Biodistribution and Radiation Dosimetry of 18 F-FTC-146 in Humans
The purpose of this study was to assess safety, biodistribution, and radiation dosimetry in humans for the highly selective σ-1 receptor PET agent F-6-(3-fluoropropyl)-3-(2-(azepan-1-yl)ethyl)benzo[ ]thiazol-2(3H)-one ( F-FTC-146). Ten healthy volunteers (5 women, 5 men; age ± SD, 34.3 ± 6.5 y) were...
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| Veröffentlicht in: | Journal of Nuclear Medicine 2017-12, Vol.58 (12), p.2004-2009 |
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| container_title | Journal of Nuclear Medicine |
| container_volume | 58 |
| creator | Hjørnevik, Trine Cipriano, Peter W Shen, Bin Park, Jun Hyung Gulaka, Praveen Holley, Dawn Gandhi, Harsh Yoon, Daehyun Mittra, Erik S Zaharchuk, Greg Gambhir, Sanjiv S McCurdy, Christopher R Chin, Frederick T Biswal, Sandip |
| description | The purpose of this study was to assess safety, biodistribution, and radiation dosimetry in humans for the highly selective σ-1 receptor PET agent
F-6-(3-fluoropropyl)-3-(2-(azepan-1-yl)ethyl)benzo[
]thiazol-2(3H)-one (
F-FTC-146).
Ten healthy volunteers (5 women, 5 men; age ± SD, 34.3 ± 6.5 y) were recruited, and written informed consent was obtained from all participants. Series of whole-body PET/MRI examinations were acquired for up to 3 h after injection (357.2 ± 48.8 MBq). Blood samples were collected, and standard vital signs (heart rate, pulse oximetry, and body temperature) were monitored at regular intervals. Regions of interest were delineated, time-activity curves were calculated, and organ uptake and dosimetry were estimated.
All subjects tolerated the PET/MRI examination well, and no adverse reactions to
F-FTC-146 were reported. High accumulation of
F-FTC-146 was observed in σ-1 receptor-dense organs such as the pancreas and spleen, moderate uptake in the brain and myocardium, and low uptake in bone and muscle. High uptake was also observed in the kidneys and bladder, indicating renal tracer clearance. The effective dose of
F-FTC-146 was 0.0259 ± 0.0034 mSv/MBq (range, 0.0215-0.0301 mSv/MBq).
First-in-human studies with clinical-grade
F-FTC-146 were successful. Injection of
F-FTC-146 is safe, and absorbed doses are acceptable. The potential of
F-FTC-146 as an imaging agent for a variety of neuroinflammatory diseases is currently under investigation. |
| doi_str_mv | 10.2967/jnumed.117.192641 |
| format | Article |
| fullrecord | <record><control><sourceid>pubmed_cross</sourceid><recordid>TN_cdi_crossref_primary_10_2967_jnumed_117_192641</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>28572487</sourcerecordid><originalsourceid>FETCH-LOGICAL-c1137-2235243a5bc44407d15e60d4ce96ba47a91575e3eee478f1e2134cc7302b6c473</originalsourceid><addsrcrecordid>eNo1kM1Kw0AUhQdRbKw-gBuZF5g4d_6zrNFYoSBIXQ-TyQSmmKRkmkXf3tbY1eVw-Q6cD6FHoDkrlH7e9VMXmhxA51AwJeAKZSC5JFIpfY0yCgqIlFQu0F1KO0qpMsbcogUzUjNhdIZWL3FoYjqMsZ4Oceix6xv85Zro_tLrkGIXDuMRDy0GgytSbUsCQuHY4_XUuT7do5vW_aTw8H-X6Lt625Zrsvl8_yhXG-IBuCaMcckEd7L2QgiqG5BB0Ub4UKjaCe0KkFoGHkIQ2rQQGHDhveaU1coLzZcI5l4_DimNobX7MXZuPFqg9qzDzjrsSYeddZyYp5nZT_X5dSEu-_kviKpaJw</addsrcrecordid><sourcetype>Aggregation Database</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype></control><display><type>article</type><title>Biodistribution and Radiation Dosimetry of 18 F-FTC-146 in Humans</title><source>MEDLINE</source><source>Elektronische