Current radiopharmaceuticals最新文献

Background and objective: The study aimed to investigate the clinical efficacy of CT-guided microwave ablation (MWA) combined with ¹²⁵I seed implantation or bronchial arterial infusion (BAI) chemotherapy in the treatment of malignant pulmonary tumors.

Methods: A total of 56 patients who underwent MWA, MWA combined with ¹²⁵I particle implantation, or MWA combined with BAI chemotherapy for advanced lung cancer or metastatic lung cancer from January 2015 to June 2021 in Guangdong Provincial People's Hospital were enrolled. Among them, 21 patients were treated with MWA (MWA), 18 with MWA combined with ¹²⁵I seed implantation (MWA+¹²⁵I), and 17 with MWA combined with BAI chemotherapy (MWA+BAI). The short-term outcomes, complications, Eastern Cooperative Oncology Group (ECOG) performance score (Zubrod-ECOG-WHO, ZPS), survival, and factors related to survival were compared between the three groups.

Results: The response rate of the MWA group (9.52%) was significantly lower than that of the MWA+¹²⁵I group (50.00%) and MWA+BAI chemotherapy group (47.06%), and the differences were statistically significant (p < 0.05). The incidence of complications in the MWA, MWA+¹²⁵I, and MWA+BAI chemotherapy groups was 47.62%, 55.56%, and 52.94%, respectively, with no significant difference (p > 0.05). Three months after the treatment, the ZPS of the MWA+¹²⁵I and MWA+BAI chemotherapy groups was significantly lower than before treatment and significantly lower than that of the MWA group in the same period; the differences were statistically significant (p < 0.05). The median survival time of the MWA+¹²⁵I group was 18 (9.983, 26.017) months and that of the MWA+BAI chemotherapy group was 21 (0.465, 41.535) months, both of which were higher than that of the MWA group [11 (6.686, 15.314) months]; the differences were statistically significant (p < 0.05). Cox regression analysis was performed on the factors related to survival and revealed treatment mode as a protective factor [HR = 0.433, 95% CI = (0.191, 0.984), p = 0.046]. Other factors, such as gender, age, and tumor size, did not independently affect survival.

Conclusion: CT-guided MWA combined with ¹²⁵I seed implantation and MWA combined with BAI chemotherapy are safe and effective for the treatment of advanced lung cancer and metastatic lung cancer, and can control tumor progression and prolong survival time.

Background: The development of molecular imaging agents targeting epidermal growth factor receptor (EGFR) with L858R mutation may help with the selection of non-small cell lung carcinoma (NSCLCL) patients who may benefit from EFGR tyrosine kinase inhibitor (TKI) therapy.

Objective: In this study, we developed ^99mTc STHHYYP-GHEG-ECGK-tetramethylrhodamine (STHHYYP-ECGK-TAMRA) to target EGFR with L858R mutation in NSCLC tumors and verified its probability as a molecular imaging agent.

Methods: Fmoc solid-phase peptide synthesis was used to synthesize STHHYYP-ECGKTAMRA. ^99mTc labelled STHHYYP-ECGK-TAMRA was prepared. Gamma imaging, fluorescent imaging and biodistribution were performed in murine models bearing NCI-H1975 and NCI-H1650 tumors.

Results: The binding affinity value (K_d) of ^99mTc STHHYYP-ECGK-TAMRA was estimated to be 130.6 ± 29.2 nM in NCI-H1975 cells. The gamma camera images showed a substantial uptake of ^99mTc STHHYYP-ECGK-TAMRA in the NCI-H1975 tumor. The % injected dose/gram of the NCI-H1975 tumor tissue was 2.77 ± 0.70 and 3.48 ± 1.01 at 1 and 3 h, respectively.

Conclusion: Specific binding of ^99mTc STHHYYP-ECGK-TAMRA to L858R-mutated EGFRpositive NCI-H1975 cells and tumors was demonstrated in in vivo and in vitro studies. The results suggest that ^99mTc STHHYYP-ECGK-TAMRA is a good candidate agent for dualmodality imaging targeting EGFR with L858R mutation.

Introduction: The most important toxicity of transarterial radioembolization therapy applied in liver malignancies is radiation pneumonitis and fibrosis due to hepatopulmonary shunt of Yttrium-90 (⁹⁰Y) microspheres. Currently, Technetium-99m macroaggregated albumin (^99mTc-MAA) scintigraphic images are used to estimate lung shunt fraction (LSF) before treatment. The aim of this study was to create a phantom to calculate exact LFS rates according to ^99mTc activities in the phantom and to compare these rates with LSF values calculated from scintigraphic images.

Materials and methods: A 3D-printed lung and liver phantom containing two liver tumors was developed from Polylactic Acid (PLA) material, which is similar to the normal-sized human body in terms of texture and density. Actual %LSFs were calculated by filling phantoms and tumors with ^99mTc radionuclide. After the phantoms were placed in the water tank made of plexiglass material, planar, SPECT, and SPECT/CT images were obtained. The actual LSF ratio calculated from the activity amounts filled into the phantom was used for the verification of the quantification of scintigraphic images and the results obtained by the Simplicity⁹⁰Y^TM method.

