Dosimetry and efficacy of a tau PET tracer [18F]MK-6240 in Japanese healthy elderly and patients with Alzheimer’s disease
Objective A new tau PET tracer [ 18 F]MK-6240 has been developed; however, its dosimetry and pharmacokinetics have been published only for a European population. This study investigated the safety, radiation dosimetry, pharmacokinetics and biodistribution of [ 18 F]MK-6240 in Japanese elderly subjec...
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| Veröffentlicht in: | Annals of nuclear medicine 2023-02, Vol.37 (2), p.108-120 |
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| creator | Ohnishi, Akihito Akamatsu, Go Ikari, Yasuhiko Nishida, Hiroyuki Shimizu, Keiji Matsumoto, Keiichi Aita, Kazuki Sasaki, Masahiro Yamamoto, Yasuji Yamane, Tomohiko Senda, Michio |
| description | Objective
A new tau PET tracer [
18
F]MK-6240 has been developed; however, its dosimetry and pharmacokinetics have been published only for a European population. This study investigated the safety, radiation dosimetry, pharmacokinetics and biodistribution of [
18
F]MK-6240 in Japanese elderly subjects. Also, the pattern and extent of brain retention of [
18
F]MK-6240 in Japanese healthy elderly subjects and patients with Alzheimer’s disease (AD) were investigated. These Japanese results were compared with previous reports on non-Japanese.
Methods
Three healthy elderly subjects and three AD patients were enrolled. Dynamic whole-body PET scans were acquired for up to 232 min after starting injection of [
18
F]MK-6240 (370.4 ± 27.0 MBq) for the former, while a dynamic brain scan was performed from 0 to 75 min post injection for the latter. For both groups, brain PET scans were conducted from 90 to 110 min post injection. Sequential venous blood sampling was performed to measure the radioactivity concentration in the whole blood and plasma as well as the percentages of parent [
18
F]MK-6240 and radioactive metabolites in plasma. Organ doses and effective doses were estimated using the OLINDA Ver.2 software. Standardized uptake value ratios (SUVRs) and distribution volume ratios (DVRs) by Logan reference tissue model (LRTM) were measured in eight brain regions using the cerebellar cortex as the reference. Blood tests, urine analysis, vital signs and electrocardiography were performed for safety assessments.
Results
No adverse events were observed. The highest radiation doses were received by the gallbladder (257.7 ± 74.9 μGy/MBq) and the urinary bladder (127.3 ± 11.7 μGy/MBq). The effective dose was 26.8 ± 1.4 μSv/MBq. The parent form ([
18
F]MK-6240) was metabolized quickly and was less than 15% by 35 min post injection. While no obvious accumulation was found in the brain of healthy subjects, focal accumulation of [
18
F]MK-6240 was observed in the cerebral cortex of AD patients. Regional SUVRs of the focal lesions in AD patients increased gradually over time, and the difference of SUVRs between healthy subjects and AD patients became large and stable at 90 min after injection. High correlations of SUVR and DVR were observed (
p
|
| doi_str_mv | 10.1007/s12149-022-01808-7 |
| format | Article |
| fullrecord | <record><control><sourceid>proquest_pubme</sourceid><recordid>TN_cdi_pubmedcentral_primary_oai_pubmedcentral_nih_gov_9902412</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>2773851060</sourcerecordid><originalsourceid>FETCH-LOGICAL-c498t-2b925ed40e94ccf9449d8c7ce962d2f8eda5a2c631c037e2d138107f07d5b03a3</originalsourceid><addsrcrecordid>eNp9kctu1DAUhi0EotPCC7BAllinHF8S2xukqrRAWwSLskLI8tgnTapMMrU9oIENr8Hr8SR1SSmwYXUW579JHyFPGOwzAPU8Mc6kqYDzCpgGXal7ZMF0I6tGCnGfLMAwWSmm1Q7ZTekSgOta84dkRzSSMVGrBfn2ckr9CnPcUjcGim3be-e3dGqpo9lt6Pujc5qj8xjpR6aPP709rRougfYjPXFrN2JC2qEbcrelOASMw5y0drnHMSf6pc8dPRi-dlh64s_vPxINfUKX8BF50Loh4ePbu0c-HB-dH76uzt69enN4cFZ5aXSu-NLwGoMENNL71khpgvbKo2l44K3G4GrHfSOYB6GQByY0A9WCCvUShBN75MWcu94sVxh8mRXdYNexX7m4tZPr7b-fse_sxfTZGgNcMl4Cnt0GxOlqgynby2kTx7LZcqWErhk0UFR8Vvk4pRSxvWtgYG-A2RmYLcDsL2BWFdPTv7fdWX4TKgIxC1J5jRcY_3T_J_YaniCidg</addsrcrecordid><sourcetype>Open