Current radiopharmaceuticals最新文献

{"title":"Guideline Adherence as an Indicator of PET Scan Overuse in an Italian Teaching Hospital: An Observational Study.","authors":"Giuseppe Lucio Cascini, Marianna Mauro, Barbara Catalfamo, Monica Giancotti, Roberta Muraca","doi":"10.2174/0118744710290906240408094829","DOIUrl":"10.2174/0118744710290906240408094829","url":null,"abstract":"<p><strong>Background: </strong>Evidence of inappropriate overuse and underuse of medical procedures has been documented in modern healthcare systems around the world. Excessive use of health services can contribute to a rapid increase in healthcare costs and harm the patient physically and psychologically; conversely, underuse can lead to the inability to provide effective treatments when clinically indicated.</p><p><strong>Objective: </strong>The study's aim is twofold: a) to measure the appropriateness of PET prescription in a cohort of patients, offering empirical evidence of overuse of health care services; b) to evaluate how the overuse of PET could affect public health expenditure and, consequently, the system's financial sustainability.</p><p><strong>Methods: </strong>In this observational study, we have analyzed prospectively and retrospectively health patient records who underwent 18F-FDG PET/TC scan at the Nuclear Medicine Department of the University Hospital Mater Domini in Catanzaro (Italy) from 29/09/2022 to 10/02/2023. Patients' diagnostic questions have been defined as appropriate, not completely appropriate and completely inappropriate according to the 18F-FDG PET/CT recommendations defined by the \"Conditions of Supply and Indications of Prescriptive Appropriateness of Italian NHS (National Health Systems)\" published in the Official Gazette no. 15 of 20 January 2016 (Decree 9 December 2015) and by the AIMN (Italian Association of Nuclear Medicine) guidelines.</p><p><strong>Results: </strong>We gathered data from 500 oncological patients (242 males and 258 females). The results show that 423/500 of patients' prescriptions were appropriate, while 77/500 of patients' prescriptions were completely inappropriate (63/77) or not completely appropriate (14/77).</p><p><strong>Conclusion: </strong>Analysis showed a not complete adherence to national guidelines and no shared decision-making approach.</p>","PeriodicalId":10991,"journal":{"name":"Current radiopharmaceuticals","volume":" ","pages":"56-63"},"PeriodicalIF":1.5,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140876128","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Development of [⁶⁴Cu]Cu-NODAGA-RGD-BBN as a Novel Radiotracer for Dual Integrin and GRPR-targeted Tumor PET Imaging.","authors":"Naeimeh Amraee, Behrouz Alirezapour, Mohammad Hosntalab, Asghar Hadadi, Hassan Yousefnia","doi":"10.2174/0118744710246897240209070005","DOIUrl":"10.2174/0118744710246897240209070005","url":null,"abstract":"<p><strong>Background: </strong>In this study, [⁶⁴Cu]Cu-NODAGA-RGD-BBN was prepared and its preclinical assessments were evaluated for PET imaging of GRPR overexpressing tumors.</p><p><strong>Methods: </strong>NODAGA-RGD-BBN heterodimer peptide was successfully labeled with cyclotronproduced copper-64 at optimized conditions. The radiochemical purity of the radiotracer was checked by HPLC and RTLC methods. The stability of the radiolabeled compound was assessed in PBS (4°C) and in human blood serum (37°C). Binding affinity and internalization of [⁶⁴Cu]Cu-NODAGA-RGD-BBN were studied on PC3, LNCaP, and CHO cell lines. The biodistribution of the radiotracer was evaluated in normal and tumor-bearing mice.</p><p><strong>Results: </strong>[⁶⁴Cu]Cu-NODAGA-RGD-BBN was prepared with radiochemical purity >99 ± 0.7% (HPLC/ITLC) and specific activity of 18.5 ± 2.2 TBq/mmol. The radiotracer showed high stability in PBS (95 ± 1.05%) and in human blood serum (96 ± 1.24%) and, high affinity to the GRP expressing tumor cells. [⁶⁴Cu]Cu-NODAGA-RGD-BBN showed hydrophilic (log p = -1.14) and agonistic nature. The biodistribution and imaging studies demonstrated high uptake at the tumor site at all intervals post-injection and 3-4 h post-injection can be considered an appropriate time of imaging.