Zeitschriftenbibliothek - Frei zugängliche E-Journals</source><source>Alma/SFX Local Collection</source><creator>Hjørnevik, Trine ; Cipriano, Peter W ; Shen, Bin ; Park, Jun Hyung ; Gulaka, Praveen ; Holley, Dawn ; Gandhi, Harsh ; Yoon, Daehyun ; Mittra, Erik S ; Zaharchuk, Greg ; Gambhir, Sanjiv S ; McCurdy, Christopher R ; Chin, Frederick T ; Biswal, Sandip</creator><creatorcontrib>Hjørnevik, Trine ; Cipriano, Peter W ; Shen, Bin ; Park, Jun Hyung ; Gulaka, Praveen ; Holley, Dawn ; Gandhi, Harsh ; Yoon, Daehyun ; Mittra, Erik S ; Zaharchuk, Greg ; Gambhir, Sanjiv S ; McCurdy, Christopher R ; Chin, Frederick T ; Biswal, Sandip</creatorcontrib><description>The purpose of this study was to assess safety, biodistribution, and radiation dosimetry in humans for the highly selective σ-1 receptor PET agent
F-6-(3-fluoropropyl)-3-(2-(azepan-1-yl)ethyl)benzo[
]thiazol-2(3H)-one (
F-FTC-146).
Ten healthy volunteers (5 women, 5 men; age ± SD, 34.3 ± 6.5 y) were recruited, and written informed consent was obtained from all participants. Series of whole-body PET/MRI examinations were acquired for up to 3 h after injection (357.2 ± 48.8 MBq). Blood samples were collected, and standard vital signs (heart rate, pulse oximetry, and body temperature) were monitored at regular intervals. Regions of interest were delineated, time-activity curves were calculated, and organ uptake and dosimetry were estimated.
All subjects tolerated the PET/MRI examination well, and no adverse reactions to
F-FTC-146 were reported. High accumulation of
F-FTC-146 was observed in σ-1 receptor-dense organs such as the pancreas and spleen, moderate uptake in the brain and myocardium, and low uptake in bone and muscle. High uptake was also observed in the kidneys and bladder, indicating renal tracer clearance. The effective dose of
F-FTC-146 was 0.0259 ± 0.0034 mSv/MBq (range, 0.0215-0.0301 mSv/MBq).
First-in-human studies with clinical-grade
F-FTC-146 were successful. Injection of
F-FTC-146 is safe, and absorbed doses are acceptable. The potential of
F-FTC-146 as an imaging agent for a variety of neuroinflammatory diseases is currently under investigation.</description><identifier>ISSN: 0161-5505</identifier><identifier>EISSN: 1535-5667</identifier><identifier>EISSN: 2159-662X</identifier><identifier>DOI: 10.2967/jnumed.117.192641</identifier><identifier>PMID: 28572487</identifier><language>eng</language><publisher>United States</publisher><subject>Adult ; Azepines - adverse effects ; Azepines - chemical synthesis ; Azepines - pharmacokinetics ; Benzothiazoles - adverse effects ; Benzothiazoles - chemical synthesis ; Benzothiazoles - pharmacokinetics ; Female ; Healthy Volunteers ; Humans ; Isotope Labeling ; Magnetic Resonance Imaging ; Male ; Multimodal Imaging ; Radiometry ; Radiopharmaceuticals - adverse effects ; Radiopharmaceuticals - chemical synthesis ; Radiopharmaceuticals - pharmacokinetics ; Receptors, sigma - drug effects ; Receptors, sigma - metabolism ; Sigma-1 Receptor ; Tissue Distribution ; Whole Body Imaging</subject><ispartof>Journal of Nuclear Medicine, 2017-12, Vol.58 (12), p.2004-2009</ispartof><rights>2017 by the Society of Nuclear Medicine and Molecular Imaging.