Nuclear medicine plays an irreplaceable role in the diagnosis and treatment of tumors.Radiopharmaceuticals are important components of nuclear medicine.Among the radiopharmaceuticals approved by the Food and Drug Admi...Nuclear medicine plays an irreplaceable role in the diagnosis and treatment of tumors.Radiopharmaceuticals are important components of nuclear medicine.Among the radiopharmaceuticals approved by the Food and Drug Administration(FDA),radio-tracers targeting prostate-specific membrane antigen(PSMA)and somatostatin receptor(SSTR)have held essential positions in the diagnosis and treatment of prostate cancers and neuroendocrine neoplasms,respectively.In recent years,FDA-approved serials of immune-therapy and targeted therapy drugs targeting programmed death 1(PD-1)/programmed death ligand 1(PD-L1),human epidermal growth factor receptor 2(HER2),and nectin cell adhesion molecule 4(Nectin 4).How to screen patients suitable for these treatments and monitor the therapy?Nuclear medicine with specific radiopharmaceuticals can visualize the expression level of those targets in systemic lesions and evaluate the efficacy of treatment.In addition to radiopharmaceuticals,imaging equipment is also a key step for nuclear medicine.Advanced equipment including total-body positron emission tomography/computed tomography(PET/CT)and positron emission tomography/magnetic resonance imaging(PET/MRI)has been developed,which contribute to the diagnosis and treatment of tumors,as well as the development of new radiopharmaceuticals.Here,we conclude most recently advances of radiopharmaceuticals in nuclear medicine,and they substantially increase the“arsenal”of clinicians for tumor therapy.展开更多
Pancreatic cancer(PC) is a major health problem. Conventional imaging modalities show limited accuracy for reliable assessment of the tumor. Recent researches suggest that molecular imaging techniques with tracers pro...Pancreatic cancer(PC) is a major health problem. Conventional imaging modalities show limited accuracy for reliable assessment of the tumor. Recent researches suggest that molecular imaging techniques with tracers provide more biologically relevant information and are benefit for the diagnosis of the cancer. In addition,radiopharmaceuticals also play more important roles in treatment of the disease. This review summaries the advancement of the radiolabeled compounds in the theranostics of PC.展开更多
Various single or multi-modality therapeutic options are available to treat pain of bone metastasis in patients with prostate cancer.Different radionuclides that emitβ-rays such as 153Samarium and 89Strontium and ach...Various single or multi-modality therapeutic options are available to treat pain of bone metastasis in patients with prostate cancer.Different radionuclides that emitβ-rays such as 153Samarium and 89Strontium and achieve palliation are commercially available.In contrast toβ-emitters,223Radium as a a-emitter has a short path-length.The advantage of the a-emitter is thus a highly localized biological effect that is caused by radiation induced DNA double-strand breaks and subsequent cell killing and/or limited effectiveness of cellular repair mechanisms.Due to the limited range of the a-particles the bone surface to red bone marrow dose ratio is also lower for 223Radium which is expressed in a lower myelotoxicity.The a emitter 223Radium dichloride is the first radiopharmaceutical that significantly prolongslife in castrate resistant prostate cancer patients with wide-spread bone metastatic disease.In a phaseⅢ,randomized,double-blind,placebo-controlled study 921patients with castration-resistant prostate cancer and bone metastases were randomly assigned.The analysis confirmed the 223Radium survival benefit compared to the placebo(median,14.9 mo vs 11.3 mo;P<0.001).In addition,the treatment results in pain palliation and thus,improved quality of life and a delay of skeletal related events.At the same time the toxicity profile of223Radium was favourable.Since May 2013,223Radium dichloride(Xofigo?)is approved by the US Food and Drug Administration.展开更多
