this study, the β−-emitter 177Lu was conjugated to DTPA-polyethylene glycol (PEG) decorated gold nanostars (177Lu-DTPA-pAuNS) used in surface-enhanced Raman scattering and photothermal therapy (PTT). The accumulation and therapeutic efficacy of 177Lu-DTPA-pAuNS were compared with those of 177Lu-DTPA on an orthotopic HNSCC tumor model. The SPECT/CT imaging and biodistribution studies showed that 177Lu-DTPA-pAuNS can be accumulated in the tumor up to 15 day

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22

Plas, Pascale, Lorenzo Limana, Denis Carré, et al. "Comparison of the Anti-Tumour Activity of the Somatostatin Receptor (SST) Antagonist [177Lu]Lu-Satoreotide Tetraxetan and the Agonist [177Lu]Lu-DOTA-TATE in Mice Bearing AR42J SST2-Positive Tumours." Pharmaceuticals 15, no. 9 (2022): 1085. http://dx.doi.org/10.3390/ph15091085.

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Limited experiments have compared the treatment effects of repetitive cycles of radiolabelled somatostatin (SST) analogues. In vitro and in vivo experiments were conducted in an AR42J cancer cell model, comparing the antagonist [177Lu]Lu-satoreotide tetraxetan with the agonist [177Lu]Lu-DOTA-TATE in terms of their binding properties, biodistribution, anti-tumour activity and toxicity. Histopathological and immunohistochemical examinations were performed at different timepoints. In the in vitro assays, [177Lu]Lu-satoreotide tetraxetan recognised twice as many SST2 binding sites as [177Lu]Lu-DOT

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23

Hartmann, Holger, Gerd Wunderlich, Margret Schottelius, Hans-Jürgen Wester, Jörg Kotzerke, and Claudia Brogsitter. "Twins in spirit part IV – [177Lu] high affinity DOTATATE." Nuklearmedizin 56, no. 01 (2017): 1–8. http://dx.doi.org/10.3413/nukmed-0860-16-11.

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Summary Aim: Besides the use of somatostatin analogues, small molecules like sunitinib and everolimus as well as conventional chemotherapy, peptide receptor radiotherapy (PRRT) using radiolabelled somatostatin analogues has gained an important role in the treatment of inoperable, metastasized neuroendocrine tumours (NET). There are various radiotracers in use. Based on our experience with the PET tracer [68Ga]DOTA-3-iodo- Tyr3-octreotate ([68Ga]HA-DOTATATE), a DOTATATE derivative with an increased binding affinity to hsst5, the current retrospective analysis is exploring the therapeutic potent

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24

Sharifi, Mehdi, Amir Reza Jalilian, Hassan Yousefnia, Behrouz Alirezapour, Ali Bahrami-Samani, and Samaneh Zolghadri. "Production, quality control, biodistribution and imaging studies of 177Lu-PSMA-617 in breast adenocarcinoma model." Radiochimica Acta 106, no. 6 (2018): 507–13. http://dx.doi.org/10.1515/ract-2017-2874.

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Abstract 177Lu-PSMA-617 therapeutic agent was prepared successfully under optimized condition of pH=4.5, molar ratio of metal to ligand 1:10, temperature of 95°C and 40 min reaction time. 177LuCl3 was obtained with specific activity of 70–80 GBq/mg by the thermal neutron irradiation (5×1013 n cm−2 s−1) of the enriched Lu2O3 (52% 176Lu) samples. The radionuclidic purity of 177LuCl3 (>99%) was checked by a HPGe detector. The radiochemical purities of 177LuCl3 solution and 177Lu-PSMA-617 compound (>98%) were checked by ITLC and HPLC techniques and stability studies were assayed in the prese

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25

Тищенко, Виктория Константиновна, Василий Михайлович Петриев, Александр Викторович Матвеев, Алена Владимировна Федорова та Катерина Андреевна Кузенкова. "Биораспределение <sup>177</sup>Lu-ЭДТМФ — потенциального препарата для радионуклидной терапии костных метастазов". Химико-фармацевтический журнал 56, № 7 (2022): 3–8. http://dx.doi.org/10.30906/0023-1134-2022-56-7-3-8.

