Literature DB >> 27378195

Fully automated synthesis of [(18) F]fluoro-dihydrotestosterone ([(18) F]FDHT) using the FlexLab module.

Uwe Ackermann1,2,3,4, Jason S Lewis5, Kenneth Young1, Michael J Morris6, Andrew Weickhardt2, Ian D Davis7,8, Andrew M Scott1,2,3,4.   

Abstract

Imaging of androgen receptor expression in prostate cancer using F-18 FDHT is becoming increasingly popular. With the radiolabelling precursor now commercially available, developing a fully automated synthesis of [(18) F] FDHT is important. We have fully automated the synthesis of F-18 FDHT using the iPhase FlexLab module using only commercially available components. Total synthesis time was 90 min, radiochemical yields were 25-33% (n = 11). Radiochemical purity of the final formulation was > 99% and specific activity was > 18.5 GBq/µmol for all batches. This method can be up-scaled as desired, thus making it possible to study multiple patients in a day. Furthermore, our procedure uses 4 mg of precursor only and is therefore cost-effective. The synthesis has now been validated at Austin Health and is currently used for [(18) F]FDHT studies in patients. We believe that this method can easily adapted by other modules to further widen the availability of [(18) F]FDHT.
Copyright © 2016 John Wiley & Sons, Ltd.

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Year:  2016        PMID: 27378195      PMCID: PMC4990449          DOI: 10.1002/jlcr.3417

Source DB:  PubMed          Journal:  J Labelled Comp Radiopharm        ISSN: 0362-4803            Impact factor:   1.921


  15 in total

1.  Clinical states in prostate cancer: toward a dynamic model of disease progression.

Authors:  H I Scher; G Heller
Journal:  Urology       Date:  2000-03       Impact factor: 2.649

2.  Highly efficient production of [(18)F]fallypride using small amounts of base concentration.

Authors:  Byung Seok Moon; Jun Hyung Park; Hong Jin Lee; Ji Sun Kim; Hee Sup Kil; Byoung Se Lee; Dae Yoon Chi; Byung Chul Lee; Yu Kyeong Kim; Sang Eun Kim
Journal:  Appl Radiat Isot       Date:  2010-06-22       Impact factor: 1.513

3.  Fully automated synthesis and coupling of [(18) F]FBEM to glutathione using the iPHASE FlexLab module.

Authors:  Uwe Ackermann; Lucie Plougastel; Christian Wichmann; Yit Wooi Goh; Shinn Dee Yeoh; Stan S Poniger; Henri J Tochon-Danguy; Andrew M Scott
Journal:  J Labelled Comp Radiopharm       Date:  2014-01-07       Impact factor: 1.921

4.  Fully-automated synthesis of 16β-(18)F-fluoro-5α-dihydrotestosterone (FDHT) on the ELIXYS radiosynthesizer.

Authors:  Mark Lazari; Serge K Lyashchenko; Eva M Burnazi; Jason S Lewis; R Michael van Dam; Jennifer M Murphy
Journal:  Appl Radiat Isot       Date:  2015-05-21       Impact factor: 1.513

5.  Optimization of the preparation of fluorine-18-labeled steroid receptor ligands 16alpha-[18F]fluoroestradiol (FES), [18F]fluoro furanyl norprogesterone (FFNP), and 16beta-[18F]fluoro-5alpha-dihydrotestosterone (FDHT) as radiopharmaceuticals.

Authors:  Dong Zhou; Mai Lin; Norio Yasui; Mohammed H Al-Qahtani; Carmen S Dence; Sally Schwarz; John A Katzenellenbogen
Journal:  J Labelled Comp Radiopharm       Date:  2014-02-17       Impact factor: 1.921

Review 6.  Multidimensional MR spectroscopic imaging of prostate cancer in vivo.

Authors:  M Albert Thomas; Rajakumar Nagarajan; Amir Huda; Daniel Margolis; Manoj K Sarma; Ke Sheng; Robert E Reiter; Steven S Raman
Journal:  NMR Biomed       Date:  2013-07-31       Impact factor: 4.044

Review 7.  Prostate cancer: PET with 18F-FDG, 18F- or 11C-acetate, and 18F- or 11C-choline.

