99m Tc-labeling and evaluation of a HYNIC modified small-molecular inhibitor of prostate-specific membrane antigen

Xu, Xiaoping; Zhang, Jianping; Hu, Silong; He, Simin; Bao, Xiao; Ma, Guoying; Luo, Jianmin; Cheng, Jingyi; Zhang, Yingjian

doi:10.1016/j.nucmedbio.2017.01.010

Cited by 42 publications

(43 citation statements)

References 38 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…Due to the exclusively high expression of PSMA by PCa, radionuclide-labelled PSMA small-molecule inhibitors have been reported as a promising radiopharmaceuticals for the clinical application to molecular imaging for PCa diagnosis 9,10 , one of which is HYNIC-Glu-Urea-A ( 99m Tc-HYNIC-PSMA). Its targeting property has been evaluated in both in vitro and in vivo using PCa models (PC-3 for PSMA − and LNCaP for PSMA + ) which revealed a clear difference between the two models 11 . This result suggests that 99m Tc-HYNIC-PSMA is a promising SPECT/CT imaging agent for the PSMA + PCa.…”

mentioning

confidence: 99%

Evaluation of Radiation dosimetry of 99mTc-HYNIC-PSMA and imaging in prostate cancer

Zhang

et al. 2020

Sci Rep

Self Cite

View full text Add to dashboard Cite

This study aims to evaluate the radiation dosimetry of a new technetium-99m-labelled small-molecule inhibitor of prostate-specific membrane antigen (HYNIC-Glu-Urea-A, 99m tc-HYnic-pSMA) and its feasibility as a tumor-imaging agent in prostate cancer (PCa) patients. A total of 15 PCa patients were enrolled in this study. For the dosimetry study, 5 PCa patients received whole-body planar scans at 0.5 h, 1 h, 2 h, 4 h and 8 h after 99m Tc-HYNIC-PSMA injection. The Dosimetry Toolkit (GE, Milwaukee) was used to process the data and segment the organs in the SPECT/CT images, which were then projected onto planar images. The organ-specific absorbed doses, total-body absorbed doses and 99m tc-HYnic-PSMA effective doses of patients were calculated using OLINDA/EXM 1.1 software. Whole-body SPECT/ CT images were also acquired from additional 10 prostate patients to investigate the feasibility of 99m tc-HYNIC-PSMA for imaging tumors by calculating the ratio of tumor-to-background tracer uptake at 2 h after 740 MBq administration. The total-body absorbed dose was 1.54E-03 ± 2.43E-04 mGy/MBq, and the effective dose was 3.72E-03 ± 4.5E-04 mSv/MBq. Compared to published studies of other similar pSMA tracers and 99m Tc-targeted conventional tracers, the absorbed doses of 99m tc-HYnic-pSMA in all organs showed that it could be used safely in the human body. In addition, 99m tc-HYnic-pSMA showed high tracer uptake (with a tumor-to-background ratio of 9.42 ± 2.62) in the malignant lesions of PCa patients, making it a promising radiopharmaceutical imaging method for site-specific management of PCa.

show abstract

mentioning

confidence: 99%

Evaluation of Radiation dosimetry of 99mTc-HYNIC-PSMA and imaging in prostate cancer

Zhang

et al. 2020

Sci Rep

Self Cite

View full text Add to dashboard Cite

show abstract

“…A Tc‐99m labeled PSMA inhibitor (Tc‐99m HYNIC PSMA) was used as described previously . Briefly, carrier free Tc‐pertechnetate was freshly eluted with saline from a 99 Mo/Tc‐generator (Atom Kexing Pharmaceutical Co., Shanghai, China).…”

Section: Methodsmentioning

confidence: 99%

Relationship between PSA kinetics and Tc‐99m HYNIC PSMA SPECT/CT detection rates of biochemical recurrence in patients with prostate cancer after radical prostatectomy

Liu

Zhu

et al. 2018

The Prostate

Self Cite

View full text Add to dashboard Cite

show abstract

“…The second ligand HYNIC-ALUG, developed by Xu et al also showed specific uptake into LNCaP cells. 142 Imaging confirmed specificity to PSMA and high tumor uptake of the compound. A subsequent biodistribution showed a peak tumor uptake of 19.45 ± 2.14 %ID/g at 2 hr after injection, maintaining until 4 hr after injection with 11.23 ± 2.80 %ID/g.…”

Section: Technetium-99mmentioning

confidence: 65%

Targeting prostate cancer: Prostate‐specific membrane antigen based diagnosis and therapy

Wüstemann

Haberkorn

Babich

et al. 2018

Medicinal Research Reviews

View full text Add to dashboard Cite

The high incidence rates of prostate cancer (PCa) raise demand for improved therapeutic strategies. Prostate tumors specifically express the prostate-specific membrane antigen (PSMA), a membrane-bound protease. As PSMA is highly overexpressed on malignant prostate tumor cells and as its expression rate correlates with the aggressiveness of the disease, this tumor-associated biomarker provides the possibility to develop new strategies for diagnostics and therapy of PCa. Major advances have been made in PSMA targeting, ranging from immunotherapeutic approaches to therapeutic small molecules. This review elaborates the diversity of PSMA targeting agents while focusing on the radioactively labeled tracers for diagnosis and endoradiotherapy. A variety of radionuclides have been shown to either enable precise diagnosis or efficiently treat the tumor with minimal effects to nontargeted organs. Most small molecules with affinity for PSMA are based on either a phosphonate or a urea-based binding motif. Based on these pharmacophores, major effort has been made to identify modifications to achieve ideal pharmacokinetics while retaining the specific targeting of the PSMA binding pocket. Several tracers have now shown excellent clinical usability in particular for molecular imaging and therapy as proven by the efficiency of theranostic approaches in current studies. The archetypal expression profile of PSMA may be exploited for the treatment with alpha emitters to break radioresistance and thus to bring the power of systemic therapy to higher levels.

show abstract

99m Tc-labeling and evaluation of a HYNIC modified small-molecular inhibitor of prostate-specific membrane antigen

Cited by 42 publications

References 38 publications

Evaluation of Radiation dosimetry of 99mTc-HYNIC-PSMA and imaging in prostate cancer

Evaluation of Radiation dosimetry of 99mTc-HYNIC-PSMA and imaging in prostate cancer

Relationship between PSA kinetics and Tc‐99m HYNIC PSMA SPECT/CT detection rates of biochemical recurrence in patients with prostate cancer after radical prostatectomy

Targeting prostate cancer: Prostate‐specific membrane antigen based diagnosis and therapy

Contact Info

Product

Resources

About