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Фосфонаты, меченные бета-излучающими радионуклидами, широко используются в ядерной медицине для паллиативной терапии костных метастазов. Цель работы — изучить биораспределение нового остеотропного соединения на основе N,N,N’,N’-этилендиаминтетракис(метиленфосфоновой кислоты) с 177Lu (177Lu-ЭДТМФ) в организме интактных лабораторных животных. Для оценки стабильности 177Lu-ЭДТМФ in vivo также было исследовано распределение свободного лютеция в виде 177LuCl3. Исследования были выполнены на интактных крысах Wistar. Было установлено, что 177Lu-ЭДТМФ накапливается преимущественно в скелете (22,67 – 5

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Rahbar, Kambiz, Markus Essler, Matthias Eiber, et al. "Time interval between radium-223 (²²³Ra) therapy and Lutetium-177–prostate-specific membrane antigen (¹⁷⁷Lu-PSMA) treatment and outcomes in the RALU study." Journal of Clinical Oncology 41, no. 6_suppl (2023): 73. http://dx.doi.org/10.1200/jco.2023.41.6_suppl.73.

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73 Background: 223Ra and 177Lu-PSMA-617 both prolong overall survival (OS) in different mCRPC settings. The observational, retrospective study, RALU, investigated safety and clinical outcomes of sequential 223Ra/177Lu-PSMA therapy in patients (pts) with mCRPC. This analysis evaluated the association of time interval between 223Ra and 177Lu-PSMA treatments and safety and OS outcomes of 177Lu-PSMA. Methods: Retrospective data were collected from 2021–22 in German nuclear medicine centers for all pts receiving 177Lu-PSMA with prior history of 223Ra therapy. Time intervals were <6 months (mo) (

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27

Lundsten, Sara, Diana Spiegelberg, Nakul R. Raval, and Marika Nestor. "The radiosensitizer Onalespib increases complete remission in 177Lu-DOTATATE-treated mice bearing neuroendocrine tumor xenografts." European Journal of Nuclear Medicine and Molecular Imaging 47, no. 4 (2020): 980–90. http://dx.doi.org/10.1007/s00259-019-04673-1.

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Abstract Purpose 177Lu-DOTATATE targeting the somatostatin receptor (SSTR) is utilized for treatment of neuroendocrine tumors (NETs). Onalespib, a heat shock protein 90 (HSP90) inhibitor, has demonstrated radiosensitizing properties and may thus enhance the effect of 177Lu-DOTATATE. Consequently, the aim of this study was to assess the potential of Onalespib in combination with 177Lu-DOTATATE in vivo and to examine the toxicity profiles of the treatments. Methods 177Lu-DOTATATE selectivity and distribution in NET xenografts were studied using biodistribution and autoradiography. Therapeutic ef

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Zakaly, Hesham MH, Mostafa YA Mostafa, and Micael Zhukovsky. "Biokinetic Model Development of 177Lu-labeled Methylene Diphosphonate as a Radiopharmaceutical Treatment." INTERNATIONAL JOURNAL OF DRUG DELIVERY TECHNOLOGY 12, no. 04 (2022): 1802–7. http://dx.doi.org/10.25258/ijddt.12.4.52.

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177Lu is a lanthanide radionuclide. In recent years, the possibility of applying a drug based on the 177Lu radionuclide as a palliative treatment for bone metastases has increased. 177Lu has many prospects in terms of its applications in nuclear medicine. The high-energy beta particles and the relatively short half-life of the radionuclide are used to provide an effective treatment. In this work, a comparison of organ and tissue doses is performed with two different drugs: 177Lu in an ionic radionuclide form and 177Lu labeled methylene diphosphonate (177Lu-MDP). 177Lu in an ionic form actively

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Wang, Lei, Devon E. Chapple, Hsiou-Ting Kuo, et al. "Novel 177Lu-Labeled [Thz14]Bombesin(6–14) Derivatives with Low Pancreas Accumulation for Targeting Gastrin-Releasing Peptide Receptor-Expressing Cancer." Pharmaceuticals 18, no. 4 (2025): 449. https://doi.org/10.3390/ph18040449.

