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Fully automated radiosynthesis of [18F]LBT999 on TRACERlab FXFN and AllinOne modules, a PET radiopharmaceutical for imaging the dopamine transporter in human brain
Johnny Vercoullie
Corresponding Author
ORCiD: https://orcid.org/0000-0002-7474-7778
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View the published version at EJNMMI Radiopharmacy and Chemistry.
Background: Fluorine labelled 8-((E)-4-fluoro-but-2-enyl)-3b-p-tolyl-8-aza-bicyclo[3.2.1]octane-2b-carboxylic acid methyl ester ([18F]LBT999) is a selective radioligand for the in vivo neuroimaging and quantification of the dopamine transporter by Positron Emission Tomography (PET). [18F]LBT999 was produced on a TRACERlab FXFN for the Phase I study but for Phase III and a potent industrial production transfer, production was also implemented on an AllinOne (AIO) system requiring a single use cassette. Both production methods are reported herein.
Results: Automation of [18F]LBT999 radiosynthesis on FXFN was carried out in 35% yield (decay-corrected) in 65 min (n=16), with a radiochemical purity higher than 99 % and a molar activity of 158 GBq/µmol at the end of synthesis. The transfer to the AIO platform followed by optimizations allowed the production of [18F]LBT999 in 32.7% yield (decay-corrected) within 48 min (n=5), with a radiochemical purity better than 98% and a molar activity above 154 GBq/µmol on average at the end of synthesis. Quality controls of both methods met the specification for clinical application.
Conclusion: Both modules allow efficient and reproducible radiosynthesis of [18F]LBT999 with good radiochemical yields and a reasonable synthesis time. The developments made on AIO, such as its ability to meet pharmaceutical criteria and to more easily comply with GMP requirements, make it an optimal approach for the potent industrial production of [18F]LBT999 and future wider use.
Keywords
automation, radiosynthesis, [18F]LBT999, PET, dopamine transporter, Parkinson’s disease
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CURRENT STATUS: Published
Version 2
Posted 14 Aug, 2020
Published
On 16 Nov, 2020
No community comments so far
Editorial decision: Accept
On 24 Aug, 2020
Editor assigned
On 11 Aug, 2020
Submission checks complete
On 10 Aug, 2020
Editor invited
On 10 Aug, 2020
No comments provided
Review #1 received
Received 22 Jul, 2020
Editorial decision: Minor revision
On 22 Jul, 2020
Reviewer #2 agreed
On 21 Jul, 2020
Review #2 received
Received 21 Jul, 2020
Reviewer #1 agreed
On 10 Jul, 2020
Editor assigned
On 07 Jul, 2020
Reviewers invited
Invitations sent on 07 Jul, 2020
Editor invited
On 06 Jul, 2020
Submission checks complete
On 18 Jun, 2020
First submitted
On 16 Jun, 2020
Metrics
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Subject Areas
General Biochemistry
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This preprint is under consideration at EJNMMI Radiopharmacy and Chemistry. A preprint is a preliminary version of a manuscript that has not completed peer review at a journal. Research Square does not conduct peer review prior to posting preprints. The posting of a preprint on this server should not be interpreted as an endorsement of its validity or suitability for dissemination as established information or for guiding clinical practice.
Learn more about In Review
Research article
Fully automated radiosynthesis of [18F]LBT999 on TRACERlab FXFN and AllinOne modules, a PET radiopharmaceutical for imaging the dopamine transporter in human brain
Johnny Vercoullie
Corresponding Author
ORCiD: https://orcid.org/0000-0002-7474-7778
Badges
Prescreen
This manuscript passed our Prescreen assessment
Complete author information
Appropriate declaration statements
Potential risks to human health
Prescreen
Peer Review Timeline
CURRENT STATUS: Published
Version 2
Posted 14 Aug, 2020
Published
On 16 Nov, 2020
No community comments so far
Editorial decision: Accept
On 24 Aug, 2020
Editor assigned
On 11 Aug, 2020
Submission checks complete
On 10 Aug, 2020
Editor invited
On 10 Aug, 2020
No comments provided
Review #1 received
Received 22 Jul, 2020
Editorial decision: Minor revision
On 22 Jul, 2020
Reviewer #2 agreed
On 21 Jul, 2020
Review #2 received
Received 21 Jul, 2020
Reviewer #1 agreed
On 10 Jul, 2020
Editor assigned
On 07 Jul, 2020
Reviewers invited
Invitations sent on 07 Jul, 2020
Editor invited
On 06 Jul, 2020
Submission checks complete
On 18 Jun, 2020
First submitted
On 16 Jun, 2020
Metrics
Comments: 0
PDF Downloads: ...
HTML Views: ...
Subject Areas
General Biochemistry
License:
This work is licensed under a CC BY 4.0 License. Read Full License
View the published version at EJNMMI Radiopharmacy and Chemistry.
Background: Fluorine labelled 8-((E)-4-fluoro-but-2-enyl)-3b-p-tolyl-8-aza-bicyclo[3.2.1]octane-2b-carboxylic acid methyl ester ([18F]LBT999) is a selective radioligand for the in vivo neuroimaging and quantification of the dopamine transporter by Positron Emission Tomography (PET). [18F]LBT999 was produced on a TRACERlab FXFN for the Phase I study but for Phase III and a potent industrial production transfer, production was also implemented on an AllinOne (AIO) system requiring a single use cassette. Both production methods are reported herein.
Results: Automation of [18F]LBT999 radiosynthesis on FXFN was carried out in 35% yield (decay-corrected) in 65 min (n=16), with a radiochemical purity higher than 99 % and a molar activity of 158 GBq/µmol at the end of synthesis. The transfer to the AIO platform followed by optimizations allowed the production of [18F]LBT999 in 32.7% yield (decay-corrected) within 48 min (n=5), with a radiochemical purity better than 98% and a molar activity above 154 GBq/µmol on average at the end of synthesis. Quality controls of both methods met the specification for clinical application.
Conclusion: Both modules allow efficient and reproducible radiosynthesis of [18F]LBT999 with good radiochemical yields and a reasonable synthesis time. The developments made on AIO, such as its ability to meet pharmaceutical criteria and to more easily comply with GMP requirements, make it an optimal approach for the potent industrial production of [18F]LBT999 and future wider use.
Figure 1
Figure 2
Figure 3
Figure 4
Figure 5
Figure 6