Natural products provide a bountiful supply of pharmacologically relevant precursors for the development of various drug-related molecules,including radiopharmaceuticals.However,current knowledge regarding the importa...Natural products provide a bountiful supply of pharmacologically relevant precursors for the development of various drug-related molecules,including radiopharmaceuticals.However,current knowledge regarding the importance of natural products in developing new radiopharmaceuticals remains limited.To date,several radionuclides,including gallium-68,technetium-99m,fluorine-18,iodine-131,and iodine-125,have been extensively studied for the synthesis of diagnostic and therapeutic radiopharmaceuticals.The availability of various radiolabeling methods allows the incorporation of these radionuclides into bioactive molecules in a practical and efficient manner.Of the radiolabeling methods,direct radioiodination,radiometal complexation,and halogenation are generally suitable for natural products owing to their simplicity and robustness.This review highlights the pharmacological benefits of curcumin and its analogs,flavonoids,and marine peptides in treating human pathologies and provides a perspective on the potential use of these bioactive compounds as molecular templates for the design and development of new radiopharmaceuticals.Additionally,this review provides insights into the current strategies for labeling natural products with various radionuclides using either direct or indirect methods.展开更多
The electrochemical properties of perrhenate were studied in hydrochloric acid solution via cyclic voltammetry by disk glassy carbon electrode. The electroreduction of perrhenate was performed at a constant potential-...The electrochemical properties of perrhenate were studied in hydrochloric acid solution via cyclic voltammetry by disk glassy carbon electrode. The electroreduction of perrhenate was performed at a constant potential-0.33 V(vs. Ag/AgCl) with a potentiostat by a flow type electrolysis cell. It was found that the change of rhenium ion concentration before and after electrolysis was negligible. This means almost no rhenium or rhenium oxides were deposited on the carbon fiber electrode during the electroreduction. The rhenium ion solution changed from colorless into yellow-brown after electrolysis process. UV-Visible spectrophotometry was used to characterize the oxidation states of Re before and after electrolysis. Some obvious peaks were detected after electrolysis, indicating that Re(Ⅶ) was reduced to Re(V). The complex behavior and stability of Re(V)-HEDP were discussed for the purpose of electroreduction of Re(Ⅶ) or Tc(Ⅶ) on radiopharmaceuticals production.展开更多
Routine clinical PET radiopharmaceuticals for the noninvasive imaging of brain receptors, transporters, and enzymes are commonly labeled with positron emitting nuclides such as carbon-11 or fluorine-18. Certain minima...Routine clinical PET radiopharmaceuticals for the noninvasive imaging of brain receptors, transporters, and enzymes are commonly labeled with positron emitting nuclides such as carbon-11 or fluorine-18. Certain minimal conditions need to be fulfilled for these PET ligands to be used as imaging agents in vivo. Some of these prerequisites are discussed and examples of the most useful clinical PET radiopharmaceuticals that have found application in the central nervous system are reviewed.展开更多
The metaiodobenzylguanidine (MIBG) radiopharmaceutical, an analogue of norepinephrine, has been used to diagnose certain diseases in the cardiovascular system when radiolabeled with 123I. This radiopharmaceutical can ...The metaiodobenzylguanidine (MIBG) radiopharmaceutical, an analogue of norepinephrine, has been used to diagnose certain diseases in the cardiovascular system when radiolabeled with 123I. This radiopharmaceutical can also be used to treat tumors, such as neuroblastomas and pheochromocytomas, when radiolabeled with 131I. Its clinical use is often accompanied by a slow intravenous administration, where a significant dose of radiation can directly affect workers in nuclear medicine services. To overcome this problem, the incorporation and controlled release of radiopharmaceuticals from the matrix of mesoporous systems based on silica, such as SBA-15 and hybrid [SBA-15/P(N-iPAAm)], can lead to a significant reduction in radiation doses received by workers. In the present study, silica matrices SBA-15 and hybrid [SBA-15/P(N-iPAAm)] containing the radiopharmaceutical MIBG were prepared and physicochemically characterized through FTIR, SEM, and small angle X-ray diffraction techniques. The release profiles of MIBG from SBA-15 and [SBA-15/P(N-iPAAm)] were studied in a simulated body fluid (SBF) to evaluate their potential application as vehicles for controlled releases. Furthermore, in vitro studies were performed to assess the cytotoxicity of matrices as compared to human lung fibroblast cells (MRC-5). The results revealed that the amount of MIBG incorporated within the studied matrices was indeed quite different, showing that only the hybrid [SBA-15/P(N-iPAAm)] system allowed for a more adequate release profile of MIGB. Taking all results into consideration, it can be concluded that the hybrid matrix [SBA-15/P(N-iPAAm)] can be considered a potential alternative material for the controlled release delivery of radio-pharmaceuticals.展开更多