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Background/Objectives: Gastrin-releasing peptide receptor is a promising target for cancer diagnosis and therapy. However, the high pancreas uptake of reported GRPR-targeted radioligands limits their clinical applications. Our group previously reported one 68Ga-labeled GRPR antagonist, [68Ga]Ga-TacsBOMB5 (68Ga-DOTA-Pip-[D-Phe6,NMe-Gly11,Leu13ψThz14]Bombesin(6–14)), and two agonists, [68Ga]Ga-LW01110 (68Ga-DOTA-Pip-[D-Phe6,Tle10,NMe-His12,Thz14]Bombesin(6–14)) and [68Ga]Ga-LW01142 (68Ga-DOTA-Pip-[D-Phe6,His7,Tle10,NMe-His12,Thz14]Bombesin(6–14)) showing minimal pancreas uptake. Thus, in this st

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30

ANDO, A., I. ANDO, N. TONAMI, et al. "177Lu-EDTMP." Nuclear Medicine Communications 19, no. 6 (1998): 587–92. http://dx.doi.org/10.1097/00006231-199806000-00012.

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Raguin, Olivier, Marcel Krüger, Peggy Provent, et al. "Abstract 5044: Antitumor activity comparison of two somatostatin receptor ligands radiolabeled with Lutetium-177 (SSO110 and DOTA-TATE) alone or combined with chemotherapy in mice bearing AR42J SST2-positive tumors." Cancer Research 83, no. 7_Supplement (2023): 5044. http://dx.doi.org/10.1158/1538-7445.am2023-5044.

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Abstract Only a limited number of studies have compared the therapeutic effects of repetitive cycles of radiolabeled somatostatin (SST) analogues or assessed potential synergy of these analogues with chemotherapy agents. Hence, a comparison was conducted in an in vivo AR42J tumor model with an SST2 antagonist, [177Lu]Lu-satoreotide tetraxetan ([177Lu]LuSSO110), and a SST2 agonist, [177Lu]Lu-DOTA-TATE. The efficacy of treatment combining [177Lu]Lu-satoreotide tetraxetan with capecitabine plus temozolomide was also assessed. Swiss Nude mice were xenografted with AR42J tumor cells. For the evalua

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Kunz, Pamela L., Diego Ferone, Daniel M. Halperin, et al. "Safety and time to response of [¹⁷⁷Lu]Lu-DOTATATE in patients with newly diagnosed advanced grade 2 and grade 3, well-differentiated gastroenteropancreatic neuroendocrine tumors: Sub-analysis of the phase 3 randomized NETTER-2 study." Journal of Clinical Oncology 42, no. 16_suppl (2024): 4131. http://dx.doi.org/10.1200/jco.2024.42.16_suppl.4131.

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4131 Background: NETTER-2 (NCT03972488) is the first randomized study to evaluate radioligand therapy ([177Lu]Lu-DOTA-TATE; hereafter 177Lu-DOTATATE) at first line (1L) in patients (pts) with advanced, well-differentiated higher grade (G2 and G3) gastroenteropancreatic neuroendocrine tumors (GEP-NETs). Significant improvements in progression-free survival and objective response rate (ORR) were observed for pts receiving 177Lu-DOTATATE. This sub-analysis of NETTER-2 assessed safety and time to response (TTR). Methods: Eligible pts (n=226) were newly diagnosed with somatostatin receptor-positive

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Ballal, Sanjana, Madhav Prasad Yadav, Euy Sung Moon, et al. "First-In-Human Results on the Biodistribution, Pharmacokinetics, and Dosimetry of [177Lu]Lu-DOTA.SA.FAPi and [177Lu]Lu-DOTAGA.(SA.FAPi)2." Pharmaceuticals 14, no. 12 (2021): 1212. http://dx.doi.org/10.3390/ph14121212.

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Recently, great interest has been gained regarding fibroblast activation protein (FAP) as an excellent target for theranostics. Several FAP inhibitor molecules such as [68Ga]Ga-labelled FAPI-02, 04, 46, and DOTA.SA.FAPi have been introduced and are highly promising molecular targets from the imaging point of view. FAP inhibitors introduced via bifunctional DOTA and DOTAGA chelators offer the possibility to complex Lutetium-177 due to an additional coordination site, and are suitable for theranostic applications owing to the increased tumor accumulation and prolonged tumor retention time. Howev

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Batra, Jaspreet S., Beerinder S. Karir, Shankar Vallabhajosula, et al. "Fractionated dose radiolabeled antiprostate specific membrane antigen (PSMA) radioimmunotherapy (177Lu-J591) with or without docetaxel for metastatic castration-resistant prostate cancer (mCRPC)." Journal of Clinical Oncology 33, no. 7_suppl (2015): 194. http://dx.doi.org/10.1200/jco.2015.33.7_suppl.194.