</p><p><strong>Conclusion: </strong>The results indicated that [⁶⁴Cu]Cu-NODAGA-RGD-BBN radiolabeled heterodimer peptide can be considered as a high-potential agent for PET imaging of GRPRoverexpressing tumors.</p>","PeriodicalId":10991,"journal":{"name":"Current radiopharmaceuticals","volume":" ","pages":"37-44"},"PeriodicalIF":1.5,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139971331","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Preclinical Aspects of [89Zr]Zr-DFO-Rituximab: A High Potential Agent for Immuno-PET Imaging.","authors":"Zahra Rouhollahi, Seyed Mahmoud Reza Aghamiri, Hassan Yousefnia, Behrouz Alirezapour, Ali Moghaddasi, Samaneh Zolghadri","doi":"10.2174/0118744710326742241018050220","DOIUrl":"https://doi.org/10.2174/0118744710326742241018050220","url":null,"abstract":"<p><strong>Background: </strong>An early diagnosis of cancer can lead to choosing more effective treatment and increase the number of cancer survivors. In this study, the preparation and preclinical aspects of [89Zr]Zr-DFO-Rituximab, a high-potential agent for PET imaging of Non- Hodgkin Lymphoma (NHL), were evaluated.</p><p><strong>Methods: </strong>DFO was conjugated to rituximab monoclonal antibody (mAb), and DFO-rituximab was successfully labeled with zirconium-89 (89Zr) at optimized conditions. The stability of the complex was assessed in human blood serum and PBS buffer. Radioimmunoreactivity (RIA) of the radioimmunoconjugate (RIC) was evaluated on CD20-overexpressing Raji cell line and CHO cells. The biodistribution of the radiolabeled mAb was studied in normal and tumorbearing rodents. Finally, the absorbed dose in human organs was estimated.</p><p><strong>Results: </strong>The radiolabeled compound was prepared with radiochemical purity (RCP) >99% (RTLC) and a specific activity of 180±1.8 GBq/g. The RCP of the final complex PBS buffer and human blood serum was higher than 95%, even after 48 h post incubation. The RIA assay demonstrated that more than 63% of the radiolabeled compound (40 ng/ml, 0.5 mL) was bound to 5×106 Raji cells. The biodistribution of the final product in tumor-bearing mice showed a high accumulation of the RIC in the tumor site in all intervals post-injection. Tumor/ non-target ratios were increased over time, and longer imaging time was suggested. The dosimetry data indicated that the liver received the most absorbed dose after the complex injection.</p><p><strong>Conclusion: </strong>[89Zr]Zr-DFO-Rituximab represents a significant advancement in the field of oncological imaging and offers a robust platform for both diagnostic and therapeutic applications in the management of B-cell malignancies.</p>","PeriodicalId":10991,"journal":{"name":"Current radiopharmaceuticals","volume":" ","pages":""},"PeriodicalIF":1.5,"publicationDate":"2024-10-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142496720","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Enhancing Ketoprofen Solubility: A Strategic Approach Using Solid Dispersion and Response Surface Methodology.","authors":"Devika Tripathi, Dinesh Kumar Sharma, Jagannath Sahoo","doi":"10.2174/0118744710311951241018054453","DOIUrl":"https://doi.org/10.2174/0118744710311951241018054453","url":null,"abstract":"&lt;p&gt;&lt;strong&gt;Background: &lt;/strong&gt;In the pharmaceutical sciences, the solubility profile of therapeutic molecules is crucial for identifying and formulating drugs and evaluating their quality across the drug discovery pipeline based on factors like oral bioavailability, metabolic transformation, biodistribution kinetics, and potential toxicological implications. The investigation aims to enhance the solubility parameters of ketoprofen (BCS-II class), which exhibits low solubility and high permeability.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Methods: &lt;/strong&gt;In this method, hydrotrope blends of aromatic sodium benzoate and electrolyte sodium acetate were employed to enhance the solubility parameter of ketoprofen. Several batches of solid dispersion of ketoprofen were made using a solvent evaporation method, and the response surface method 3² factorial design was used to find the best one. The optimised formulation, KSD9, underwent in-vitro drug dissolution, DSC, pXRD, and SEM studies.