Automated GMP synthesis of [(18)F]ICMT-11 for in vivo imaging of caspase-3 activity.

Nuclear Medicine and Biology
Robin ForttEric O Aboagye

Abstract

Isatin-5-sulfonamide ([(18)F]ICMT-11) is a sub-nanomolar inhibitor of caspase-3 previously evaluated as an apoptosis imaging agent. Herein, an alternative radiosynthesis of [(18)F]ICMT-11 with increased purity and specific activity is presented. Finally, a GMP-applicable automated radiosynthesis of [(18)F]ICMT-11 is described. The preparation of [(18)F]ICMT-11 was evaluated under a variety of reaction conditions, including reaction solvent, by employing alternative phase transfer catalysts and under different deprotection conditions. Following initial investigations, the process was transferred onto a fully automated GE FASTlab synthesis platform for further development and optimisation. The synthesis of [(18)F]ICMT-11 was successfully validated under GMP conditions, resulting in a yield of 4.6 ± 0.4 GBq with a radiochemical purity of >98% at EOS and a specific activity of 685 ± 237 GBq/μmol within 90 min. Quality control was carried out in accordance with the European Pharmacopoeia and demonstrated that [(18)F]ICMT-11 can be consistently manufactured on the FASTlab to meet specifications. A simplified methodology for the synthesis of the apoptosis imaging agent, [(18)F]ICMT-11, has been achieved by the S(N)2 displacement of a ...Continue Reading

References

Jan 27, 2000·Cell·D Hanahan, R A Weinberg
Jun 29, 2000·Annual Review of Biochemistry·W C EarnshawS H Kaufmann
Jul 18, 2002·Nature Reviews. Drug Discovery·Jason Y Zhang
Dec 13, 2006·Journal of Medicinal Chemistry·Klaus KopkaBodo Levkau
Jul 17, 2008·Bioconjugate Chemistry·Xuehe LiJonathan F Tait
Mar 8, 2011·Cell·Douglas Hanahan, Robert A Weinberg
Oct 28, 2011·Bioorganic & Medicinal Chemistry Letters·Matthias GlaserEric O Aboagye

❮ Previous
Next ❯

Citations

Jul 25, 2013·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Marc PretzeConstantin Mamat
Jul 9, 2014·BioMed Research International·Kathrin KettenbachTobias L Ross
Jun 14, 2017·Chemical Society Reviews·Dion van der BornDanielle J Vugts
Mar 13, 2017·Bioorganic & Medicinal Chemistry·Christian Paul OrtmeyerVerena Hugenberg
Mar 13, 2018·Medicinal Research Reviews·Anna A RybczynskaAren van Waarde
Feb 21, 2019·EJNMMI Research·Vessela VassilevaEric O Aboagye
Aug 13, 2020·Cancers·Segundo Francisco García-ArgüelloGraham Smith
Apr 2, 2020·Molecular Imaging and Biology : MIB : the Official Publication of the Academy of Molecular Imaging·Alvaro A OrdonezSanjay K Jain
Sep 28, 2018·European Journal of Nuclear Medicine and Molecular Imaging·S R DubashEric O Aboagye
Jun 5, 2013·Clinical Cancer Research : an Official Journal of the American Association for Cancer Research·Quang-Dé NguyenEric O Aboagye
Jan 28, 2020·Journal of Labelled Compounds & Radiopharmaceuticals·Imtiaz KhanWilliam Trigg
May 1, 2021·International Journal of Molecular Sciences·Lucas BeroskeFilipe Elvas
May 26, 2018·Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine·Kathrin HeinzmannEric Aboagye
Aug 21, 2013·Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine·Amarnath ChallapalliEric O Aboagye
May 21, 2021·Molecular Imaging and Biology : MIB : the Official Publication of the Academy of Molecular Imaging·Richard EdwardsTimothy H Witney
Feb 6, 2017·Bioconjugate Chemistry·Federica PisaneschiSteven W Millward
May 21, 2020·Molecular Pharmaceutics·Louis Allott, Eric O Aboagye

❮ Previous
Next ❯

Related Concepts

Related Feeds

Apoptotic Caspases

Apoptotic caspases belong to the protease enzyme family and are known to play an essential role in inflammation and programmed cell death. Here is the latest research.

Apoptosis

Apoptosis is a specific process that leads to programmed cell death through the activation of an evolutionary conserved intracellular pathway leading to pathognomic cellular changes distinct from cellular necrosis

Related Papers

Proceedings of the National Academy of Sciences of the United States of America
Quang-De NguyenEric O Aboagye
Clinical Cancer Research : an Official Journal of the American Association for Cancer Research
Quang-De NguyenEric O Aboagye
Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine
Amarnath ChallapalliEric O Aboagye
European Journal of Cancer : Official Journal for European Organization for Research and Treatment of Cancer (EORTC) [and] European Association for Cancer Research (EACR)
Quang-De NguyenEric O Aboagye
© 2021 Meta ULC. All rights reserved