Access Repository</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>2773851060</pqid></control><display><type>article</type><title>Dosimetry and efficacy of a tau PET tracer [18F]MK-6240 in Japanese healthy elderly and patients with Alzheimer’s disease</title><source>MEDLINE</source><source>SpringerLink Journals</source><creator>Ohnishi, Akihito ; Akamatsu, Go ; Ikari, Yasuhiko ; Nishida, Hiroyuki ; Shimizu, Keiji ; Matsumoto, Keiichi ; Aita, Kazuki ; Sasaki, Masahiro ; Yamamoto, Yasuji ; Yamane, Tomohiko ; Senda, Michio</creator><creatorcontrib>Ohnishi, Akihito ; Akamatsu, Go ; Ikari, Yasuhiko ; Nishida, Hiroyuki ; Shimizu, Keiji ; Matsumoto, Keiichi ; Aita, Kazuki ; Sasaki, Masahiro ; Yamamoto, Yasuji ; Yamane, Tomohiko ; Senda, Michio</creatorcontrib><description>Objective
A new tau PET tracer [
18
F]MK-6240 has been developed; however, its dosimetry and pharmacokinetics have been published only for a European population. This study investigated the safety, radiation dosimetry, pharmacokinetics and biodistribution of [
18
F]MK-6240 in Japanese elderly subjects. Also, the pattern and extent of brain retention of [
18
F]MK-6240 in Japanese healthy elderly subjects and patients with Alzheimer’s disease (AD) were investigated. These Japanese results were compared with previous reports on non-Japanese.
Methods
Three healthy elderly subjects and three AD patients were enrolled. Dynamic whole-body PET scans were acquired for up to 232 min after starting injection of [
18
F]MK-6240 (370.4 ± 27.0 MBq) for the former, while a dynamic brain scan was performed from 0 to 75 min post injection for the latter. For both groups, brain PET scans were conducted from 90 to 110 min post injection. Sequential venous blood sampling was performed to measure the radioactivity concentration in the whole blood and plasma as well as the percentages of parent [
18
F]MK-6240 and radioactive metabolites in plasma. Organ doses and effective doses were estimated using the OLINDA Ver.2 software. Standardized uptake value ratios (SUVRs) and distribution volume ratios (DVRs) by Logan reference tissue model (LRTM) were measured in eight brain regions using the cerebellar cortex as the reference. Blood tests, urine analysis, vital signs and electrocardiography were performed for safety assessments.
Results
No adverse events were observed. The highest radiation doses were received by the gallbladder (257.7 ± 74.9 μGy/MBq) and the urinary bladder (127.3 ± 11.7 μGy/MBq). The effective dose was 26.8 ± 1.4 μSv/MBq. The parent form ([
18
F]MK-6240) was metabolized quickly and was less than 15% by 35 min post injection. While no obvious accumulation was found in the brain of healthy subjects, focal accumulation of [
18
F]MK-6240 was observed in the cerebral cortex of AD patients. Regional SUVRs of the focal lesions in AD patients increased gradually over time, and the difference of SUVRs between healthy subjects and AD patients became large and stable at 90 min after injection. High correlations of SUVR and DVR were observed (
p
< 0.01).
Conclusion
The findings supported safety and efficacy of [
18
F]MK-6240 as a tau PET tracer for Japanese populations. Even though the number of subjects was limited, the radiation dosimetry profiles, pharmacokinetics, and biodistribution of [
18
F]MK-6240 were consistent with those for non-Japanese populations.