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Results: &lt;/strong&gt;The optimized batch demonstrated substantial improvement in ketoprofen solubility, attributed to mixed hydrotropy. The results indicated that both solubility and %CDR improved when hydrotropes were employed, suggesting a direct proportionality between the rise in solubility and %CDR. Formulations KSD1-KSD9 exhibited solubility enhancements ranging from 2.23 to 5.77-fold, along with an elevation in %CDR from 72.28% to 94.76%. This implies that the %CDR was modulated by the hydrotropes, specifically influenced by the concentration levels of the independent variables. An increase in hydrotrope levels corresponded to an increase in %CDR. The positive coefficients in the quadratic equation for %CDR underscored the significant role of these independent variables in augmenting the in-vitro release of Ketoprofen. Similarly, during a comparative dissolution investigation, the optimized KSD9 formulation exhibited remarkable solubility and drug content compared to conventional Ketoprofen dispersible tablets.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Conclusion: &lt;/strong&gt;The synergistic effect of combining two hydrotropic agents significantly increased the solubility of ketoprofen by up to 58 times. The results indicated that the independent variables exerted a positive influence on solubility and %CDR. Furthermore, the responses were contingent on the specific hydrotropes selected, which functioned as the independent variables. Analyzing the r² and ANOVA results suggested that the dependent variables aligned well with the chosen model. Visual representations, such as the 3D response surface plot and contour plot, demonstrated the impact of each hydrotrope individually and when combined. Overall, employing hydrotropes led to improved solubility and %CDR, highlighting a direct proportionality between the rise in solubility and %CDR. Mixed hydrotropic lessens the toxicity associated with individual hydrotrope concentrations while also offering a sustainable and eco-friendly alternative. This study pave","PeriodicalId":10991,"journal":{"name":"Current radiopharmaceuticals","volume":" ","pages":""},"PeriodicalIF":1.5,"publicationDate":"2024-10-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142496719","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Apigenin's Influence on Inflammatory and Epigenetic Responses in Rat Lungs After Radiotherapy.","authors":"Fatemeh Rajabinasab, Pooya Hajimirzaei, Fatemeh Ramezani, Fariborz Moayer, Fazel Gorjipour, Alireza Nikoofar, Leila Hasanzadeh, Michael R Hamblin, Atousa Janzadeh, Reza Paydar","doi":"10.2174/0118744710336823241011095632","DOIUrl":"https://doi.org/10.2174/0118744710336823241011095632","url":null,"abstract":"<p><strong>Introduction: </strong>The lung is a moderately radio-sensitive organ. When cells are damaged due to accidental radiation exposure or treatment, they release molecules that lead to the recruitment of immune cells, accumulating inflammatory cytokines at the site of damage. Apigenin (Api) is a natural flavonoid known for its anti-inflammatory properties. In this study, we investigated the radioprotective properties of Api in the lung.</p><p><strong>Methods: </strong>Thirty-six Wistar rats were randomly assigned to nine groups: control, radiation (Rad), CMC+Rad, Api10+Rad, and Api20+Rad. Api was administered with an intraperitoneal injection for 7 days, after which the rats were irradiated with 6 Gy whole-body X-ray. At 6 and 72 hours post-irradiation, the rats were euthanized, and their lung tissue was extracted.</p><p><strong>Results: </strong>Radiation led to increased alveolar wall thickness and the infiltration of macrophages and lymphocytes. Furthermore, the expression levels of inflammatory factors such as a nuclear factor of kappa light polypeptide gene enhancer in B-cells (NF-ĸB), Glycogen synthase kinase-3 beta (GSK-3β), transforming growth factor-beta1 (TGF-β1), and epigenetic factors including DNA methyltransferase 3a (DNMT3a) and Histone deacetylase 2 (HDAC2) were elevated in the lung tissue following radiation. Meanwhile, the expression level of IκB-α decreased. However, administration of Api (at both 10&20 mg/kg) reversed the adverse effects of radiation.