乳腺癌是目前世界范围内发病率最高的肿瘤,早发现、早诊断对于乳腺癌患者的治疗及预后具有重要意义。乳腺专用PET(dedicated breast PET,dbPET)是一种新兴的分子成像设备,在临床实践中用于乳腺癌的检测和肿瘤生物学的评估,具有比传统影...乳腺癌是目前世界范围内发病率最高的肿瘤,早发现、早诊断对于乳腺癌患者的治疗及预后具有重要意义。乳腺专用PET(dedicated breast PET,dbPET)是一种新兴的分子成像设备,在临床实践中用于乳腺癌的检测和肿瘤生物学的评估,具有比传统影像学手段更高的空间分辨率,可以识别乳房内放射性示踪剂摄取的详细形态学模式。鉴于国内外对dbPET的综合性分析较少,文章从dbPET在乳腺癌的筛查、诊断、摄取模式、新辅助化疗后评估及PET显像剂等方面的应用进行综述。展开更多
With dual-radiopharmaceutical (DR) parathyroid scintigraphy, imaging with 99mTcO4-or 123I-NaI is combined with 99mTc-sestamibi scintigraphy for localization of parathyroid adenomas. The set images are then either visu...With dual-radiopharmaceutical (DR) parathyroid scintigraphy, imaging with 99mTcO4-or 123I-NaI is combined with 99mTc-sestamibi scintigraphy for localization of parathyroid adenomas. The set images are then either visually compared or digitally subtracted to aid in interpretation. While both EANM and SNMMI guidelines recommend use of digital subtraction over visual interpretation alone, to date, the few formal comparisons performed have not demonstrated superiority. The purpose of this investigation is to rigorously assess the added value of digital subtraction over visual interpretation alone using simultaneously-acquired 123I-NaI and 99mTc-sestamibi images. Materials: 90 consecutive patients with DR parathyroid scintigraphy for primary hyperparathyroidism who underwent successful parathyroidectomy were included. DR planar acquisition was performed 15 minutes post injection using 10% dual energy windows. Digital subtraction was subsequently performed using commercially available software. Images were independently reviewed by 3 nuclear medicine trainees and 2 experienced nuclear medicine physicians with and without digital subtraction. Results were compared with surgical and histopathologic findings, which served as ground truth. Results: 90 patients had a total of 91 confirmed parathyroid lesions. All 5 readers had significantly greater sensitivity with digital subtraction compared with visual interpretation alone while specificity was not significantly diminished. Area under the ROC curve was significantly greater with digital subtraction in 3 of 5 readers. Agreement was greater among trainees and experienced physicians when using digital subtraction. Conclusion: Using an optimized DR planar co-imaging technique, digital subtraction significantly improved inter-observer agreement and confidence of interpretation and increased sensitivity, without diminishing specificity.展开更多
TTHMP (triethylenetetraaminehexamethylenephosphonic acid) was labeled with 153Sm. The labeling condition, stability, mole ratio of 153Sm to TTHMP, rabbit bone imaging and bio-distribution of 153Sm-TTHMP in mice were i...TTHMP (triethylenetetraaminehexamethylenephosphonic acid) was labeled with 153Sm. The labeling condition, stability, mole ratio of 153Sm to TTHMP, rabbit bone imaging and bio-distribution of 153Sm-TTHMP in mice were investigated. The results showed that weak basic media and high concentration ligands were favorable to form 153Sm-TTHMP; labeling compounds were stable at pH 7 in 7 days. The results also indicated that the chemical mole ratio of 153Sm-TTHMP is n(153Sm)﹕n(TTHMP) = 1﹕1 and skeleton uptake of 153Sm-TTHMP is high((13.96(3.51)%/g at 1h post injection and (13.54(2.98)%/g at 48h post injection), while the non-target tissue uptake is relatively low, so 153Sm-TTHMP is a promising bone tumor therapeutic agent.展开更多
文摘Nuclear medicine plays an irreplaceable role in the diagnosis and treatment of tumors.Radiopharmaceuticals are important components of nuclear medicine.Among the radiopharmaceuticals approved by the Food and Drug Administration(FDA),radio-tracers targeting prostate-specific membrane antigen(PSMA)and somatostatin receptor(SSTR)have held essential positions in the diagnosis and treatment of prostate cancers and neuroendocrine neoplasms,respectively.In recent years,FDA-approved serials of immune-therapy and targeted therapy drugs targeting programmed death 1(PD-1)/programmed death ligand 1(PD-L1),human epidermal growth factor receptor 2(HER2),and nectin cell adhesion molecule 4(Nectin 4).How to screen patients suitable for these treatments and monitor the therapy?Nuclear medicine with specific radiopharmaceuticals can visualize the expression level of those targets in systemic lesions and evaluate the efficacy of treatment.In addition to radiopharmaceuticals,imaging equipment is also a key step for nuclear medicine.Advanced equipment including total-body positron emission tomography/computed tomography(PET/CT)and positron emission tomography/magnetic resonance imaging(PET/MRI)has been developed,which contribute to the diagnosis and treatment of tumors,as well as the development of new radiopharmaceuticals.Here,we conclude most recently advances of radiopharmaceuticals in nuclear medicine,and they substantially increase the“arsenal”of clinicians for tumor therapy.