Trial registration
Japan Pharmaceutical Information Center ID, JapicCTI-194972.</description><identifier>ISSN: 0914-7187</identifier><identifier>EISSN: 1864-6433</identifier><identifier>DOI: 10.1007/s12149-022-01808-7</identifier><identifier>PMID: 36411357</identifier><language>eng</language><publisher>Singapore: Springer Nature Singapore</publisher><subject>Accumulation ; Aged ; Alzheimer Disease - diagnostic imaging ; Alzheimer Disease - metabolism ; Alzheimer's disease ; Biodistribution ; Blood ; Blood levels ; Brain ; Cerebellum ; Cerebral cortex ; Dosimeters ; Dosimetry ; Effectiveness ; EKG ; Electrocardiography ; Gallbladder ; Humans ; Imaging ; Information centers ; Injection ; Isoquinolines - metabolism ; Medicine ; Medicine & Public Health ; Metabolites ; Neurodegenerative diseases ; Nuclear Medicine ; Older people ; Original ; Original Article ; Pharmacokinetics ; Pharmacology ; Population studies ; Populations ; Positron emission ; Positron-Emission Tomography - methods ; Radiation ; Radiation dosage ; Radioactivity ; Radiology ; Radiometry ; Safety ; Tau protein ; Tissue Distribution</subject><ispartof>Annals of nuclear medicine, 2023-02, Vol.37 (2), p.108-120</ispartof><rights>The Author(s) 2022</rights><rights>2022. The Author(s).</rights><rights>The Author(s) 2022. This work is published under http://creativecommons.org/licenses/by/4.0/ (the “License”). Notwithstanding the ProQuest Terms and Conditions, you may use this content in accordance with the terms of the License.</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c498t-2b925ed40e94ccf9449d8c7ce962d2f8eda5a2c631c037e2d138107f07d5b03a3</citedby><cites>FETCH-LOGICAL-c498t-2b925ed40e94ccf9449d8c7ce962d2f8eda5a2c631c037e2d138107f07d5b03a3</cites><orcidid>0000-0002-7520-0942</orcidid></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://link.springer.com/content/pdf/10.1007/s12149-022-01808-7$$EPDF$$P50$$Gspringer$$Hfree_for_read</linktopdf><linktohtml>$$Uhttps://link.springer.com/10.1007/s12149-022-01808-7$$EHTML$$P50$$Gspringer$$Hfree_for_read</linktohtml><link.rule.ids>230,314,776,780,881,27901,27902,41464,42533,51294</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/36411357$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Ohnishi, Akihito</creatorcontrib><creatorcontrib>Akamatsu, Go</creatorcontrib><creatorcontrib>Ikari, Yasuhiko</creatorcontrib><creatorcontrib>Nishida, Hiroyuki</creatorcontrib><creatorcontrib>Shimizu, Keiji</creatorcontrib><creatorcontrib>Matsumoto, Keiichi</creatorcontrib><creatorcontrib>Aita, Kazuki</creatorcontrib><creatorcontrib>Sasaki, Masahiro</creatorcontrib><creatorcontrib>Yamamoto, Yasuji</creatorcontrib><creatorcontrib>Yamane, Tomohiko</creatorcontrib><creatorcontrib>Senda, Michio</creatorcontrib><title>Dosimetry and efficacy of a tau PET tracer [18F]MK-6240 in Japanese healthy elderly and patients with Alzheimer’s disease</title><title>Annals of nuclear medicine</title><addtitle>Ann Nucl Med</addtitle><addtitle>Ann Nucl Med</addtitle><description>Objective
A new tau PET tracer [
18
F]MK-6240 has been developed; however, its dosimetry and pharmacokinetics have been published only for a European population. This study investigated the safety, radiation dosimetry, pharmacokinetics and biodistribution of [
18
F]MK-6240 in Japanese elderly subjects. Also, the pattern and extent of brain retention of [
18
F]MK-6240 in Japanese healthy elderly subjects and patients with Alzheimer’s disease (AD) were investigated. These Japanese results were compared with previous reports on non-Japanese.
Methods
Three healthy elderly subjects and three AD patients were enrolled. Dynamic whole-body PET scans were acquired for up to 232 min after starting injection of [
18
F]MK-6240 (370.4 ± 27.0 MBq) for the former, while a dynamic brain scan was performed from 0 to 75 min post injection for the latter. For both groups, brain PET scans were conducted from 90 to 110 min post injection. Sequential venous blood sampling was performed to measure the radioactivity concentration in the whole blood and plasma as well as the percentages of parent [
18
F]MK-6240 and radioactive metabolites in plasma. Organ doses and effective doses were estimated using the OLINDA Ver.2 software. Standardized uptake value ratios (SUVRs) and distribution volume ratios (DVRs) by Logan reference tissue model (LRTM) were measured in eight brain regions using the cerebellar cortex as the reference. Blood tests, urine analysis, vital signs and electrocardiography were performed for safety assessments.