</p><p><strong>Conclusion: </strong>Api administration mitigated radiation-induced lung damage by reversing inflammatory and epigenetic changes.</p>","PeriodicalId":10991,"journal":{"name":"Current radiopharmaceuticals","volume":" ","pages":""},"PeriodicalIF":1.5,"publicationDate":"2024-10-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142496718","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"An Analysis of the Radiosensitiser Applications in the Biomedical Field.","authors":"Teng Sheng Lim, Irman Abdul Rahman, Aminah Umar, Norsyahidah Mohd Hidzir, Kenton Paul Arkill, Razinah Sharif, Mohd Anuar Jonet, Hur Munawar Kabir Mohd, Faizal Mohamed","doi":"10.2174/0118744710269842240825160247","DOIUrl":"https://doi.org/10.2174/0118744710269842240825160247","url":null,"abstract":"<p><strong>Background: </strong>Various types of radiosensitisers have been introduced from the past until the present day for applications in the biomedical field. However, there is a lack of understanding and comparison between the various parameters introduced in addition to a lack of consensus among researchers on the optimal radiosensitiser for applications in the biomedical field.</p><p><strong>Objective: </strong>This review aimed to investigate the usage of radiosensitisers in the biomedical field, determine their important parameters, and suggest radiosensitisers with potential among the analysed radiosensitisers.</p><p><strong>Results and conclusion: </strong>This review has discussed several parameters for radiosensitisers, including median lethal dose, cell survival, tumour size, cell viability, Dose Enhancement Factor (DEF), Reactive Oxygen Species (ROS) concentration, radiosensitiser production complexity, radiosensitiser administration technique, and radiosensitiser toxicity. General trends regarding the development of radiosensitisers, including the types, effectiveness, and their production complexity, have also been discussed within this review article.</p>","PeriodicalId":10991,"journal":{"name":"Current radiopharmaceuticals","volume":" ","pages":""},"PeriodicalIF":1.5,"publicationDate":"2024-09-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142119212","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Left Ventricular Wall Motion as an Additional Valuable Parameter in Diabetic Patients with Normal Myocardial Perfusion Imaging.","authors":"Amirhesam Davari, Fatemeh Jalali-Zefrei, Bahareh Gholami-Chabok, Shiva Tabaghi, Soghra Farzipour, Kourosh Delpasand, Seyed Mehdi Mousavi","doi":"10.2174/0118744710312688240814100448","DOIUrl":"https://doi.org/10.2174/0118744710312688240814100448","url":null,"abstract":"<p><strong>Background: </strong>Gated SPECT is an established technique for assessment of left ventricular function in cardiovascular disease patients. However, there is little information about the influence of diabetes mellitus on gated SPECT parameters. This study was established to assess gated SPECT parameters in Diabetes Mellitus (DM) and non-diabetes mellitus (non-DM) patients with normal Myocardial Perfusion Imaging (MPI).</p><p><strong>Methods: </strong>In this analytical cross-sectional study, 314 patients (157 DM, 157 non-DM) with normal MPI were enrolled. Prevalence of risk factors for CAD like hypertension (HTN), and dyslipidemia were found to be significantly higher (p <0.01) in DM patients compared to non-DM.</p><p><strong>Results: </strong>No statistically significant difference was observed among the TID, ESV, EDV, PFR, TTPF, and Wall Thickness (WT) parameters between DM and non-DM patients. Wall motion (Wm) in DM patients was significantly higher compared to non-DM patients. (3.9 ± 0.51 vs. 2.69 ± 0.48 for DM and non-DM patients, respectively, p-value:0.01). Also, there was no significant difference in Wm in the two groups with and without HTN. This shows the independent effect of DM on the Wm.</p><p><strong>Conclusion: </strong>This study believes that the Wm parameter should be noted for the early diagnosis or prevention of heart disease in DM patients. These findings can indicate the gradual changes in the movements of the left ventricle and the beginning of the progression of diabetic cardiomyopathy.