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放射性药物转化医学研究

      针对靶向integrin αvβ3的RGD多肽分子探针进行了深入系统的基础研究，完成了从小动物显像到大动物显像再到临床应用的过渡，发表了一系列研究论文，研制出新型特异性肿瘤显像剂^99mTc-3PRGD2，并获得国家发明专利。经有关部门批准备案后，进行了 ^99mTc-3PRGD2 的临床研究，与北京协和医院李方教授团队合作在国际上首次报道了^99mTc-3PRGD2用于肿瘤显像诊断的多中心临床研究，证实了其有效性。研制的显像剂^99mTc-3PRGD2 用于SPECT 显像，检查费用大大降低，这将使更多的中国老百姓享受到更好的医疗服务。此项研究工作已成功进行成果转化，获得了佛山市政府和社会基金的资助，启动了国家一类新药的申报，开始了产业化进程。

 

    

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

^99mTc-3PRGD2临床应用文献：

 

1.       Zhang Z, Zhao X, Ding C, Wang J, Zhang J, Wang F. ^99mTc-3PRGD2 SPECT/CT Imaging for Monitoring Early Response of EGFR-TKIs Therapy in Patients with Advanced-Stage Lung Adenocarcinoma. Cancer Biother Radiopharm. 2016 September, 31(7): 238-245.. （DOI:10.1089/cbr.2016.2052）

 

2.       Jin X, Liang N, Wang M, Meng Y, Jia B, Shi X, Li S, Luo J, Luo Y, Cui Q, Zheng K, Liu Z, Shi J, Li F, Wang F, Zhu Z. Integrin Imaging with ^99mTc-3PRGD2 SPECT/CT Shows High Specificity in the Diagnosis of Lymph Node Metastasis from Non-Small Cell Lung Cancer. Radiology. 2016 Jul 29.（DOI：10.1148/radiol.2016150813）

 

3.       Yu X, Wu Y, Liu H, Gao L, Sun X, Zhang C, Shi J, Zhao H, Jia B, Liu Z, Wang F. Small-Animal SPECT/CT of the Progression and Recovery of Rat Liver Fibrosis by Using an Integrin αvβ3-targeting Radiotracer. Radiology. 2016 May; 279(2):502-12.（DOI:10.1148/radiol.2015150090）

 

4.       Chen Q, Xie Q, Zhao M, Chen B, Gao S, Zhang H, Xing H, Ma Q. Diagnostic value of ^99mTc-3PRGD2 scintimammography for differentiation of malignant from benign breast lesions: Comparison of visual and semi-quantitative analysis. Hell J Nucl Med. 2015 Sep-Dec;18(3):193-8.（DOI:10.1967/s002449910302）

 

5.       Huang C, Zheng Q, Miao W. Study of novel molecular probe ^99mTc-3PRGD2 in the diagnosis of rheumatoid arthritis. Nucl Med Commun. 2015 Dec;36(12):1208-14.（DOI:10.1097/MNM.0000000000000375）

 

6.       Ji B, Chen B, Wang T, Song Y, Chen M, Ji T, Wang X, Gao S, Ma Q. ^99mTc-3PRGD2 SPECT to monitor early response to neoadjuvant chemotherapy in stage II and III breast cancer. Eur J Nucl Med Mol Imaging. 2015 Aug;42(9):1362-70.（DOI:10.1007/s00259-015-3062-1）

 

7.       Ma Q, Min K, Wang T, Chen B, Wen Q, Wang F, Ji T, Gao S. ^99mTc-3PRGD2 SPECT/CT predicts the outcome of advanced nonsquamous non-small cell lung cancer receiving chemoradiotherapy plus bevacizumab. Ann Nucl Med. 2015 Jul;29(6):519-27.（DOI：10.1007/s12149-015-0975-5)

 

8.       Chen Q, Ma Q, Chen M, Chen B, Wen Q, Jia B, Wang F, Sun B, Gao S. An exploratory study on ^99mTc-RGD-BBN peptide scintimammography in the assessment of breast malignant lesions compared to ^99mTc-3PRGD2. PLoS One. 2015 Apr 7; 10(4):e0123401.（DOI:10.1371/journal.pone.0123401)

 

9.       Gao R, Zhang G, Chen L, Zhu Z, Wang F, Yang A. Utility of ^99mTc-PEG₄-E[PEG₄-c(RGDfK)]₂ in Posttherapy Surveillance of Patients with Reelevated Carcinoembryonic Antigen Levels. Med Princ Pract. 2015;24(3):244-9.(DOI:10.1159/000381287)

 

10.    Miao W, Zheng S, Dai H, Wang F, Jin X, Zhu Z, Jia B. Comparison of ^99mTc-3PRGD2 integrin receptor imaging with ^99mTc-MDP bone scan in diagnosis of bone metastasis in patients with lung cancer: a multicenter study. PLoS One. 2014 Oct 22;9(10):e111221.(DOI:10.1371/journal.pone.0111221)

 

11.    Liu L, Song Y, Gao S, Ji T, Zhang H, Ji B, Chen B, Jia B, Wang F, Xu Z, Ma Q. ^99mTc-3PRGD2 scintimammography in palpable and nonpalpable breast lesions. Mol Imaging. 2014;13.(DOI: 10.2310/7290.2014.00010)

 

12.    Hou Y, Zhu Z, Jin X, Wang R, Xing B. Combined ¹⁸F-FDG PET/CT and ^99mTc-3PRGD2 SPECT/CT imaging in a case of pituitary metastases. Clin Nucl Med. 2013 Jul;38(7):550-2.(DOI:10.1097/RLU.0b013e318292aa2f)

 

13.    Jin X, Meng Y, Zhu Z, Jing H, Li F. Elevated ^99mTc-3PRGD2 activity in benign metastasizing leiomyoma. Clin Nucl Med. 2013 Feb;38(2):117-9.(DOI:10.1097/RLU.0b013e318279f14d)

 

14.    Zhao D, Jin X, Li F, Liang J, Lin Y. Integrin αvβ3 imaging of radioactive iodine-refractory thyroid cancer using ^99mTc-3PRGD2. J Nucl Med. 2012 Dec;53(12):1872-7.(DOI:10.2967/jnumed.112.107821)

 

15.    Zhu Z, Miao W, Li Q, Dai H, Ma Q, Wang F, Yang A, Jia B, Jing X, Liu S, Shi J, Liu Z, Zhao Z, Wang F, Li F. ^99mTc-3PRGD2 for integrin receptor imaging of lung cancer: a multicenter study. J Nucl Med. 2012 May;53(5):716-22.（DOI:10.2967/jnumed.111.098988）

 

16.    Ma Q, Ji B, Jia B, Gao S, Ji T, Wang X, Han Z, Zhao G. Differential diagnosis of solitary pulmonary nodules using ^99mTc-3PRGD2 scintigraphy. Eur J Nucl Med Mol Imaging. 2011 Dec; 38(12):2145-52.(DOI:10.1007/s00259-011-1901-2)