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c1137-2235243a5bc44407d15e60d4ce96ba47a91575e3eee478f1e2134cc7302b6c473</citedby><cites>FETCH-LOGICAL-c1137-2235243a5bc44407d15e60d4ce96ba47a91575e3eee478f1e2134cc7302b6c473</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,27924,27925</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/28572487$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Hjørnevik, Trine</creatorcontrib><creatorcontrib>Cipriano, Peter W</creatorcontrib><creatorcontrib>Shen, Bin</creatorcontrib><creatorcontrib>Park, Jun Hyung</creatorcontrib><creatorcontrib>Gulaka, Praveen</creatorcontrib><creatorcontrib>Holley, Dawn</creatorcontrib><creatorcontrib>Gandhi, Harsh</creatorcontrib><creatorcontrib>Yoon, Daehyun</creatorcontrib><creatorcontrib>Mittra, Erik S</creatorcontrib><creatorcontrib>Zaharchuk, Greg</creatorcontrib><creatorcontrib>Gambhir, Sanjiv S</creatorcontrib><creatorcontrib>McCurdy, Christopher R</creatorcontrib><creatorcontrib>Chin, Frederick T</creatorcontrib><creatorcontrib>Biswal, Sandip</creatorcontrib><title>Biodistribution and Radiation Dosimetry of 18 F-FTC-146 in Humans</title><title>Journal of Nuclear Medicine</title><addtitle>J Nucl Med</addtitle><description>The purpose of this study was to assess safety, biodistribution, and radiation dosimetry in humans for the highly selective σ-1 receptor PET agent
F-6-(3-fluoropropyl)-3-(2-(azepan-1-yl)ethyl)benzo[
]thiazol-2(3H)-one (
F-FTC-146).
Ten healthy volunteers (5 women, 5 men; age ± SD, 34.3 ± 6.5 y) were recruited, and written informed consent was obtained from all participants. Series of whole-body PET/MRI examinations were acquired for up to 3 h after injection (357.2 ± 48.8 MBq). Blood samples were collected, and standard vital signs (heart rate, pulse oximetry, and body temperature) were monitored at regular intervals. Regions of interest were delineated, time-activity curves were calculated, and organ uptake and dosimetry were estimated.
All subjects tolerated the PET/MRI examination well, and no adverse reactions to
F-FTC-146 were reported. High accumulation of
F-FTC-146 was observed in σ-1 receptor-dense organs such as the pancreas and spleen, moderate uptake in the brain and myocardium, and low uptake in bone and muscle. High uptake was also observed in the kidneys and bladder, indicating renal tracer clearance. The effective dose of
F-FTC-146 was 0.0259 ± 0.0034 mSv/MBq (range, 0.0215-0.0301 mSv/MBq).
First-in-human studies with clinical-grade
F-FTC-146 were successful. Injection of
F-FTC-146 is safe, and absorbed doses are acceptable. The potential of
F-FTC-146 as an imaging agent for a variety of neuroinflammatory diseases is currently under investigation.</description><subject>Adult</subject><subject>Azepines - adverse effects</subject><subject>Azepines - chemical synthesis</subject><subject>Azepines - pharmacokinetics</subject><subject>Benzothiazoles - adverse effects</subject><subject>Benzothiazoles - chemical synthesis</subject><subject>Benzothiazoles - pharmacokinetics</subject><subject>Female</subject><subject>Healthy Volunteers</subject><subject>Humans</subject><subject>Isotope Labeling</subject><subject>Magnetic Resonance Imaging</subject><subject>Male</subject><subject>Multimodal Imaging</subject><subject>Radiometry</subject><subject>Radiopharmaceuticals - adverse effects</subject><subject>Radiopharmaceuticals - chemical synthesis</subject><subject>Radiopharmaceuticals - pharmacokinetics</subject><subject>Receptors, sigma - drug effects</subject><subject>Receptors, sigma - metabolism</subject><subject>Sigma-1 Receptor</subject><subject>Tissue Distribution</subject><subject>Whole Body Imaging</subject><issn>0161-5505</issn><issn>1535-5667</issn><issn>2159-662X</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2017</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNo1kM1Kw0AUhQdRbKw-gBuZF5g4d_6zrNFYoSBIXQ-TyQSmmKRkmkXf3tbY1eVw-Q6cD6FHoDkrlH7e9VMXmhxA51AwJeAKZSC5JFIpfY0yCgqIlFQu0F1KO0qpMsbcogUzUjNhdIZWL3FoYjqMsZ4Oceix6xv85Zro_tLrkGIXDuMRDy0GgytSbUsCQuHY4_XUuT7do5vW_aTw8H-X6Lt625Zrsvl8_yhXG-IBuCaMcckEd7L2QgiqG5BB0Ub4UKjaCe0KkFoGHkIQ2rQQGHDhveaU1coLzZcI5l4_DimNobX7MXZuPFqg9qzDzjrsSYeddZyYp5nZT_X5dSEu-_kviKpaJw</recordid><startdate>201712</startdate><enddate>201712</enddate><creator>Hjørnevik, Trine</creator><creator>Cipriano, Peter W</creator><creator>Shen, Bin</creator><creator>Park, Jun Hyung</creator><creator>Gulaka, Praveen</creator><creator>Holley, Dawn</creator><creator>Gandhi, Harsh</creator><creator>Yoon, Daehyun</creator><creator>Mittra, Erik S</creator><creator>Zaharchuk, Greg</creator><creator>Gambhir, Sanjiv S</creator><creator>McCurdy, Christopher R</creator><creator>Chin, Frederick T</creator><creator>Biswal, Sandip</creator><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope></search><sort><creationdate>201712</creationdate><title>Biodistribution and Radiation Dosimetry of 18 F-FTC-146 in Humans</title><author>Hjørnevik, Trine ; Cipriano, Peter W ; Shen, Bin ; Park, Jun Hyung ; Gulaka, Praveen ; Holley, Dawn ; Gandhi, Harsh ; Yoon, Daehyun ; Mittra, Erik S ; Zaharchuk, Greg ; Gambhir, Sanjiv S ; McCurdy, Christopher R ; Chin, Frederick T ; Biswal, Sandip</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c1137-2235243a5bc44407d15e60d4ce96ba47a91575e3eee478f1e2134cc7302b6c473</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2017</creationdate><topic>Adult</topic><topic>Azepines - adverse effects</topic><topic>Azepines - chemical synthesis</topic><topic>Azepines - pharmacokinetics</topic><topic>Benzothiazoles - adverse effects</topic><topic>Benzothiazoles - chemical synthesis</topic><topic>Benzothiazoles - pharmacokinetics</topic><topic>Female</topic><topic>Healthy Volunteers</topic><topic>Humans</topic><topic>Isotope Labeling</topic><topic>Magnetic Resonance Imaging</topic><topic>Male</topic><topic>Multimodal Imaging</topic><topic>Radiometry</topic><topic>Radiopharmaceuticals - adverse effects</topic><topic>Radiopharmaceuticals - chemical synthesis</topic><topic>Radiopharmaceuticals - pharmacokinetics</topic><topic>Receptors, sigma - drug effects</topic><topic>Receptors, sigma - metabolism</topic><topic>Sigma-1 Receptor</topic><topic>Tissue Distribution</topic><topic>Whole Body Imaging</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Hjørnevik, Trine</creatorcontrib><creatorcontrib>Cipriano, Peter W</creatorcontrib><creatorcontrib>Shen, Bin</creatorcontrib><creatorcontrib>Park, Jun Hyung</creatorcontrib><creatorcontrib>Gulaka, Praveen</creatorcontrib><creatorcontrib>Holley, Dawn</creatorcontrib><creatorcontrib>Gandhi, Harsh</creatorcontrib><creatorcontrib>Yoon, Daehyun</creatorcontrib><creatorcontrib>Mittra, Erik S</creatorcontrib><creatorcontrib>Zaharchuk, Greg</creatorcontrib><creatorcontrib>Gambhir, Sanjiv S</creatorcontrib><creatorcontrib>McCurdy, Christopher R</creatorcontrib><creatorcontrib>Chin, Frederick