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194 Background: A phase II trial single-dose 177Lu-J591 was published. Dose fractionation offers theoretic advantages and 2 phase I dose-escalation studies of 177Lu-J591 have been performed to test the hypothesis that higher cumulative radiation doses can be administered with an acceptable toxicity profile. Methods: Pts with mCRPC and normal neutrophil and platelet counts were enrolled in 2 sequential phase I dose-escalation studies: (1) 177Lu-J591 administered as a single-agent 2 doses 2-weeks apart to determine the maximum tolerated dose (MTD) with expansion cohorts at the recommend phase II

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Rahbar, Kambiz, Markus Essler, Matthias Eiber, et al. "Safety and survival outcomes in patients (pts) with metastatic castration-resistant prostate cancer (mCRPC) treated with lutetium-177–prostate-specific membrane antigen (¹⁷⁷Lu-PSMA) after radium-223 (²²³Ra): Interim analysis of the RALU study." Journal of Clinical Oncology 40, no. 16_suppl (2022): 5040. http://dx.doi.org/10.1200/jco.2022.40.16_suppl.5040.

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5040 Background: 223Ra and 177Lu-PSMA both prolong overall survival (OS) in different mCRPC settings. Previous data from the observational REASSURE (Sartor O, et al. 2021) and WARMTH (Ahmadzadehfar H, et al. 2021) studies suggested the feasibility of sequencing 223Ra and 177Lu-PSMA therapies. Here we used data from the observational, retrospective RALU study to further examine the safety and clinical outcomes of sequential 223Ra/177Lu-PSMA therapy in pts with mCRPC. Methods: This interim analysis investigated the baseline characteristics, safety (primary endpoint) and OS (secondary endpoint) i

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Rahbar, Kambiz, Markus Essler, Matthias Eiber, et al. "Safety and survival outcomes in patients (pts) with metastatic castration-resistant prostate cancer (mCRPC) treated with lutetium-177–prostate-specific membrane antigen (¹⁷⁷Lu-PSMA) after radium-223 (²²³Ra): Interim analysis of the RALU study." Journal of Clinical Oncology 40, no. 16_suppl (2022): 5040. http://dx.doi.org/10.1200/jco.2022.40.16_suppl.5040.

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5040 Background: 223Ra and 177Lu-PSMA both prolong overall survival (OS) in different mCRPC settings. Previous data from the observational REASSURE (Sartor O, et al. 2021) and WARMTH (Ahmadzadehfar H, et al. 2021) studies suggested the feasibility of sequencing 223Ra and 177Lu-PSMA therapies. Here we used data from the observational, retrospective RALU study to further examine the safety and clinical outcomes of sequential 223Ra/177Lu-PSMA therapy in pts with mCRPC. Methods: This interim analysis investigated the baseline characteristics, safety (primary endpoint) and OS (secondary endpoint) i

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Busslinger, Sarah D., Anna E. Becker, Christian Vaccarin, et al. "Investigations Using Albumin Binders to Modify the Tissue Distribution Profile of Radiopharmaceuticals Exemplified with Folate Radioconjugates." Cancers 15, no. 17 (2023): 4259. http://dx.doi.org/10.3390/cancers15174259.

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Introducing an albumin-binding entity into otherwise short-lived radiopharmaceuticals can be an effective means to improve their pharmacokinetic properties due to enhanced blood residence time. In the current study, DOTA-derivatized albumin binders based on 4-(p-iodophenyl)butanoate (DOTA-ALB-1 and DOTA-ALB-3) and 5-(p-iodophenyl)pentanoate entities (DOTA-ALB-24 and DOTA-ALB-25) without and with a hydrophobic 4-(aminomethyl)benzoic acid (AMBA) linker unit, respectively, were synthesized and labeled with lutetium-177 for in vitro and in vivo comparison. Overall, [177Lu]Lu-DOTA-ALB-1 demonstrate

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Ranzani, Marco, Sravanth Hindupur, Alessandro Cicconi, et al. "Abstract LB222: Elucidating the cellular responses and mechanism of action of 177Lu-based radioligand therapy." Cancer Research 84, no. 7_Supplement (2024): LB222. http://dx.doi.org/10.1158/1538-7445.am2024-lb222.