Results: In our experimental model, LSFs calculated from ^99mTc activities filled into the lungs, normal liver, small tumor, and large tumor were found to be 0%, 6.2%, 10.8%, and 16.9%. According to these actual LSF values, LSF values were calculated from planar, SPECT/CT (without attenuation correction), and SPECT/CT (with both attenuation and scatter correction) scintigraphic images of the phantom. In each scintigraphy, doses were calculated for lung, small tumor, large tumor, normal liver, and Simplicity⁹⁰Y^TM. The doses calculated from planar and SPECT/CT (NoAC+NoSC) images were found to be higher than the actual doses. The doses calculated from SPECT/CT (with AC+with SC) images and Simplicity⁹⁰Y^TM were found to be closer to the real dose values.

Conclusion: LSF is critical in dosimetry calculations of ⁹⁰Y microsphere therapy. The newly introduced hepatopulmonary shunt phantom in this study is suitable for LSF verification for all models/brands of SPECT and SPECT/CT devices.

Diagnostic and interventional angiograms are instrumental in the multidisciplinary approach to CAD management, enabling accurate diagnosis and effective targeted treatments that significantly enhance patient care and cardiovascular outcomes. However, cath lab staff, including interventional cardiologists, is consistently exposed to ionizing radiation, which poses inherent health risks. Radiation exposure in the cath lab primarily results from the use of fluoroscopy and cineangiography during diagnostic and interventional procedures. Understanding these risks and implementing effective radiation protection measurements are imperative to ensure the well-being of healthcare professionals while delivering high-quality cardiac care. Prolonged and repeated exposure can lead to both deterministic and stochastic effects. Deterministic effects, such as skin erythema and tissue damage, are more likely to occur at high radiation doses. Interventional cardiologists and staff may experience these effects when safety measures are not rigorously followed. In fact, while ionizing radiation is essential in the practice of radiation cardiology ward, cath lab staff faces inherent risks from radiation exposure. Stochastic effects, on the other hand, are characterized by a probabilistic relationship between radiation exposure and the likelihood of harm. These effects include the increased risk of cancer, particularly for those with long-term exposure. Interventional cardiologists, due to their frequent presence in the cath lab, face a higher lifetime cumulative radiation dose, potentially elevating their cancer risk. Protective measures, including the use of lead aprons, thyroid shields, and radiation monitoring devices, play a crucial role in reducing radiation exposure for cath lab personnel. Adherence to strict dose optimization protocols, such as minimizing fluoroscopy time and maximizing distance from the radiation source, is also essential in mitigating these risks. Ongoing research and advancements in radiation safety technology are essential in further for minimizing the adverse effects of ionizing radiation in the cath lab.

Thyroid cancer is the fifth most prevalent cancer in women and the fastest-growing malignancy. Although surgery is still the basis of treatment, internal radiation therapy (Brachytherapy) with radioactive iodine-131, which functions by releasing beta particles with low tissue penetration and causing DNA damage, is also a potential option. The three basic aims of RAI therapy in well-differentiated thyroid tumors are ablation of the remnant, adjuvant therapy, and disease management. Radioactive iodine dose is selected in one of two ways, empiric and dosimetric, which relies on numerous criteria. The dosage for ablation is 30-100 mCi, 30-150 mCi for adjuvant therapy, and 100-200 mCi for treatment. The RAI treatment effectively aids in the treatment to achieve complete removal of the disease and increase survival. The present review intends to emphasize the significance of radioactive iodine in the management of differentiated thyroid cancer and put forward the current breakthroughs in therapy.

Introduction: The aim of this work was to prepare a selective nuclear medicine imaging probe for the Endothelin 1 receptor A in the brain.

Material and methods: Ferulic acid (an ETRA antagonist) was radiolabeled using ¹³¹I by direct electrophilic substitution method. The radiolabeled ferulic acid was formulated as polymeric micelles to allow intranasal brain delivery. Biodistribution was studied in Swiss albino mice by comparing brain uptake of ¹³¹I-ferulic acid after IN administration of ¹³¹I-ferulic acid polymeric micelles, IN administration of ¹³¹I-ferulic acid solution and IV administration of ¹³¹I-ferulic acid solution.

Results: Successful radiolabeling was achieved with an RCY of 98 % using 200 μg of ferulic acid and 60 μg of CAT as oxidizing agents at pH 6, room temperature and 30 min reaction time. ¹³¹I-ferulic acid polymeric micelles were successfully formulated with the particle size of 21.63 nm and polydispersity index of 0.168. Radioactivity uptake in the brain and brain/blood uptake ratio for I.N ¹³¹I-ferulic acid polymeric micelles were greater than the two other routes at all periods.

Conclusion: Our results provide ¹³¹I-ferulic acid polymeric micelles as a hopeful nuclear medicine tracer for ETRA brain receptor.

Background: Mediastinal lymph node metastasis is an important prognostic factor in non-small cell lung cancer (NSCLC) patients without distant metastases. ¹⁸F-2-fluoro-2-deoxy-Dglucose Positron Emission Tomography/Computed Tomography (¹⁸F-FDG PET/CT) is recommended for detecting and staging lymph nodes and distant metastases in NSCLC patients.