T</creatorcontrib><creatorcontrib>Biswal, Sandip</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><jtitle>Journal of Nuclear Medicine</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Hjørnevik, Trine</au><au>Cipriano, Peter W</au><au>Shen, Bin</au><au>Park, Jun Hyung</au><au>Gulaka, Praveen</au><au>Holley, Dawn</au><au>Gandhi, Harsh</au><au>Yoon, Daehyun</au><au>Mittra, Erik S</au><au>Zaharchuk, Greg</au><au>Gambhir, Sanjiv S</au><au>McCurdy, Christopher R</au><au>Chin, Frederick T</au><au>Biswal, Sandip</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Biodistribution and Radiation Dosimetry of 18 F-FTC-146 in Humans</atitle><jtitle>Journal of Nuclear Medicine</jtitle><addtitle>J Nucl Med</addtitle><date>2017-12</date><risdate>2017</risdate><volume>58</volume><issue>12</issue><spage>2004</spage><epage>2009</epage><pages>2004-2009</pages><issn>0161-5505</issn><eissn>1535-5667</eissn><eissn>2159-662X</eissn><abstract>The purpose of this study was to assess safety, biodistribution, and radiation dosimetry in humans for the highly selective σ-1 receptor PET agent
F-6-(3-fluoropropyl)-3-(2-(azepan-1-yl)ethyl)benzo[
]thiazol-2(3H)-one (
F-FTC-146).
Ten healthy volunteers (5 women, 5 men; age ± SD, 34.3 ± 6.5 y) were recruited, and written informed consent was obtained from all participants. Series of whole-body PET/MRI examinations were acquired for up to 3 h after injection (357.2 ± 48.8 MBq). Blood samples were collected, and standard vital signs (heart rate, pulse oximetry, and body temperature) were monitored at regular intervals. Regions of interest were delineated, time-activity curves were calculated, and organ uptake and dosimetry were estimated.
All subjects tolerated the PET/MRI examination well, and no adverse reactions to
F-FTC-146 were reported. High accumulation of
F-FTC-146 was observed in σ-1 receptor-dense organs such as the pancreas and spleen, moderate uptake in the brain and myocardium, and low uptake in bone and muscle. High uptake was also observed in the kidneys and bladder, indicating renal tracer clearance. The effective dose of
F-FTC-146 was 0.0259 ± 0.0034 mSv/MBq (range, 0.0215-0.0301 mSv/MBq).
First-in-human studies with clinical-grade
F-FTC-146 were successful. Injection of
F-FTC-146 is safe, and absorbed doses are acceptable. The potential of
F-FTC-146 as an imaging agent for a variety of neuroinflammatory diseases is currently under investigation.</abstract><cop>United States</cop><pmid>28572487</pmid><doi>10.2967/jnumed.117.192641</doi><tpages>6</tpages></addata></record> |
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| source | MEDLINE; Elektronische Zeitschriftenbibliothek - Frei zugängliche E-Journals; Alma/SFX Local Collection |
| subjects | Adult Azepines - adverse effects Azepines - chemical synthesis Azepines - pharmacokinetics Benzothiazoles - adverse effects Benzothiazoles - chemical synthesis Benzothiazoles - pharmacokinetics Female Healthy Volunteers Humans Isotope Labeling Magnetic Resonance Imaging Male Multimodal Imaging Radiometry Radiopharmaceuticals - adverse effects Radiopharmaceuticals - chemical synthesis Radiopharmaceuticals - pharmacokinetics Receptors, sigma - drug effects Receptors, sigma - metabolism Sigma-1 Receptor Tissue Distribution Whole Body Imaging |
| title | Biodistribution and Radiation Dosimetry of 18 F-FTC-146 in Humans |
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