基金Supported by National Natural Science Foundation,Nos.81171399,51473071,81101077,21401084,81401450 and 81472749Jiangsu Province Foundation,Nos.BE2014609,BE2012622,BL2012031 and BM2012066Wuxi Foundation,No.CSZ0N1320
文摘Pancreatic cancer(PC) is a major health problem. Conventional imaging modalities show limited accuracy for reliable assessment of the tumor. Recent researches suggest that molecular imaging techniques with tracers provide more biologically relevant information and are benefit for the diagnosis of the cancer. In addition,radiopharmaceuticals also play more important roles in treatment of the disease. This review summaries the advancement of the radiolabeled compounds in the theranostics of PC.
文摘Various single or multi-modality therapeutic options are available to treat pain of bone metastasis in patients with prostate cancer.Different radionuclides that emitβ-rays such as 153Samarium and 89Strontium and achieve palliation are commercially available.In contrast toβ-emitters,223Radium as a a-emitter has a short path-length.The advantage of the a-emitter is thus a highly localized biological effect that is caused by radiation induced DNA double-strand breaks and subsequent cell killing and/or limited effectiveness of cellular repair mechanisms.Due to the limited range of the a-particles the bone surface to red bone marrow dose ratio is also lower for 223Radium which is expressed in a lower myelotoxicity.The a emitter 223Radium dichloride is the first radiopharmaceutical that significantly prolongslife in castrate resistant prostate cancer patients with wide-spread bone metastatic disease.In a phaseⅢ,randomized,double-blind,placebo-controlled study 921patients with castration-resistant prostate cancer and bone metastases were randomly assigned.The analysis confirmed the 223Radium survival benefit compared to the placebo(median,14.9 mo vs 11.3 mo;P<0.001).In addition,the treatment results in pain palliation and thus,improved quality of life and a delay of skeletal related events.At the same time the toxicity profile of223Radium was favourable.Since May 2013,223Radium dichloride(Xofigo?)is approved by the US Food and Drug Administration.
文摘Natural products provide a bountiful supply of pharmacologically relevant precursors for the development of various drug-related molecules,including radiopharmaceuticals.However,current knowledge regarding the importance of natural products in developing new radiopharmaceuticals remains limited.To date,several radionuclides,including gallium-68,technetium-99m,fluorine-18,iodine-131,and iodine-125,have been extensively studied for the synthesis of diagnostic and therapeutic radiopharmaceuticals.The availability of various radiolabeling methods allows the incorporation of these radionuclides into bioactive molecules in a practical and efficient manner.Of the radiolabeling methods,direct radioiodination,radiometal complexation,and halogenation are generally suitable for natural products owing to their simplicity and robustness.This review highlights the pharmacological benefits of curcumin and its analogs,flavonoids,and marine peptides in treating human pathologies and provides a perspective on the potential use of these bioactive compounds as molecular templates for the design and development of new radiopharmaceuticals.Additionally,this review provides insights into the current strategies for labeling natural products with various radionuclides using either direct or indirect methods.
文摘The electrochemical properties of perrhenate were studied in hydrochloric acid solution via cyclic voltammetry by disk glassy carbon electrode. The electroreduction of perrhenate was performed at a constant potential-0.33 V(vs. Ag/AgCl) with a potentiostat by a flow type electrolysis cell. It was found that the change of rhenium ion concentration before and after electrolysis was negligible. This means almost no rhenium or rhenium oxides were deposited on the carbon fiber electrode during the electroreduction. The rhenium ion solution changed from colorless into yellow-brown after electrolysis process. UV-Visible spectrophotometry was used to characterize the oxidation states of Re before and after electrolysis. Some obvious peaks were detected after electrolysis, indicating that Re(Ⅶ) was reduced to Re(V). The complex behavior and stability of Re(V)-HEDP were discussed for the purpose of electroreduction of Re(Ⅶ) or Tc(Ⅶ) on radiopharmaceuticals production.
文摘Routine clinical PET radiopharmaceuticals for the noninvasive imaging of brain receptors, transporters, and enzymes are commonly labeled with positron emitting nuclides such as carbon-11 or fluorine-18. Certain minimal conditions need to be fulfilled for these PET ligands to be used as imaging agents in vivo. Some of these prerequisites are discussed and examples of the most useful clinical PET radiopharmaceuticals that have found application in the central nervous system are reviewed.
基金This research was supported by the Brazilian agencies CAPES,CNPq,and FAPEMIGThe authors would like to thank the Microscopy Center at UFMG for its techni-cal support during electron microscopy work.