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Abstract Radioligand therapy (RLT) is emerging as a safe and effective targeted approach for treating several types of cancers. Lutathera® (177Lu-Dotatate) and Pluvicto® (177Lu-PSMA-617) are two examples of FDA-approved 177Lu-based RLT drugs for the treatment of somatostatin receptor-positive gastroenteropancreatic neuroendocrine tumors (GEP-NETs) and of PSMA-positive metastatic castration-resistant prostate cancer (mCRPC), respectively. Despite the clinical success of 177Lu-RLT, there are still patients lacking complete, durable responses. Arguably, elucidating the cellular responses to 177Lu

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Dias, Gemma, Sarah Able, Irini Skaripa-Koukelli, Rachel Anderson, Gracie Wilson, and Katherine A. Vallis. "Abstract 5038: Evaluation of anti-tumor immunity in response to [177Lu]Lu-PSMA in a mouse model of prostate cancer." Cancer Research 83, no. 7_Supplement (2023): 5038. http://dx.doi.org/10.1158/1538-7445.am2023-5038.

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Abstract [177Lu]Lu-PSMA improves progression-free and overall survival in metastatic castration resistant prostate cancer. However, the role of immune stimulation by molecularly targeted radionuclide therapy (MRT) is poorly understood. The aim of this study was to evaluate the anti-tumor immune response induced by [177Lu]Lu-PSMA. The markers of immunogenic cell death (ICD), translocation of calreticulin (CRT) to the cell membrane, HMGB1 release and ATP release, were evaluated in the RM1 cell line (PSMA-negative murine prostate carcinoma) and its derivative, RM1-PGLS (stably transduced with hum

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Yang, Guangjie, Hannan Gao, Chuangwei Luo та ін. "Palmitic Acid-Conjugated Radiopharmaceutical for Integrin αvβ3-Targeted Radionuclide Therapy". Pharmaceutics 14, № 7 (2022): 1327. http://dx.doi.org/10.3390/pharmaceutics14071327.

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Peptide receptor radionuclide therapy (PRRT) is an emerging approach for patients with unresectable or metastatic tumors. Our previously optimized RGD peptide (3PRGD2) has excellent targeting specificity for a variety of integrin αvβ3/αvβ5-positive tumors and has been labeled with the therapeutic radionuclide [177Lu]LuCl3 for targeted radiotherapy of tumors. However, the rapid clearance of [177Lu]Lu-DOTA-3PRGD2 (177Lu-3PRGD2) in vivo requires two doses of 111 MBq/3 mCi to achieve effective tumor suppression, limiting its further clinical application. Albumin binders have been attached to drugs

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Hänscheid, Heribert, Philipp E. Hartrampf, Andreas Schirbel, Andreas K. Buck, and Constantin Lapa. "Intraindividual comparison of [177Lu]Lu-DOTA-EB-TATE and [177Lu]Lu-DOTA-TOC." European Journal of Nuclear Medicine and Molecular Imaging 48, no. 8 (2021): 2566–72. http://dx.doi.org/10.1007/s00259-020-05177-z.

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Abstract Purpose The radiolabelled somatostatin analogue [177Lu]Lu-DOTA-EB-TATE binds to albumin via Evans blue, thereby increasing the residence time in the blood and potentially allowing more therapeutic agent to be absorbed into the target tissue during peptide receptor radionuclide therapy. It was tested in selected patients whether the substance is superior to [177Lu]Lu-DOTA-TOC. Methods Activity kinetics in organs and tumours after [177Lu]Lu-DOTA-EB-TATE and [177Lu]Lu-DOTA-TOC were compared intraindividually in five patients with progressive somatostatin receptor-positive disease schedul

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Xu, Junhua, Song Wan, Wei Chen, Yi Zhang, and Zhenzhong Ji. "Relaxin inhibits ¹⁷⁷Lu-EDTMP associated cell death in osteosarcoma cells through notch-1 pathway." Acta Pharmaceutica 72, no. 4 (2022): 575–85. http://dx.doi.org/10.2478/acph-2022-0032.