</p>","PeriodicalId":10991,"journal":{"name":"Current radiopharmaceuticals","volume":" ","pages":""},"PeriodicalIF":1.5,"publicationDate":"2024-08-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142281760","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Pressed Solid Target Production of 89Zr and its Application for Antibody Labelling.","authors":"Anjli Shrivastav, Sonu Maurya, Manish Dixit, Sarita Kumari, Sanjay Gambhir","doi":"10.2174/0118744710318544240715061530","DOIUrl":"https://doi.org/10.2174/0118744710318544240715061530","url":null,"abstract":"<p><strong>Objectives: </strong>Zirconium-89 ( 89Zr, t1/2=3.27d) is an important + emitting radionuclide used in Positron Emission Tomography (PET) immuno studies due to its unique characteristics and increased demand due to simple and cost-effective production capacity. Production of 89Zr is achieved primarily through solid natural yttrium targets via different target preparation methodologies, such as electrodeposition, pressed foils, and spark plasma sintering. In this study, we have investigated the pressed solid target methodology.</p><p><strong>Methods: </strong>The Yttrium Oxide (Y2O3) powder was pressed to pellet form and stacked over a different back support plate, such as platinum (Pt), niobium (Nb), and tantalum (Ta). The target was irradiated with approximately 12 MeV proton beam for 10-60 minutes at 20µA current. The irradiated target was purified through a solid phase extraction method via hydroxamate-based resin by manual or automatic approach. The purified 89Zr was analyzed using gamma scintigraphy, and specific activity was calculated through Deferoxamine (DFO) chelation.</p><p><strong>Results: </strong>89Zr radionuclide via pressed target was effectively produced with a production yield of 20-30 MBq/µA.h, and the purification was achieved in 35 minutes with (87.46)% average recovery and >98% purity while using automated purification, but manual purification took 2 hours with (91 ± 2)% recovery and >98% purity. The production yield was comparable to the reported pressed target approach. Deferoxamine (DFO) chelation with 89Zr-oxalate was performed with purity >98% and specific activity of 25-30 µCi/mmol.</p><p><strong>Conclusion: </strong>In this study, we explored the production of 89Zr by pressed targets and purification via manual or automated methods with good radionuclide purity. The chelation with DFO or its analog was performed with good labeling efficiency and stability</p>.</p>","PeriodicalId":10991,"journal":{"name":"Current radiopharmaceuticals","volume":" ","pages":""},"PeriodicalIF":1.5,"publicationDate":"2024-07-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141747686","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Radiation-induced Testicular Damage in Mice: Protective Effects of Apigenin Revealed by Histopathological Evaluation.","authors":"Rasool Azmoonfar, Fatemeh Mirzaei, Masoud Najafi, Maryam Varkeshi, Karim Ghazikhanlousani, Sara Momeni, Korosh Saber","doi":"10.2174/0118744710271290231226105727","DOIUrl":"10.2174/0118744710271290231226105727","url":null,"abstract":"<p><strong>Background: </strong>Radiation exposure poses a significant threat to reproductive health, particularly the male reproductive system. The testes, being highly sensitive to radiation, are susceptible to damage that can impair fertility and overall reproductive function. The study aims to investigate the radioprotective effects of apigenin on the testis through histopathological evaluation.</p><p><strong>Materials and methods: </strong>This research involved utilizing a total of 40 mice, which were randomly divided into eight groups of five mice each. The groups were categorized as follows: A) negative control group, B, C, and D) administration of apigenin at three different doses (0.3 mg/kg, 0.6 mg/kg, and 1.2 mg/kg) respectively, E) irradiation group, and F, H, and I) administration of apigenin at three different doses (0.3 mg/kg, 0.6 mg/kg, and 1.2 mg/kg) in combination with irradiation. The irradiation procedure involved exposing the mice to a 2Gy X-ray throughout their entire bodies. Subsequently, histopathological assessments were conducted seven days after the irradiation process.</p><p><strong>Results: </strong>The findings indicated that radiation exposure significantly impacted the spermatogenesis system. This research provides evidence that administering apigenin to mice before ionizing radiation effectively mitigated the harmful effects on the testes. Apigenin demonstrated radioprotective properties, positively influencing various parameters, including the spermatogenesis process and the presence of inflammatory cells within the tubular spaces.</p><p><strong>Conclusion: </strong>Apigenin can provide effective protection for spermatogenesis, minimize the adverse effects of ionizing radiation, and safeguard normal tissues.</p>","PeriodicalId":10991,"journal":{"name":"Current radiopharmaceuticals","volume":" ","pages":"238-246"},"PeriodicalIF":1.5,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139680876","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Automated Synthesis of [¹¹C]PiB <i>via</i> [¹¹CH₃OTf]-as Methylating Agent for PET Imaging of β-Amyloid.","authors":"Akhilesh K Singh, Sanjay Gambhir, Manish Dixit","doi":"10.2174/0118744710295705240229114137","DOIUrl":"10.2174/0118744710295705240229114137","url":null,"abstract":"<p><strong>Aim: </strong>Efficient synthesis of precursor from commercially available starting materials and automated radiosynthesis of [¹¹C]PiB using commercially available dedicated [¹¹C]- Chemistry module from the synthesized precursor.</p><p><strong>Background: </strong>[¹¹C]PiB is a promising radiotracer for PET imaging of β-Amyloid, advancing Alzheimer's disease research. The availability of precursors and protocols for efficient radiolabelling foster the applications of any radiotracer. Efficient synthesis of PiB precursor was performed using anisidine and 4-nitrobenzoyl chloride as starting materials in 5 steps, having addition, substitutions, and cyclization chemical methodologies. This precursor was used for fully automated radiosynthesis of [¹¹C]PiB in a commercially available synthesizer, MPS-100 (SHI, Japan). The synthesized [¹¹C]PiB was purified via solid-phase methodology, and its quality control was performed by the quality and safety criteria required for clinical use.</p><p><strong>Methods: </strong>The synthesis of desired precursors and standard authentic compounds started with commercially available materials with 70-80% yields. The standard analytical methods were characterized all synthesized compounds. The fully automated [¹¹C]-chemistry synthesizer (MPS-100) used for radiosynthesis of [¹¹C]PiB with [¹¹C]CH₃OTf acts as a methylating agent. For radiolabelling, varied amounts of precursor and time of reaction were explored. The resulting crude product underwent purification through solid-phase cartridges. The synthesized radiotracer was analyzed using analytical tools such as radio TLC, HPLC, pH endo-toxicity, and half-life.</p><p><strong>Results: </strong>The precursor for radiosynthesis of [¹¹C]PiB was achieved in excellent yield using simple and feasible chemistry. A protocol for radiolabelling of precursor to synthesized [¹¹C]PiB was developed using an automated synthesizer. The crude radiotracer was purified by solid-phase cartridge, with a decay-corrected radiochemical yield of 40±5% and radiochemical purity of more than 97% in approx 20 minutes (EOB). The specific activity was calculated and found in a 110-121 mCi/μmol range.</p><p><strong>Conclusion: </strong>A reliable methodology was developed for preparing precursor followed by fully automated radiolabeling using [¹¹C]MeOTf as a methylating agent to synthesize [¹¹C]PiB. The final HPLC-free purification yielded more than 97% radiochemical purity tracer within one radionuclide half-life. The method was reproducible and efficient for any clinical center.</p>","PeriodicalId":10991,"journal":{"name":"Current radiopharmaceuticals","volume":" ","pages":"302-311"},"PeriodicalIF":1.5,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140058905","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}