文摘The metaiodobenzylguanidine (MIBG) radiopharmaceutical, an analogue of norepinephrine, has been used to diagnose certain diseases in the cardiovascular system when radiolabeled with 123I. This radiopharmaceutical can also be used to treat tumors, such as neuroblastomas and pheochromocytomas, when radiolabeled with 131I. Its clinical use is often accompanied by a slow intravenous administration, where a significant dose of radiation can directly affect workers in nuclear medicine services. To overcome this problem, the incorporation and controlled release of radiopharmaceuticals from the matrix of mesoporous systems based on silica, such as SBA-15 and hybrid [SBA-15/P(N-iPAAm)], can lead to a significant reduction in radiation doses received by workers. In the present study, silica matrices SBA-15 and hybrid [SBA-15/P(N-iPAAm)] containing the radiopharmaceutical MIBG were prepared and physicochemically characterized through FTIR, SEM, and small angle X-ray diffraction techniques. The release profiles of MIBG from SBA-15 and [SBA-15/P(N-iPAAm)] were studied in a simulated body fluid (SBF) to evaluate their potential application as vehicles for controlled releases. Furthermore, in vitro studies were performed to assess the cytotoxicity of matrices as compared to human lung fibroblast cells (MRC-5). The results revealed that the amount of MIBG incorporated within the studied matrices was indeed quite different, showing that only the hybrid [SBA-15/P(N-iPAAm)] system allowed for a more adequate release profile of MIGB. Taking all results into consideration, it can be concluded that the hybrid matrix [SBA-15/P(N-iPAAm)] can be considered a potential alternative material for the controlled release delivery of radio-pharmaceuticals.
文摘乳腺癌是目前世界范围内发病率最高的肿瘤,早发现、早诊断对于乳腺癌患者的治疗及预后具有重要意义。乳腺专用PET(dedicated breast PET,dbPET)是一种新兴的分子成像设备,在临床实践中用于乳腺癌的检测和肿瘤生物学的评估,具有比传统影像学手段更高的空间分辨率,可以识别乳房内放射性示踪剂摄取的详细形态学模式。鉴于国内外对dbPET的综合性分析较少,文章从dbPET在乳腺癌的筛查、诊断、摄取模式、新辅助化疗后评估及PET显像剂等方面的应用进行综述。
文摘With dual-radiopharmaceutical (DR) parathyroid scintigraphy, imaging with 99mTcO4-or 123I-NaI is combined with 99mTc-sestamibi scintigraphy for localization of parathyroid adenomas. The set images are then either visually compared or digitally subtracted to aid in interpretation. While both EANM and SNMMI guidelines recommend use of digital subtraction over visual interpretation alone, to date, the few formal comparisons performed have not demonstrated superiority. The purpose of this investigation is to rigorously assess the added value of digital subtraction over visual interpretation alone using simultaneously-acquired 123I-NaI and 99mTc-sestamibi images. Materials: 90 consecutive patients with DR parathyroid scintigraphy for primary hyperparathyroidism who underwent successful parathyroidectomy were included. DR planar acquisition was performed 15 minutes post injection using 10% dual energy windows. Digital subtraction was subsequently performed using commercially available software. Images were independently reviewed by 3 nuclear medicine trainees and 2 experienced nuclear medicine physicians with and without digital subtraction. Results were compared with surgical and histopathologic findings, which served as ground truth. Results: 90 patients had a total of 91 confirmed parathyroid lesions. All 5 readers had significantly greater sensitivity with digital subtraction compared with visual interpretation alone while specificity was not significantly diminished. Area under the ROC curve was significantly greater with digital subtraction in 3 of 5 readers. Agreement was greater among trainees and experienced physicians when using digital subtraction. Conclusion: Using an optimized DR planar co-imaging technique, digital subtraction significantly improved inter-observer agreement and confidence of interpretation and increased sensitivity, without diminishing specificity.
文摘TTHMP (triethylenetetraaminehexamethylenephosphonic acid) was labeled with 153Sm. The labeling condition, stability, mole ratio of 153Sm to TTHMP, rabbit bone imaging and bio-distribution of 153Sm-TTHMP in mice were investigated. The results showed that weak basic media and high concentration ligands were favorable to form 153Sm-TTHMP; labeling compounds were stable at pH 7 in 7 days. The results also indicated that the chemical mole ratio of 153Sm-TTHMP is n(153Sm)﹕n(TTHMP) = 1﹕1 and skeleton uptake of 153Sm-TTHMP is high((13.96(3.51)%/g at 1h post injection and (13.54(2.98)%/g at 48h post injection), while the non-target tissue uptake is relatively low, so 153Sm-TTHMP is a promising bone tumor therapeutic agent.
