Khatun S, Rezazadeh F, Deck AJ, Kulasekara DN et al.
Abstract Purpose: TRA-1-60 (TRA) is an established cancer stemness marker implicated in tumor initiation, therapeutic resistance, and disease relapse. It is minimally expressed in normal differentiated tissues, making it an appealing biomarker for immunopositron emission tomography (immunoPET) imaging and radiopharmaceutical therapy (RPT). Full-length monoclonal antibodies (mAb…
Fibroblast activation protein-α (FAP) is an attractive cell surface target for radiopharmaceutical development due to its tumor-restricted expression. This study aimed to develop a novel dimeric FAP inhibitor (FAPI), DOTA-PEG4-CO-N-bis(PEG4-7N) (D7ND), and evaluate its potential as a therapeutic radiopharmaceutical in preclinical models and clinical studies. The precursor D7ND …
Fibroblast activation protein (FAP) and integrin αvβ3 are attractive theranostic targets. We developed a dual-targeting radiotheranostic agent, 177Lu-DOTA-FAPI-RGD (177Lu-LNC1009), and conducted a first-in-human study to evaluate its safety, biodistribution, dosimetry, and preliminary efficacy in patients with advanced adenocarcinomas. Methods: LNC1009 was synthesized by conjug…
Rebecca Green, Alba Fernández‐Sanlés, Caterina Felici, Charlotte Warren‐Gash et al.
Abstract APOE genotype is a very strong genetic risk factor for late-onset Alzheimer’s disease (AD). This relationship may involve mediation by common infections—several of which are also dementia risk factors. We investigated associations of APOE ε2 and ε4 carriage with serostatus and antibody titres to 14 common pathogens in three population-based cohorts (UK Biobank, Nationa…
Glucagon-like peptide-1 receptor (GLP-1R) is a clinically validated therapeutic target for the treatment of obesity and type 2 diabetes. GLP-1Rs expressed in the central nervous system (CNS) regulate appetite and are therefore particularly important in the context of weight loss. There is thus an emerging need for efficient and brain-penetrating Positron Emission Tomography (PE…
Targeted radiopharmaceutical development for ovarian cancer (OC) has been limited by the lack of molecular targets that combine broad tumor expression with minimal normal-tissue distribution. TRA-1-60 (TRA) is a cancer-associated glycoepitope carried by podocalyxin. Here, we evaluated TRA as a target for OC and developed a TRA-directed immunoPET imaging platform. Immunohistoche…
Kraihammer M, Decristoforo C, Knoll A, Zavvar TS et al.
Abstract Background We report on comparison of two automated production processes for radiolabelling and formulation of three different radiopharmaceuticals [ 177 Lu]Lu-PSMA I&T, [ 177 Lu]Lu-DOTA-TATE and [ 90 Y]Y-DOTA-TOC. These processes were evaluated with and without C-18 solid phase extraction purification. Methods Radiopharmaceuticals were produced and formulated using si…
Romero-Zayas I, de Arcocha-Torres M, Peñuelas I, Martínez Montalbán E et al.
This guide outlines the radiopharmaceutical procedure for the in vitro labelling of leukocytes. Scintigraphy using leukocytes labeled with [99mTc]Tc-exametazime or [111In]In-oxine is a highly valuable diagnostic tool in infectious and inflammatory diseases due to its high sensitivity and specificity. It is based on established guidelines and consensus protocols, which incorpora…
Mizuno HL, Miyao S, Takahashi H, Akimitsu N et al.