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Abstract 177Lu-EDTMP (Ethylenediamine tetramethylene phosphonic acid) is the most used radioactive agent for pain palliation in bone cancer patients. The present study aims to study the impact of relaxin-2 on the 177Lu-EDTMP associated cell toxicity and death in osteosarcoma cells. MG63 and Saos-2 cells were cultured with 177Lu-EDTMP (37 MBq) for 24 h with and without pretreatment of recombinant relaxin 2 (RLXH2) for 12 and 24 h. 177Lu-EDTMP associated cellular deterioration and death was determined by LDH, MTT, and trypan blue dye assays. ELISA-based kit was used to determine apoptotic DNA fr

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Ytterbrink, Charlotte, Emman Shubbar, Toshima Z. Parris та ін. "Effects of Recombinant α1-Microglobulin on Early Proteomic Response in Risk Organs after Exposure to 177Lu-Octreotate". International Journal of Molecular Sciences 25, № 13 (2024): 7480. http://dx.doi.org/10.3390/ijms25137480.

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Recombinant α1-microglobulin (A1M) is proposed as a protector during 177Lu-octreotate treatment of neuroendocrine tumors, which is currently limited by bone marrow and renal toxicity. Co-administration of 177Lu-octreotate and A1M could result in a more effective treatment by protecting healthy tissue, but the radioprotective action of A1M is not fully understood. The aim of this study was to examine the proteomic response of kidneys and bone marrow early after 177Lu-octreotate and/or A1M administration. Mice were injected with 177Lu-octreotate and/or A1M, while control mice received saline or

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Guleria, Mohini, Jeyachitra Amirdhanayagam, Haladhar D. Sarma, et al. "Preparation of 177Lu-PSMA-617 in Hospital Radiopharmacy: Convenient Formulation of a Clinical Dose Using a Single-Vial Freeze-Dried PSMA-617 Kit Developed In-House." BioMed Research International 2021 (November 20, 2021): 1–12. http://dx.doi.org/10.1155/2021/1555712.

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Objective. In the recent time, endoradionuclide therapy for metastatic castration-resistant prostate carcinoma employing 177Lu-PSMA-617 has yielded encouraging results and several clinical trials with the agent are currently ongoing. Routine preparation of 177Lu-PSMA-617 patient doses can be made simpler and convenient, if the ingredients essential for radiolabeling are made available in a ready-to-use lyophilized form. Methods. PSMA-617 freeze-dried kit was formulated and used for the preparation of 177Lu-PSMA-617 clinical dose with high radiochemical purity using low/medium specific activity

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Nguyen, Jennifer, Jeetvan Patel, Barinder Kang, et al. "Patient characteristics, treatment patterns and early trends of lutetium Lu 177 vipivotide tetraxetan (¹⁷⁷Lu-PSMA-617) use by US urologists and oncologists." Journal of Clinical Oncology 42, no. 16_suppl (2024): e17048-e17048. http://dx.doi.org/10.1200/jco.2024.42.16_suppl.e17048.

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e17048 Background: 177Lu-PSMA-617 was approved by the US Food and Drug Administration in March 2022 for the treatment of patients with prostate-specific membrane antigen (PSMA) positive metastatic castration resistant prostate cancer (mCRPC) who have been treated with androgen receptor pathway inhibition (ARPI) and taxane-based chemotherapy. This study describes characteristics of patients treated with 177Lu-PSMA-617, treatment patterns and early trends in 177Lu-PSMA-617 utilization by US urologists (URO) and medical oncologists (ONC). Methods: This retrospective cohort study identified adult

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Strosberg, Jonathan R., Edward M. Wolin, Beth Chasen, et al. "Quality-of-life findings in patients with midgut neuroendocrine tumors: Results of the NETTER-1 phase III trial." Journal of Clinical Oncology 35, no. 4_suppl (2017): 348. http://dx.doi.org/10.1200/jco.2017.35.4_suppl.348.

