Study of the automated synthesis of the radiopharmaceutical 16 ?? [18F] fluoro-17??-estradiol
Autor(a) principal: | |
---|---|
Data de Publicação: | 2020 |
Outros Autores: | , , |
Tipo de documento: | Artigo de conferência |
Título da fonte: | Repositório Institucional do IPEN |
Texto Completo: | http://repositorio.ipen.br/handle/123456789/30593 |
Resumo: | Approximately 75% of breast cancer cells express estrogen receptor (ER +) and this type of cancer has incidence of 25 % a year, being the second cause of cancer death among women worldwide. The 16??-[18F]-fluoro-17??-estradiol, 18F-FES, is a lipophilic molecule with in vivo characteristics similar to estradiol being a valuable marker in molecular imaging for non-invasive diagnosis of primary and metastatic breast cancer using PET-CT, because it binds to estrogen receptors (ER binding). The objective of this work was to study the synthesis of 18F-FES in the GE TRACERlab?? MXFDG module, using Chemical Kit and disposable cassette ABX?? and determine the yield of the process and the analytical parameters to be employed in the routinely production of this radiopharmaceutical. The automated synthesis occurs in 75 min. and includes percolation of the [18F] fluoride in an anion exchange cartridge, elution of the cartridge, azeotropic drying in 3 steps, labeling using 3-methoxymethyl-16??,17??-epiestriol-O-cyclic sulfone (MMSE) and the hydrolysis in 1 step. Purification of the product is done in the module itself using solid phase extraction (SPE) cartridges, without the use of HPLC. The data about synthesis efficiency and quality control parameters are under analysis. Preliminary results suggest an increase in synthesis efficiency when minimal changes in the synthesis program were introduced. The results of quality control assays (radiochemical purity, residual solvent, radionuclidic purity and identity and chemical purity (TBA) suggest that final radiopharmaceutical meets the criteria established for other fluor-18 radiopharmaceuticals that have monographs in official compendia. |
id |
IPEN_9168afac836c290e479d6542df8c7961 |
---|---|
oai_identifier_str |
oai:repositorio.ipen.br:123456789/30593 |
network_acronym_str |
IPEN |
network_name_str |
Repositório Institucional do IPEN |
repository_id_str |
4510 |
spelling |
2020-01-07T14:45:40Z2020-01-07T14:45:40ZOctober 21-25, 2019http://repositorio.ipen.br/handle/123456789/305930000-0002-3442-6830Approximately 75% of breast cancer cells express estrogen receptor (ER +) and this type of cancer has incidence of 25 % a year, being the second cause of cancer death among women worldwide. The 16??-[18F]-fluoro-17??-estradiol, 18F-FES, is a lipophilic molecule with in vivo characteristics similar to estradiol being a valuable marker in molecular imaging for non-invasive diagnosis of primary and metastatic breast cancer using PET-CT, because it binds to estrogen receptors (ER binding). The objective of this work was to study the synthesis of 18F-FES in the GE TRACERlab?? MXFDG module, using Chemical Kit and disposable cassette ABX?? and determine the yield of the process and the analytical parameters to be employed in the routinely production of this radiopharmaceutical. The automated synthesis occurs in 75 min. and includes percolation of the [18F] fluoride in an anion exchange cartridge, elution of the cartridge, azeotropic drying in 3 steps, labeling using 3-methoxymethyl-16??,17??