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Development of the 99mTc-labelled SST2 antagonist TECANT-1 for a first-in-man multicentre clinical study
ID
Novak, Doroteja
(
Author
),
ID
Janota, Barbara
(
Author
),
ID
Hörmann, Anton Amadeus
(
Author
),
ID
Sawicka, Agnieszka
(
Author
),
ID
Krošelj, Marko
(
Author
),
ID
Hubalewska-Dydejczyk, Alicja
(
Author
),
ID
Fani, Melpomeni
(
Author
),
ID
Mikolajczak, Renata
(
Author
),
ID
Kolenc, Petra
(
Author
),
ID
Decristoforo, Clemens
(
Author
),
ID
Garnuszek, Piotr
(
Author
)
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MD5: EB3212DAA9F8AD74C5A8EB03D8258C09
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https://www.mdpi.com/1999-4923/15/3/885
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Abstract
Broad availability and cost-effectiveness of 99Mo/99mTc generators worldwide support the use, and thus the development, of novel 99mTc-labelled radiopharmaceuticals. In recent years, preclinical and clinical developments for neuroendocrine neoplasms patient management focused on somatostatin receptor subtype 2 (SST2) antagonists, mainly due to their superiority in SST2-tumour targeting and improved diagnostic sensitivity over agonists. The goal of this work was to provide a reliable method for facile preparation of a 99mTc-labelled SST2 antagonist, [99mTc]Tc-TECANT-1, in a hospital radiopharmacy setting, suitable for a multi-centre clinical trial. To ensure successful and reproducible on-site preparation of the radiopharmaceutical for human use shortly before administration, a freeze-dried three-vial kit was developed. The final composition of the kit was established based on the radiolabelling results obtained during the optimisation process, in which variables such as precursor content, pH and buffer, as well as kit formulations, were tested. Finally, the prepared GMP-grade batches met all predefined specification parameters together with long-term kit stability and stability of the product [99mTc]Tc-TECANT-1. Furthermore, the selected precursor content complies with micro-dosing, based on an extended single-dose toxicity study, where histopathology NOEL was established at 0.5 mg/kg BW, being more than 1000 times higher than the planned human dose of 20 µg. In conclusion, [99mTc]Tc-TECANT-1 is suitable to be advanced into a first-in-human clinical trial.
Language:
English
Keywords:
technetium-99m
,
somatostatin receptor antagonists
,
kit formulation
,
single dose toxicity
,
SPECT
,
radiopharmaceuticals
,
neuroendocrine neoplasms
Work type:
Article
Typology:
1.01 - Original Scientific Article
Organization:
FFA - Faculty of Pharmacy
Publication status:
Published
Publication version:
Version of Record
Year:
2023
Number of pages:
16 str.
Numbering:
Vol. 15, iss. 3, ǂart. ǂ885
PID:
20.500.12556/RUL-144722
UDC:
615.849.2
ISSN on article:
1999-4923
DOI:
10.3390/pharmaceutics15030885
COBISS.SI-ID:
144626179
Publication date in RUL:
09.03.2023
Views:
1122
Downloads:
61
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Record is a part of a journal
Title:
Pharmaceutics
Shortened title:
Pharmaceutics
Publisher:
MDPI
ISSN:
1999-4923
COBISS.SI-ID:
517949977
Licences
License:
CC BY 4.0, Creative Commons Attribution 4.0 International
Link:
http://creativecommons.org/licenses/by/4.0/
Description:
This is the standard Creative Commons license that gives others maximum freedom to do what they want with the work as long as they credit the author.
Secondary language
Language:
Slovenian
Keywords:
tehnecij-99m
,
antagonisti receptorjev somatostatina
,
formulacija kompleta
,
toksičnost enkratnega odmerka
,
SPECT
,
radiofarmacevtiki
,
nevroendokrine neoplazme
,
radiofarmacija
Projects
Funder:
Other - Other funder or multiple funders
Project number:
ERAPERMED2018-125
Acronym:
ERA PerMed
Funder:
Other - Other funder or multiple funders
Funding programme:
Austrian Science Fund
Project number:
I 4220-B
Funder:
Other - Other funder or multiple funders
Funding programme:
National Centre for Research and Development
Project number:
ERA-PerMed/01/2019
Funder:
Other - Other funder or multiple funders
Funding programme:
Jagiellonian University Medical College
Project number:
ERAPerMed/ 02/2019
Funder:
Other - Other funder or multiple funders
Funding programme:
National Centre for Nuclear Research
Project number:
C3330-19-522011
Name:
Razvoj inovativnega, z gama sevalcem tehnecijem-99m označenega antagonista somatostatinskih receptorjev za diagnostiko nevroendokrinih novotvorb - raziskava izvedljivosti
Acronym:
TECANT
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