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348 Background: Neuroendocrine tumor progression is associated with decline in quality of life, both due to tumor and hormone-related symptoms. The Phase III NETTER-1 trial randomized patients with advanced, progressive midgut NETs to receive treatment with 177Lu-DOTATATE (177Lu; Lutathera) versus high-dose (60 mg) Octreotide LAR (Oct). EORTC questionnaires C30 and GINET21 were assessed during the trial in order to determine the impact of treatment on health-related quality of life (HRQoL). Methods: Patients completed EORTC QLQ-30 and QLQ-G.I.NET21 questionnaires at baseline and every 12 weeks

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Sartor, A. Oliver, Christian la Fougère, Markus Essler, et al. "Disease characteristics and outcome of patients (pts) with metastatic castration-resistant prostate cancer (mCRPC) who received a beta emitter (177Lu-PSMA) after an alpha emitter (radium-223)." Journal of Clinical Oncology 38, no. 15_suppl (2020): e17592-e17592. http://dx.doi.org/10.1200/jco.2020.38.15_suppl.e17592.

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e17592 Background: Ra-223, a targeted alpha therapy, showed an overall survival (OS) benefit and favorable safety profile in mCRPC pts in a phase 3 trial. 177Lu-PSMA radioligand is an investigational agent for mCRPC. REASSURE (NCT02141438) is a global, prospective, observational study investigating Ra-223 safety in routine clinical practice over 7 years’ follow-up in mCRPC pts. Data from the second prespecified interim analysis (IA) were used to investigate safety and outcomes of pts who received 177Lu-PSMA after Ra-223 therapy. Methods: Data cut-off for the second prespecified IA was March 20

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Deberle, Luisa M., Viviane J. Tschan, Francesca Borgna, et al. "Albumin-Binding PSMA Radioligands: Impact of Minimal Structural Changes on the Tissue Distribution Profile." Molecules 25, no. 11 (2020): 2542. http://dx.doi.org/10.3390/molecules25112542.

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The concept of using ibuprofen as an albumin-binding entity was recently demonstrated by the development of [177Lu]Lu-Ibu-PSMA-01. In the present study, we designed a novel ibuprofen-containing radioligand (Ibu-PSMA-02) with subtle structural changes regarding the linker entity in order to investigate a potential impact on the in vitro and in vivo properties. Ibu-PSMA-02 was prepared using solid-phase synthesis techniques and labeled with lutetium-177. [177Lu]Lu-Ibu-PSMA-02 was evaluated in vitro with regard to its plasma protein-binding properties, PSMA affinity and uptake into PSMA-expressin

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Wu, Yitian, Xiaojun Zhang, Xiaojiang Duan, Xing Yang, Feng Wang, and Jinming Zhang. "Optimized Therapeutic 177Lu-Labeled PSMA-Targeted Ligands with Improved Pharmacokinetic Characteristics for Prostate Cancer." Pharmaceuticals 15, no. 12 (2022): 1530. http://dx.doi.org/10.3390/ph15121530.

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Clinical trials have shown the significant efficacy of [177Lu]Lu-PSMA-617 for treating prostate cancer. However, the pharmacokinetic characteristics and therapeutic performance of [177Lu]Lu-PSMA-617 still need further improvement to meet clinical expectations. The aim of this study was to evaluate the feasibility and therapeutic potential of three novel 177Lu-labeled ligands for the treatment of prostate cancer. The novel ligands were efficiently synthesized and radiolabeled with non-carrier added 177Lu; the radiochemical purity of the final products was determined by Radio-HPLC. The specific

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Li, Hongmei, Tingting Xu, Qingchu Hua, Li Wang, and Yue Chen. "177Lu-DOTA-IBA Therapy in Prostate Cancer With Bone Metastases." Clinical Nuclear Medicine 48, no. 8 (2023): 740–42. http://dx.doi.org/10.1097/rlu.0000000000004717.

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Abstract Bone is the most common metastatic site in patients with prostate cancer. 177Lu-DOTA-ibandronic acid (177Lu-DOTA-IBA) is a new therapeutic radiopharmaceutical targeting bone metastasis. We report a case of refractory bone pain due to bone metastasis, who demonstrated an excellent therapy response after 3 cycles of 177Lu-DOTA-IBA therapy. In addition, the patient did not have any observable adverse reactions. 177Lu-DOTA-IBA may be a promising radiopharmaceutical for the treatment of bone metastasis.

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