BackgroundRadioactive isotopes, such as Indium-111 (111In), are pivotal for highly sensitive noninvasive imaging and targeted radiotherapy. However, achieving stable in vivo retention remains a critical barrier. Conventional nanocarriers typically rely on surface-bound chelators, exposing the isotopes to biological transchelation and detachment, while potentially altering the c…
Chronic neuropathic pain represents a significant global health burden and is hypothesized to be maintained by an altered astrocyte-neuron interplay. Evidence of astrocyte contributions to neuropathic pain are derived from both post-mortem immunohistochemical analyses and in vivo pharmacological studies. These data cannot provide insights into dynamic changes in astrocytes with…
ObjectivesHospital radiopharmacy plays a central role in ensuring the quality, safety and regulatory compliance of radiopharmaceuticals used for diagnostic and therapeutic purposes. Given the complexity and multidisciplinary nature of the radiopharmaceutical circuit, professional practice evaluation represents a key tool for continuous quality improvement. This study aimed to e…
Background: Hepatocellular carcinoma (HCC) remains the major cause of cancer-related mortality worldwide due to high postoperative recurrence rates and limited treatment options for minimal residual disease (MRD).Methods: In this study, glypican-3 (GPC3)-targeted radiopharmaceutical, 177Lu-DOTA-GPC3, was developed and evaluated as a potential adjuvant targeted radionuclide ther…
Maintenance-induced configuration drift detected during a 3-lot validation study is described, highlighting the role of nuclear medicine technologists and site engineers in its resolution. A radio-high-performance liquid chromatography system was used during validation of a new positron-emitting radiopharmaceutical. After routine maintenance, reduced peak intensity was observed…
Claude G, Balzer M, Brenner W, Bruchertseifer F et al.
BackgroundAnalytical data for 225Ac-labeled radiopharmaceuticals are currently obtained using thin-layer chromatography and high-performance liquid chromatography, the latter followed by offline fraction collection and delayed gamma-counting after secular equilibrium with gamma-emitting daughters has been reached. These procedures are slow and do not depict the distribution of …
BackgroundHitherto, clinically applied 99mTc-based cholecystokinin-2 receptor (CCK-2R) ligands suffer from limited in vivo stability. Therefore, we focused on the development of pharmacokinetically optimized 99mTc-labeled CCK-2R ligands for improved imaging of CCK-2R-overexpressing malignancies via single-photon emission computed tomography (SPECT). The novel CCK-2R ligands wer…
Building upon our previous work on [68Ga]Ga/[177Lu]Lu-DOTA-Ibandronate and its demonstrated clinical applicability, this study investigates the biological behavior and translational potential of the novel therapeutic radiopharmaceutical terbium-161 (161Tb)-labeled DOTA-IBA. The radiolabeling parameters of [161Tb]Tb-DOTA-IBA were first optimized, followed by a systematic assessm…
Itaconic acid (ITA), a naturally occurring dicarboxylic acid, demonstrates potent antibacterial and anti-inflammatory activity. Differentiating bacterial infections from sterile inflammation remains a significant clinical challenge, necessitating the development of specific diagnostic radiopharmaceuticals. This research presents the radiolabeling of ITA with technetium-99m (99m…
BackgroundEpidermal Growth Factor Receptor (EGFR) overexpression in Head and Neck Squamous Cell Carcinoma (HNSCC) is well documented and strongly correlated with aggressive phenotypes. As such EGFR is an excellent choice for molecular imaging of HNSCC as the high overexpression levels allow for a specific marker of tumors. Currently the only established EGFR radiopharmaceutical…
Background4-Borono-2-[18F]fluorophenylalanine ([18F]FBPA) is an important imaging agent for identifying suitable candidates for boron neutron capture therapy (BNCT). This study aimed to develop three new precursors for the no-carrier-added synthesis of [18F]FBPA and to establish corresponding automated radiosynthesis protocols suitable for routine production.ResultsFollowing ma…
Introduction/objectivesThis study aimed to develop a Technetium-99m-labeled nano-structured lipid carrier (Tc-99m-IMT-NSLC) system for passive targeted imaging of colon cancer and to theoretically characterize its dosimetric properties using computational modeling.MethodsNano-Structured Lipid Carriers (NSLCs) loaded with Imatinib were prepared and radiolabeled with Tc-99m. The …
BackgroundThe clinical translation of molecularly targeted therapeutics and imaging agents represents a cornerstone of precision oncology, with the global theranostics market projected to exceed $25 billion by 2030. However, the development of theragnostic agents or diagnostic companions remains constrained by analytical bottlenecks in quality control, such as target-binding fr…
BackgroundGallium-68 (68Ga) is a PET isotope that is finding more use in the clinical setting as a PET diagnostic tool, for example 68Ga PSMA is widely used in the diagnosis of prostate cancer, and 68Ga dotatate for the diagnosis of neuroendocrine tumors. Current production is mostly performed using either 68Ge/68Ga generators or liquid targets containing 68Zn and irradiated wi…
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