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Significant reduction of activity retention in the kidneys via optimized linker sequences in radiohybrid-based minigastrin analogs
BackgroundWe recently introduced radiohybrid (rh)-based minigastrin analogs e.g., DOTA-rhCCK-18 (DOTA-D-Dap(p-SiFA)-(D-γ-Glu) 8 -Ala-Tyr-Gly-Trp-Nle-Asp-Phe-NH...
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Investigation of the structure-activity relationship at the N-terminal part of minigastrin analogs
BackgroundOver the last years, several strategies have been reported to improve the metabolic stability of minigastrin analogs. However, currently...
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Synthesis and preclinical evaluation of novel 99mTc-labeled PSMA ligands for radioguided surgery of prostate cancer
BackgroundRadioguided surgery (RGS) has recently emerged as a valuable new tool in the management of recurrent prostate cancer (PCa). After...
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Postmortem redistribution of drugs: a literature review
Postmortem drug analysis is crucial in identifying the potential cause and manner of death. However, it is threatened by a significant phenomenon...
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Development of a novel 18F-labeled small molecule probe for PET imaging of mesenchymal epithelial transition receptor expression
AbstractThe mesenchymal epithelial transition factor (c-Met) is frequently overexpressed in numerous cancers and has served as a validated anticancer...
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Development and first-in-human study of PSMA-targeted PET tracers with improved pharmacokinetic properties
PurposeA series of new 68 Ga-labeled tracers based on [ 68 Ga]Ga-PSMA-617 were developed to augment the tumor-to-kidney ratio and reduce the activity...
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Predictive Potential of Acido-Basic Properties, Solubility and Food on Bioequivalence Study Outcome: Analysis of 128 Studies
Background and ObjectivesRisk assessment related to bioequivalence study outcome is critical for effective planning from the early stage of drug...
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Synthesis and preclinical evaluation of novel 18F-vancomycin-based tracers for the detection of bacterial infections using positron emission tomography
IntroductionBacterial infections are a major problem in medicine, and the rapid and accurate detection of such infections is essential for optimal...
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99mTc-labeled FAPI compounds for cancer and inflammation: from radiochemistry to the first clinical applications
BackgroundIn recent years, fibroblast activating protein (FAP), a biomarker overexpressed by cancer-associated fibroblasts, has emerged as one of the...
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Translational imaging of the fibroblast activation protein (FAP) using the new ligand [68Ga]Ga-OncoFAP-DOTAGA
PurposeThe fibroblast activation protein (FAP) is an emerging target for molecular imaging and therapy in cancer. OncoFAP is a novel small organic...
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Efficacy and Safety of Naftifine Hydrochloride 2% Gel in Interdigital Tinea Pedis: A Phase III Randomised, Double-Blind, Parallel-Group, Active-Controlled Study in Indian Adult Patients
Background and ObjectiveNaftifine, an allylamine, is highly effective against tinea pedis and exhibits relatively greater affinity to skin and nail...
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The Role of Patch Testing in Evaluating Delayed Hypersensitivity Reactions to Medications
Confirming drug imputability is an important step in the management of cutaneous adverse drug reactions (CADR). Re-challenge is inconvenient and in...
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Translocator protein (18 kDa) positron emission tomography imaging as a biomarker of neuroinflammation in epilepsy
Increasing evidence indicate that neuroinflammation triggered by glial cells plays a significant role in epileptogenesis. To this effect, the...
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Predictions of Bedaquiline Central Nervous System Exposure in Patients with Tuberculosis Meningitis Using Physiologically based Pharmacokinetic Modeling
Background and ObjectiveThe use of bedaquiline as a treatment option for drug-resistant tuberculosis meningitis (TBM) is of interest to address the...
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Synthesis and Biological Evaluation of [18F]FECNT-d4 as a Novel PET Agent for Dopamine Transporter Imaging
PurposeThe dopamine transporter (DAT) is a marker of the occurrence and development of Parkinson’s disease (PD) and other diseases with nigrostriatal...
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Synthesis and in vitro and in vivo evaluation of urea-based PSMA inhibitors with increased lipophilicity
BackgroundSeveral radiolabeled prostate-specific membrane antigen (PSMA) inhibitors based on the lysine-urea-glutamate (KuE) motif as the...
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A radiohybrid theranostics ligand labeled with fluorine-18 and lutetium-177 for fibroblast activation protein-targeted imaging and radionuclide therapy
PurposeA series of radiotracers targeting fibroblast activation protein (FAP) with great pharmacokinetics have been developed for cancer diagnosis...
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Synthesis and evaluation of fluorine-18 labelled tetrazines as pre-targeting imaging agents for PET
BackgroundThe brain is a challenging target for antibody-based positron emission tomography (immunoPET) imaging due to the restricted access of...
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Small peptide-based GLP-1R ligands: an approach to reduce the kidney uptake of radiolabeled GLP-1R-targeting agents?
AimElevated kidney uptake in insulinoma patients remains a major limitation of radiometallated exendin-derived ligands of the glucagon-like peptide 1...