Dosimetric Analysis of a Phase I Study of PSMA-Targeting Radiopharmaceutical Therapy With [Lu]Ludotadipep in Patients With Metastatic Castration-Resistant Prostate Cancer.

Objective: Lutetium [Lu] Ludotadipep is a novel prostate-specific membrane antigen targeting therapeutic agent with an albumin motif added to increase uptake in the tumors. We assessed the biodistribution and dosimetry of [Lu]Ludotadipep in patients with metastatic castration-resistant prostate cancer (mCRPC).

Materials And Methods: Data from 25 patients (median age, 73 years; range, 60-90) with mCRPC from a phase I study with activity escalation design of single administration of [Lu]Ludotadipep (1.

A Single Dose of Novel PSMA-Targeting Radiopharmaceutical Agent [Lu]Ludotadipep for Patients with Metastatic Castration-Resistant Prostate Cancer: Phase I Clinical Trial.

[Lu]Ludotadipep, which enables targeted delivery of beta-particle radiation to prostate tumor cells, had been suggested as a promising therapeutic option for mCRPC. From November 2020 to March 2022, a total of 30 patients were enrolled for single dose of [Lu]Ludotadipep RPT, 6 subjects in each of the 5 different activity groups of 1.9 GBq, 2.

Feasibility of Gd-Based prostate cancer targeted magnetic resonance agents using prostate specific membrane antigen.

The aim of this work was to evaluate Gd-FC705, a prostate-specific membrane antigen (PSMA)-targeted MRI contrast agent. The r and r relaxivities of Gd-FC705 are 5.94 mMs and 17.

Improving Theranostic Gallium-68/Lutetium-177-Labeled PSMA Inhibitors with an Albumin Binder for Prostate Cancer.

We developed a novel therapeutic radioligand, [Lu], with an albumin binding motif and evaluated it in a prostate-specific membrane antigen (PSMA)-expressing tumor xenograft mouse model. Fourteen PSMA target candidates were synthesized, and binding affinity was evaluated with an competitive binding assay. First, four compound candidates were selected depending on binding affinity results.

F-labeled 1,2,3-triazole-linked Glu-urea-Lys-based PSMA ligands have good pharmacokinetic properties for positron emission tomography imaging of prostate cancer.

Background: Prostate-specific membrane antigen (PSMA) is increasingly recognized as an excellent target for prostate cancer imaging and therapy. Finding compounds with a high target-to-nontarget ratio are an important challenge in the development of positron emission tomography (PET) imaging agents. In this study, we attempted to find a suitable compound from a simply-synthesized compound library.

A microdose clinical trial to evaluate [F]Florastamin as a positron emission tomography imaging agent in patients with prostate cancer.

Purpose: To evaluate the biodistribution of [F]Florastamin, a novel F-labelled positron emission tomography (PET) tracer for prostate-specific membrane antigen (PSMA) for the diagnosis of prostate cancer.

Methods: PET was performed for five healthy controls and 10 patients with prostate cancer at 0, 10, 30, 70, and 120 mins after injecting 370 MBq of [F]Florastamin. The maximum standardised uptake value (SUV) was evaluated in the primary tumour.

The correlation of neuropsychological evaluation with 11C-PiB and 18F-FC119S amyloid PET in mild cognitive impairment and Alzheimer disease.

For the diagnosis of mild cognitive impairment (MCI) and Alzheimer disease (AD), variable neuroimaging and neuropsychological tests have been used. We aimed to evaluate the correlation of neuropsychological domain with new amyloid positron emission tomography (PET) study and to validate the availability of new PET tracer.We enrolled 20 patients who underwent C-PiB-PET/CT, new PET tracer F-FC119S PET/CT from November, 2014 to July, 2015.

Early Detection of A Deposition in the 5xFAD Mouse by Amyloid PET.

F-FC119S is a positron emission tomography (PET) tracer for imaging -amyloid (A) plaques in Alzheimer's disease (AD). The aim of this study is to evaluate the efficacy of F-FC119S in quantitating A deposition in a mouse model of early amyloid deposition (5xFAD) by PET. .

Preliminary PET Study of F-FC119S in Normal and Alzheimer's Disease Models.

To evaluate the efficacy of F-FC119S as a positron emission tomography (PET) radiopharmaceutical for the imaging of Alzheimer's disease (AD), we studied the drug absorption characteristics and distribution of F-FC119S in normal mice. In addition, we evaluated the specificity of F-FC119S for β-amyloid (Aβ) in the AD group of an APP/PS1 mouse model and compared it with that in the wild-type (WT) group. The behavior of F-FC119S in the normal mice was characteristic of rapid brain uptake and washout patterns.

Head-to-head comparison of 11C-PiB and 18F-FC119S for Aβ imaging in healthy subjects, mild cognitive impairment patients, and Alzheimer's disease patients.

As a new beta amyloid (Aβ) positron emission tomography (PET) tracer, F-FC119S has shown higher cortical uptake in patients with Alzheimer's disease (AD) than that in healthy control subjects without adverse effects in a previous preliminary study. The aim of this study was to compare F-FC119S PET and C-PiB PET in healthy control (HC) subjects, mild cognitive impairment (MCI) patients, and AD patients.A total of 48 subjects, including 28 HC subjects, 10 MCI patients, and 10 AD patients, underwent static F-FC119S PET (30 minutes after intravenous [i.

Synthesis and evaluation of 6-(3-[(18)F]fluoro-2-hydroxypropyl)-substituted 2-pyridylbenzothiophenes and 2-pyridylbenzothiazoles as potential PET tracers for imaging Aβ plaques.

3-[(18)F]Fluoro-2-hydroxypropyl substituted compounds were synthesized and evaluated as novel (18)F-labeled PET tracers for imaging Aβ plaque in a living brain. All compounds exhibited high binding affinities toward the synthetic Aβ1-42 aggregate and/or Alzheimer's disease brain homogenate. In the microPET study with normal mice, the 3-[(18)F]fluoro-2-hydroxypropyl substituted compounds resulted in fast brain washout by reducing the lipophilicities of the compounds.

Alternative synthesis for the preparation of 16α-[(18) F]fluoroestradiol.

We have developed a new precursor, 3,17β-O-bis(methoxymethyl)-16β-O-p-nitrobenzenesulfonylestriol (14c) of 16α-[(18) F]fluoroestradiol ([(18) F]FES). Although we could not selectively protect the C17 alcohol in the presence of the C16 alcohol, we were able to prepare and chromatographically isolate the desired C16 TBDMS, C17,C3-dimethoxymethyl (diMOM) protected estriol derivative and convert into the ultimate fluorination precursor. The MOM protective group proved to be more quickly removed than the cyclic sulfate group.

Copper nitride nanoparticles supported on a superparamagnetic mesoporous microsphere for toxic-free click chemistry.

Copper nitride nanoparticles supported on a mesoporous superparamagnetic silica microsphere exhibit superior activity toward the Huisgen cycloaddition of azides and alkynes. The nitride catalyst offers significant advantages over homogeneous Cu catalysts.