Results
No adverse events were observed. The highest radiation doses were received by the gallbladder (257.7 ± 74.9 μGy/MBq) and the urinary bladder (127.3 ± 11.7 μGy/MBq). The effective dose was 26.8 ± 1.4 μSv/MBq. The parent form ([
18
F]MK-6240) was metabolized quickly and was less than 15% by 35 min post injection. While no obvious accumulation was found in the brain of healthy subjects, focal accumulation of [
18
F]MK-6240 was observed in the cerebral cortex of AD patients. Regional SUVRs of the focal lesions in AD patients increased gradually over time, and the difference of SUVRs between healthy subjects and AD patients became large and stable at 90 min after injection. High correlations of SUVR and DVR were observed (
p
< 0.01).
Conclusion
The findings supported safety and efficacy of [
18
F]MK-6240 as a tau PET tracer for Japanese populations. Even though the number of subjects was limited, the radiation dosimetry profiles, pharmacokinetics, and biodistribution of [
18
F]MK-6240 were consistent with those for non-Japanese populations.
Trial registration
Japan Pharmaceutical Information Center ID, JapicCTI-194972.</description><subject>Accumulation</subject><subject>Aged</subject><subject>Alzheimer Disease - diagnostic imaging</subject><subject>Alzheimer Disease - metabolism</subject><subject>Alzheimer's disease</subject><subject>Biodistribution</subject><subject>Blood</subject><subject>Blood levels</subject><subject>Brain</subject><subject>Cerebellum</subject><subject>Cerebral cortex</subject><subject>Dosimeters</subject><subject>Dosimetry</subject><subject>Effectiveness</subject><subject>EKG</subject><subject>Electrocardiography</subject><subject>Gallbladder</subject><subject>Humans</subject><subject>Imaging</subject><subject>Information centers</subject><subject>Injection</subject><subject>Isoquinolines - metabolism</subject><subject>Medicine</subject><subject>Medicine & Public Health</subject><subject>Metabolites</subject><subject>Neurodegenerative diseases</subject><subject>Nuclear Medicine</subject><subject>Older people</subject><subject>Original</subject><subject>Original Article</subject><subject>Pharmacokinetics</subject><subject>Pharmacology</subject><subject>Population studies</subject><subject>Populations</subject><subject>Positron emission</subject><subject>Positron-Emission Tomography - methods</subject><subject>Radiation</subject><subject>Radiation dosage</subject><subject>Radioactivity</subject><subject>Radiology</subject><subject>Radiometry</subject><subject>Safety</subject><subject>Tau protein</subject><subject>Tissue Distribution</subject><issn>0914-7187</issn><issn>1864-6433</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2023</creationdate><recordtype>article</recordtype><sourceid>C6C</sourceid><sourceid>EIF</sourceid><recordid>eNp9kctu1DAUhi0EotPCC7BAllinHF8S2xukqrRAWwSLskLI8tgnTapMMrU9oIENr8Hr8SR1SSmwYXUW579JHyFPGOwzAPU8Mc6kqYDzCpgGXal7ZMF0I6tGCnGfLMAwWSmm1Q7ZTekSgOta84dkRzSSMVGrBfn2ckr9CnPcUjcGim3be-e3dGqpo9lt6Pujc5qj8xjpR6aPP709rRougfYjPXFrN2JC2qEbcrelOASMw5y0drnHMSf6pc8dPRi-dlh64s_vPxINfUKX8BF50Loh4ePbu0c-HB-dH76uzt69enN4cFZ5aXSu-NLwGoMENNL71khpgvbKo2l44K3G4GrHfSOYB6GQByY0A9WCCvUShBN75MWcu94sVxh8mRXdYNexX7m4tZPr7b-fse_sxfTZGgNcMl4Cnt0GxOlqgynby2kTx7LZcqWErhk0UFR8Vvk4pRSxvWtgYG-A2RmYLcDsL2BWFdPTv7fdWX4TKgIxC1J5jRcY_3T_J_YaniCidg</recordid><startdate>20230201</startdate><enddate>20230201</enddate><creator>Ohnishi, Akihito</creator><creator>Akamatsu, Go</creator><creator>Ikari, Yasuhiko</creator><creator>Nishida, Hiroyuki</creator><creator>Shimizu, Keiji</creator><creator>Matsumoto, Keiichi</creator><creator>Aita, Kazuki</creator><creator>Sasaki, Masahiro</creator><creator>Yamamoto, Yasuji</creator><creator>Yamane, Tomohiko</creator><creator>Senda, Michio</creator><general>Springer Nature Singapore</general><general>Springer Nature B.V</general><scope>C6C</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7QP</scope><scope>7TK</scope><scope>K9.