We have located links that may give you full text access.
Validation of a [Al 18 F]PSMA-11 preparation for clinical applications.
Applied Radiation and Isotopes 2017 December
Imaging prostate-specific membrane antigen (PSMA) using positron emission tomography (PET) has been presented so far as the most sensitive and specific with regard to prostate cancer detection, in particular in high-risk prostate cancer patients. Currently, it mainly features Gallium-68 (68 Ga) labeled PSMA ligands, notably [68 Ga]Glu-urea-Lys(Ahx)-HBED-CC ([68 Ga]-PSMA-11) and [68 Ga]DOTAGA-FFK (Sub-KuE termed ([68 Ga]PSMA-I&T). However, 68 Ga has several shortcomings as radionuclide including a short half-life and non-ideal energies. This has motivated consideration of 18 F-labeled analogues for PET imaging of prostate cancer. Here, we describe a simple synthesis and validation of a fluorine-18 labeled Glu-urea-Lys(Ahx)-HBED-CC ([Al18 F]PSMA-11) for nuclear medicine applications. An efficient method for preparation of [Al18 F]PSMA-11 was developed and validated (according to Pharm Eur) for routinely clinical applications. [Al18 F]PSMA-11 was reproducibly obtained in radiochemical yields of 84 ± 6% (n = 15) and > 98% radiochemical purity using an improved one-step radiofluorination in aqueous solution. The total (production/preparation) time, including purification, pharmacological formulation of the isolated product and the quality control of the injectable solution was less than 60min. The [Al18 F]PSMA-11 was stable over 4h in 1% EtOH/saline selected as injection solution. The solution was sterile, non-pyrogenic and ready for clinical applications after sterile filtration through a 0.22µm membrane filter under sterile conditions. In addition, [Al18 F]PSMA-11 exhibited higher uptake and retention in PMSA-expressing LNCap prostate cells as compared to its clinically established 68 Ga-labeled analogues [68 Ga]PSMA-11 and [68 Ga]PSMA-I&T as well as to [68 Ga]NOTA-Bn-PSMA. The simple and fast preparation of [Al18 F]PSMA-11 combined with its favorable pharmacological properties warrant its translation to a clinical setting.
CONCLUSION: The facile and high-yielding radiosynthesis of [Al18 F]PSMA-11as well as its promising in vitro and in-vivo characteristics makes it worthy of clinical development for PET imaging of prostate cancer.
CONCLUSION: The facile and high-yielding radiosynthesis of [Al18 F]PSMA-11as well as its promising in vitro and in-vivo characteristics makes it worthy of clinical development for PET imaging of prostate cancer.
Full text links
Related Resources
Get seemless 1-tap access through your institution/university
For the best experience, use the Read mobile app
All material on this website is protected by copyright, Copyright © 1994-2024 by WebMD LLC.
This website also contains material copyrighted by 3rd parties.
By using this service, you agree to our terms of use and privacy policy.
Your Privacy Choices
You can now claim free CME credits for this literature searchClaim now
Get seemless 1-tap access through your institution/university
For the best experience, use the Read mobile app