Authors:  Hossein Jadvar
Journal:  J Nucl Med       Date:  2010-12-13       Impact factor: 10.057

8.  Pharmacokinetic assessment of the uptake of 16beta-18F-fluoro-5alpha-dihydrotestosterone (FDHT) in prostate tumors as measured by PET.

Authors:  Bradley J Beattie; Peter M Smith-Jones; Yuliya S Jhanwar; Heiko Schöder; C Ross Schmidtlein; Michael J Morris; Pat Zanzonico; Olivia Squire; Gustavo S P Meirelles; Ron Finn; Mohammad Namavari; Shangde Cai; Howard I Scher; Steven M Larson; John L Humm
Journal:  J Nucl Med       Date:  2010-01-15       Impact factor: 10.057

9.  Bone metastases in castration-resistant prostate cancer: associations between morphologic CT patterns, glycolytic activity, and androgen receptor expression on PET and overall survival.

Authors:  Hebert Alberto Vargas; Cecilia Wassberg; Josef J Fox; Andreas Wibmer; Debra A Goldman; Deborah Kuk; Mithat Gonen; Steven M Larson; Michael J Morris; Howard I Scher; Hedvig Hricak
Journal:  Radiology       Date:  2013-11-18       Impact factor: 11.105

10.  Design and end points of clinical trials for patients with progressive prostate cancer and castrate levels of testosterone: recommendations of the Prostate Cancer Clinical Trials Working Group.

Authors:  Howard I Scher; Susan Halabi; Ian Tannock; Michael Morris; Cora N Sternberg; Michael A Carducci; Mario A Eisenberger; Celestia Higano; Glenn J Bubley; Robert Dreicer; Daniel Petrylak; Philip Kantoff; Ethan Basch; William Kevin Kelly; William D Figg; Eric J Small; Tomasz M Beer; George Wilding; Alison Martin; Maha Hussain
Journal:  J Clin Oncol       Date:  2008-03-01       Impact factor: 44.544

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  4 in total

1.  Production of diverse PET probes with limited resources: 24 18F-labeled compounds prepared with a single radiosynthesizer.

Authors:  Jeffrey Collins; Christopher M Waldmann; Christopher Drake; Roger Slavik; Noel S Ha; Maxim Sergeev; Mark Lazari; Bin Shen; Frederick T Chin; Melissa Moore; Saman Sadeghi; Michael E Phelps; Jennifer M Murphy; R Michael van Dam
Journal:  Proc Natl Acad Sci U S A       Date:  2017-10-10       Impact factor: 11.205

2.  Ring opening of epoxides with [18F]FeF species to produce [18F]fluorohydrin PET imaging agents.

Authors:  Stefan Verhoog; Allen F Brooks; Wade P Winton; Benjamin L Viglianti; Melanie S Sanford; Peter J H Scott
Journal:  Chem Commun (Camb)       Date:  2019-05-30       Impact factor: 6.222

3.  [18F]-FDHT PET/CT as a tool for imaging androgen receptor expression in high-grade glioma.

Authors:  Marina Orevi; Ofer Shamni; Nomi Zalcman; Alexandre Chicheportiche; Anat Mordechai; Samuel Moscovici; Yigal Shoshan; Tal Shahar; Hanna Charbit; Mijal Gutreiman; Iddo Paldor; Eyal Mishani; Alexander Lossos; Iris Lavon
Journal:  Neurooncol Adv       Date:  2021-01-29

4.  Imaging Androgen Receptors in Breast Cancer with 18F-Fluoro-5α-Dihydrotestosterone PET: A Pilot Study.

Authors:  Heather Jacene; Mofei Liu; Su-Chun Cheng; Amanda Abbott; Shipra Dubey; Keisha McCall; Diane Young; Mayzie Johnston; Annick D Van den Abbeele; Beth Overmoyer
Journal:  J Nucl Med       Date:  2021-05-28       Impact factor: 11.082

  4 in total

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