-epiestriol-O-cyclic sulfone (MMSE) and the hydrolysis in 1 step. Purification of the product is done in the module itself using solid phase extraction (SPE) cartridges, without the use of HPLC. The data about synthesis efficiency and quality control parameters are under analysis. Preliminary results suggest an increase in synthesis efficiency when minimal changes in the synthesis program were introduced. The results of quality control assays (radiochemical purity, residual solvent, radionuclidic purity and identity and chemical purity (TBA) suggest that final radiopharmaceutical meets the criteria established for other fluor-18 radiopharmaceuticals that have monographs in official compendia.Submitted by Celia Satomi Uehara (celia.u-topservice@ipen.br) on 2020-01-07T14:45:40Z No. of bitstreams: 1 26243.pdf: 647083 bytes, checksum: 763d2c06223d9dd9be15de02f5df48b2 (MD5)Made available in DSpace on 2020-01-07T14:45:40Z (GMT). No. of bitstreams: 1 26243.pdf: 647083 bytes, checksum: 763d2c06223d9dd9be15de02f5df48b2 (MD5)1961-1967Associa????o Brasileira de Energia Nuclearcomparative evaluationsestradiolfluorine 18fluorodeoxyglucoseirradiationmammary glandspositron computed tomographyprotonsradiochemistryradiopharmaceuticalsStudy of the automated synthesis of the radiopharmaceutical 16 ?? [18F] fluoro-17??-estradiolinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/conferenceObjectINACIRio de JaneiroSantos, SP116031141664600600600BALIEIRO, LUIZA M.OLIVEIRA, HENRIQUE B. deARAUJO, ELAINE B. deINTERNATIONAL NUCLEAR ATLANTIC CONFERENCEinfo:eu-repo/semantics/openAccessreponame:Repositório Institucional do IPENinstname:Instituto de Pesquisas Energéticas e Nucleares (IPEN)instacron:IPEN262432019ARAUJO, ELAINE B. deOLIVEIRA, HENRIQUE B. deBALIEIRO, LUIZA M.20-01Proceedings664114111603ARAUJO, ELAINE B. de:664:110:NOLIVEIRA, HENRIQUE B. de:1141:110:NBALIEIRO, LUIZA M.:11603:110:SORIGINAL26243.pdf26243.pdfapplication/pdf647083http://repositorio.ipen.br/bitstream/123456789/30593/1/26243.pdf763d2c06223d9dd9be15de02f5df48b2MD51LICENSElicense.txtlicense.txttext/plain; charset=utf-81748http://repositorio.ipen.br/bitstream/123456789/30593/2/license.txt8a4605be74aa9ea9d79846c1fba20a33MD52123456789/305932020-04-06 17:33:30.736oai:repositorio.ipen.br:123456789/30593Tk9URTogUExBQ0UgWU9VUiBPV04gTElDRU5TRSBIRVJFClRoaXMgc2FtcGxlIGxpY2Vuc2UgaXMgcHJvdmlkZWQgZm9yIGluZm9ybWF0aW9uYWwgcHVycG9zZXMgb25seS4KCk5PTi1FWENMVVNJVkUgRElTVFJJQlVUSU9OIExJQ0VOU0UKCkJ5IHNpZ25pbmcgYW5kIHN1Ym1pdHRpbmcgdGhpcyBsaWNlbnNlLCB5b3UgKHRoZSBhdXRob3Iocykgb3IgY29weXJpZ2h0Cm93bmVyKSBncmFudHMgdG8gRFNwYWNlIFVuaXZlcnNpdHkgKERTVSkgdGhlIG5vbi1leGNsdXNpdmUgcmlnaHQgdG8gcmVwcm9kdWNlLAp0cmFuc2xhdGUgKGFzIGRlZmluZWQgYmVsb3cpLCBhbmQvb3IgZGlzdHJpYnV0ZSB5b3VyIHN1Ym1pc3Npb24gKGluY2x1ZGluZwp0aGUgYWJzdHJhY3QpIHdvcmxkd2lkZSBpbiBwcmludCBhbmQgZWxlY3Ryb25pYyBmb3JtYXQgYW5kIGluIGFueSBtZWRpdW0sCmluY2x1ZGluZyBidXQgbm90IGxpbWl0ZWQgdG8gYXVkaW8gb3IgdmlkZW8uCgpZb3UgYWdyZWUgdGhhdCBEU1UgbWF5LCB3aXRob3V0IGNoYW5naW5nIHRoZSBjb250ZW50LCB0cmFuc2xhdGUgdGhlCnN1Ym1pc3Npb24gdG8gYW55IG1lZGl1bSBvciBmb3JtYXQgZm9yIHRoZSBwdXJwb3NlIG9mIHByZXNlcnZhdGlvbi4KCllvdSBhbHNvIGFncmVlIHRoYXQgRFNVIG1heSBrZWVwIG1vcmUgdGhhbiBvbmUgY29weSBvZiB0aGlzIHN1Ym1pc3Npb24gZm9yCnB1cnBvc2VzIG9mIHNlY3VyaXR5LCBiYWNrLXVwIGFuZCBwcmVzZXJ2YXRpb24uCgpZb3UgcmVwcmVzZW50IHRoYXQgdGhlIHN1Ym1pc3Npb24gaXMgeW91ciBvcmlnaW5hbCB3b3JrLCBhbmQgdGhhdCB5b3UgaGF2ZQp0aGUgcmlnaHQgdG8gZ3JhbnQgdGhlIHJpZ2h0cyBjb250YWluZWQgaW4gdGhpcyBsaWNlbnNlLiBZb3UgYWxzbyByZXByZXNlbnQKdGhhdCB5b3VyIHN1Ym1pc3Npb24gZG9lcyBub3QsIHRvIHRoZSBiZXN0IG9mIHlvdXIga25vd2xlZGdlLCBpbmZyaW5nZSB1cG9uCmFueW9uZSdzIGNvcHlyaWdodC4KCklmIHRoZSBzdWJtaXNzaW9uIGNvbnRhaW5zIG1hdGVyaWFsIGZvciB3aGljaCB5b3UgZG8gbm90IGhvbGQgY29weXJpZ2h0LAp5b3UgcmVwcmVzZW50IHRoYXQgeW91IGhhdmUgb2J0YWluZWQgdGhlIHVucmVzdHJpY3RlZCBwZXJtaXNzaW9uIG9mIHRoZQpjb3B5cmlnaHQgb3duZXIgdG8gZ3JhbnQgRFNVIHRoZSByaWdodHMgcmVxdWlyZWQgYnkgdGhpcyBsaWNlbnNlLCBhbmQgdGhhdApzdWNoIHRoaXJkLXBhcnR5IG93bmVkIG1hdGVyaWFsIGlzIGNsZWFybHkgaWRlbnRpZmllZCBhbmQgYWNrbm93bGVkZ2VkCndpdGhpbiB0aGUgdGV4dCBvciBjb250ZW50IG9mIHRoZSBzdWJtaXNzaW9uLgoKSUYgVEhFIFNVQk1JU1NJT04gSVMgQkFTRUQgVVBPTiBXT1JLIFRIQVQgSEFTIEJFRU4gU1BPTlNPUkVEIE9SIFNVUFBPUlRFRApCWSBBTiBBR0VOQ1kgT1IgT1JHQU5JWkFUSU9OIE9USEVSIFRIQU4gRFNVLCBZT1UgUkVQUkVTRU5UIFRIQVQgWU9VIEhBVkUKRlVMRklMTEVEIEFOWSBSSUdIVCBPRiBSRVZJRVcgT1IgT1RIRVIgT0JMSUdBVElPTlMgUkVRVUlSRUQgQlkgU1VDSApDT05UUkFDVCBPUiBBR1JFRU1FTlQuCgpEU1Ugd2lsbCBjbGVhcmx5IGlkZW50aWZ5IHlvdXIgbmFtZShzKSBhcyB0aGUgYXV0aG9yKHMpIG9yIG93bmVyKHMpIG9mIHRoZQpzdWJtaXNzaW9uLCBhbmQgd2lsbCBub3QgbWFrZSBhbnkgYWx0ZXJhdGlvbiwgb3RoZXIgdGhhbiBhcyBhbGxvd2VkIGJ5IHRoaXMKbGljZW5zZSwgdG8geW91ciBzdWJtaXNzaW9uLgo=Repositório InstitucionalPUBhttp://repositorio.ipen.br/oai/requestbibl@ipen.bropendoar:45102020-04-06T17:33:30Repositório Institucional do IPEN - Instituto de Pesquisas Energéticas e Nucleares (IPEN)false |
dc.title.pt_BR.fl_str_mv |
Study of the automated synthesis of the radiopharmaceutical 16 ?? [18F] fluoro-17??-estradiol |
title |
Study of the automated synthesis of the radiopharmaceutical 16 ?? [18F] fluoro-17??-estradiol |
spellingShingle |
Study of the automated synthesis of the radiopharmaceutical 16 ?? [18F] fluoro-17??-estradiol BALIEIRO, LUIZA M. comparative evaluations estradiol fluorine 18 fluorodeoxyglucose irradiation mammary glands positron computed tomography protons radiochemistry radiopharmaceuticals |
title_short |
Study of the automated synthesis of the radiopharmaceutical 16 ?? [18F] fluoro-17??-estradiol |
title_full |
Study of the automated synthesis of the radiopharmaceutical 16 ?? [18F] fluoro-17??-estradiol |
title_fullStr |
Study of the automated synthesis of the radiopharmaceutical 16 ?? [18F] fluoro-17??-estradiol |
title_full_unstemmed |
Study of the automated synthesis of the radiopharmaceutical 16 ?? [18F] fluoro-17??-estradiol |
title_sort |
Study of the automated synthesis of the radiopharmaceutical 16 ?? [18F] fluoro-17??-estradiol |
author |
BALIEIRO, LUIZA M. |
author_facet |
BALIEIRO, LUIZA M. OLIVEIRA, HENRIQUE B. de ARAUJO, ELAINE B. de INTERNATIONAL NUCLEAR ATLANTIC CONFERENCE |
author_role |
author |
author2 |
OLIVEIRA, HENRIQUE B. de ARAUJO, ELAINE B. de INTERNATIONAL NUCLEAR ATLANTIC CONFERENCE |
author2_role |
author author author |
dc.contributor.author.fl_str_mv |
BALIEIRO, LUIZA M. OLIVEIRA, HENRIQUE B. de ARAUJO, ELAINE B. de INTERNATIONAL NUCLEAR ATLANTIC CONFERENCE |
dc.subject.por.fl_str_mv |
comparative evaluations estradiol fluorine 18 fluorodeoxyglucose irradiation mammary glands positron computed tomography protons radiochemistry radiopharmaceuticals |
topic |
comparative evaluations estradiol fluorine 18 fluorodeoxyglucose irradiation mammary glands positron computed tomography protons radiochemistry radiopharmaceuticals |
description |