Objective: This study aims to investigate whether maximum standardized uptake (SUVmax), mean standardized uptake (SUVmean), metabolic tumor volume (MTV), and tumor lesion glycolysis (TLG) values of the primary tumor measured by ¹⁸F-FDG PET/CT in resectable NSCLC can predict preoperative lymph node metastasis.

Methods: This retrospective study included eighty NSCLC patients who underwent preoperative Positron Emission Tomography/Computed Tomography (PET/CT) for diagnosis and staging. The patients were stage I-III and had no distant metastases. Tumor metabolic parameters such as SUVmax, SUVmean, MTV, and TLG at PET/CT imaging were measured for preoperative diagnosis and staging, and the postoperative pathology results of the patients were examined. The pathology results divided patients with and without lymph node metastasis into two groups. The groups were compared with the student's t-test and chi-square test regarding ¹⁸F-FDG PET/CT tumor metabolic parameters and other parameters.

Results: Fifteen (18.8%) patients were female, and 65 (81.3%) were male. According to the postoperative pathology results, while 30 (37.5%) patients had lymph node metastasis, 50 (62.5%) did not. There was a significant difference between the groups regarding tumor SUVmax and SUVmean values (p = 0.036, p = 0.045). Overall survival in the N0 group was significantly higher than in the N1 + N2 group (p = 0.034); median survival was 30.2 months in N0 cases and 27.3 months in N1 and N2 groups.

Conclusion: SUVmax and SUVmean values are significantly higher in patients with lymph node metastases than in patients without lymph node metastases, and this finding may provide useful information for predicting lymph node metastasis in patients with resectable NSCLC.

The low range of alpha particles provides an opportunity to better target cancer cells theoretically leading to the introduction of interesting alpha emitter radiopharmaceuticals including ²²⁵Ac, ²¹²Pb, etc. The combination of high energy and short range of alpha emitters differentiates targeted radiotherapy from other methods and reduces unwanted cytotoxicity of the cells around the tumoral tissue. Among interesting alpha emitters candidates for targeted therapy, ²¹¹At, one of the radioisotopes with the best optimal decay properties, shows great promise for targeted radiotherapy in some animal prostate cancer xenograft studies and bone micro tumors with significant effects compared to other beta and alpha emitters and also demonstrates interesting properties for clinical applications. However, production and application of this alpha emitter in the development of actinium-based radiopharmaceuticals is hampered by many obstacles. This mini-review demonstrates ²¹¹At production methods, chemical separation, radiolabeling procedures, ²¹¹At-radiopharmaceuticals and their clinical trials, transport, logistics, and costs and future trends in the field for ultimate clinical applications. This review showed that there are limited clinical trials on ²¹¹Ac-based radiopharmaceuticals, which is due to the low accessibility of this radioisotope and other limitations. However, the development programs of major industries indicate the development of ²¹¹Ac-based radiopharmaceuticals in the future.

Background: Radiotherapy plays a vital role in the management of high-grade gliomas. However, the radio resistance of glioma cells limits the effect of radiation and drives recurrence inside the irradiated tumor volume leading to poor outcomes for patients.

Methods: High-grade glioma cell radioresistance significantly contributes to radiotherapy failure, highlighting the importance of identifying predictive biomarkers for radioresistance. An increasing body of evidence complies with the Yes Associated Protein 1 (Yap-1) and heat shock protein 90 (Hsp90) as biomarkers for radioresistance in glioma cells. A number of studies suggest the potential of radioresistance-associated factors as biomarkers and/ or novel therapeutic targets in glioma cells. Thus, it is essential for glioblastoma patients to identify robust druggable targets involved in radioresistance, optimizing irradiation protocol, and understanding their underlying molecular mechanisms.

Results: Therefore, in the present study, we hypothesized that hypofractionated Gamma Knife radiation therapy (HF-GKRT) could target Yap-1 and Hsp90 and downregulate the mechanism of radioresistance in high-grade glioma cells.

Conclusion: For this purpose, expression levels of radioresistance markers Yap-1 and Hsp90 were evaluated after treatment with HF-GKRT, and this was compared with single fraction Gamma Knife radiation therapy (SF-GKRT) in U87MG primary human glioblastoma cell line model. This would help design a novel radiation therapy regimen for glioblastoma patients by reducing the risk of radioresistance.

Crocetin is a kind of apocarotenoid carboxylic acid extracted from saffron (Crocus sativus L.), which is effective in upregulating tissue oxygenation. However, crocetin is difficult to solubilize. It was shown that the trans isomer of crocetin is effective in improving oxygen diffusivity, while its cis isomer appears not to be. Hence, the isolated trans isomer of crocetin or trans-sodium crocetinate (TSC) can be used instead of crocetin. It is shown that TSC can upregulate hypoxic tissue oxygenation and be effective in treating some hypoxia-related diseases. Moreover, experimental and clinical studies have reported no adverse effects following TSC treatment, even at high doses. The current study will discuss the potential role of TSC in hemorrhagic shock, ischemia, brain tumor radiotherapy, and others.