Approximately 75% of breast cancer cells express estrogen receptor (ER +) and this type of cancer has incidence of 25 % a year, being the second cause of cancer death among women worldwide. The 16??-[18F]-fluoro-17??-estradiol, 18F-FES, is a lipophilic molecule with in vivo characteristics similar to estradiol being a valuable marker in molecular imaging for non-invasive diagnosis of primary and metastatic breast cancer using PET-CT, because it binds to estrogen receptors (ER binding). The objective of this work was to study the synthesis of 18F-FES in the GE TRACERlab?? MXFDG module, using Chemical Kit and disposable cassette ABX?? and determine the yield of the process and the analytical parameters to be employed in the routinely production of this radiopharmaceutical. The automated synthesis occurs in 75 min. and includes percolation of the [18F] fluoride in an anion exchange cartridge, elution of the cartridge, azeotropic drying in 3 steps, labeling using 3-methoxymethyl-16??,17??-epiestriol-O-cyclic sulfone (MMSE) and the hydrolysis in 1 step. Purification of the product is done in the module itself using solid phase extraction (SPE) cartridges, without the use of HPLC. The data about synthesis efficiency and quality control parameters are under analysis. Preliminary results suggest an increase in synthesis efficiency when minimal changes in the synthesis program were introduced. The results of quality control assays (radiochemical purity, residual solvent, radionuclidic purity and identity and chemical purity (TBA) suggest that final radiopharmaceutical meets the criteria established for other fluor-18 radiopharmaceuticals that have monographs in official compendia. |
publishDate |
2020 |
dc.date.evento.pt_BR.fl_str_mv |
October 21-25, 2019 |
dc.date.accessioned.fl_str_mv |
2020-01-07T14:45:40Z |
dc.date.available.fl_str_mv |
2020-01-07T14:45:40Z |
dc.type.status.fl_str_mv |
info:eu-repo/semantics/publishedVersion |
dc.type.driver.fl_str_mv |
info:eu-repo/semantics/conferenceObject |
format |
conferenceObject |
status_str |
publishedVersion |
dc.identifier.uri.fl_str_mv |
http://repositorio.ipen.br/handle/123456789/30593 |
dc.identifier.orcid.pt_BR.fl_str_mv |
0000-0002-3442-6830 |
url |
http://repositorio.ipen.br/handle/123456789/30593 |
identifier_str_mv |
0000-0002-3442-6830 |
dc.relation.authority.fl_str_mv |
11603 1141 664 |
dc.relation.confidence.fl_str_mv |
600 600 600 |
dc.rights.driver.fl_str_mv |
info:eu-repo/semantics/openAccess |
eu_rights_str_mv |
openAccess |
dc.format.none.fl_str_mv |
1961-1967 |
dc.coverage.pt_BR.fl_str_mv |
I |
dc.publisher.none.fl_str_mv |
Associa????o Brasileira de Energia Nuclear |
publisher.none.fl_str_mv |
Associa????o Brasileira de Energia Nuclear |
dc.source.none.fl_str_mv |
reponame:Repositório Institucional do IPEN instname:Instituto de Pesquisas Energéticas e Nucleares (IPEN) instacron:IPEN |
instname_str |
Instituto de Pesquisas Energéticas e Nucleares (IPEN) |
instacron_str |
IPEN |
institution |
IPEN |
reponame_str |
Repositório Institucional do IPEN |
collection |
Repositório Institucional do IPEN |
bitstream.url.fl_str_mv |
http://repositorio.ipen.br/bitstream/123456789/30593/1/26243.pdf http://repositorio.ipen.br/bitstream/123456789/30593/2/license.txt |
bitstream.checksum.fl_str_mv |
763d2c06223d9dd9be15de02f5df48b2 8a4605be74aa9ea9d79846c1fba20a33 |
bitstream.checksumAlgorithm.fl_str_mv |
MD5 MD5 |
repository.name.fl_str_mv |
Repositório Institucional do IPEN - Instituto de Pesquisas Energéticas e Nucleares (IPEN) |
repository.mail.fl_str_mv |
bibl@ipen.br |
_version_ |
1767254249634267136 |