</scope><scope>NAPCQ</scope><scope>5PM</scope><orcidid>https://orcid.org/0000-0002-7520-0942</orcidid></search><sort><creationdate>20230201</creationdate><title>Dosimetry and efficacy of a tau PET tracer [18F]MK-6240 in Japanese healthy elderly and patients with Alzheimer’s disease</title><author>Ohnishi, Akihito ; Akamatsu, Go ; Ikari, Yasuhiko ; Nishida, Hiroyuki ; Shimizu, Keiji ; Matsumoto, Keiichi ; Aita, Kazuki ; Sasaki, Masahiro ; Yamamoto, Yasuji ; Yamane, Tomohiko ; Senda, Michio</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c498t-2b925ed40e94ccf9449d8c7ce962d2f8eda5a2c631c037e2d138107f07d5b03a3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2023</creationdate><topic>Accumulation</topic><topic>Aged</topic><topic>Alzheimer Disease - diagnostic imaging</topic><topic>Alzheimer Disease - metabolism</topic><topic>Alzheimer's disease</topic><topic>Biodistribution</topic><topic>Blood</topic><topic>Blood levels</topic><topic>Brain</topic><topic>Cerebellum</topic><topic>Cerebral cortex</topic><topic>Dosimeters</topic><topic>Dosimetry</topic><topic>Effectiveness</topic><topic>EKG</topic><topic>Electrocardiography</topic><topic>Gallbladder</topic><topic>Humans</topic><topic>Imaging</topic><topic>Information centers</topic><topic>Injection</topic><topic>Isoquinolines - metabolism</topic><topic>Medicine</topic><topic>Medicine & Public Health</topic><topic>Metabolites</topic><topic>Neurodegenerative diseases</topic><topic>Nuclear Medicine</topic><topic>Older people</topic><topic>Original</topic><topic>Original Article</topic><topic>Pharmacokinetics</topic><topic>Pharmacology</topic><topic>Population studies</topic><topic>Populations</topic><topic>Positron emission</topic><topic>Positron-Emission Tomography - methods</topic><topic>Radiation</topic><topic>Radiation dosage</topic><topic>Radioactivity</topic><topic>Radiology</topic><topic>Radiometry</topic><topic>Safety</topic><topic>Tau protein</topic><topic>Tissue Distribution</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Ohnishi, Akihito</creatorcontrib><creatorcontrib>Akamatsu, Go</creatorcontrib><creatorcontrib>Ikari, Yasuhiko</creatorcontrib><creatorcontrib>Nishida, Hiroyuki</creatorcontrib><creatorcontrib>Shimizu, Keiji</creatorcontrib><creatorcontrib>Matsumoto, Keiichi</creatorcontrib><creatorcontrib>Aita, Kazuki</creatorcontrib><creatorcontrib>Sasaki, Masahiro</creatorcontrib><creatorcontrib>Yamamoto, Yasuji</creatorcontrib><creatorcontrib>Yamane, Tomohiko</creatorcontrib><creatorcontrib>Senda, Michio</creatorcontrib><collection>Springer Nature OA Free Journals</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Calcium & Calcified Tissue Abstracts</collection><collection>Neurosciences Abstracts</collection><collection>ProQuest Health & Medical Complete (Alumni)</collection><collection>Nursing & Allied Health Premium</collection><collection>PubMed Central (Full Participant titles)</collection><jtitle>Annals of nuclear medicine</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Ohnishi, Akihito</au><au>Akamatsu, Go</au><au>Ikari, Yasuhiko</au><au>Nishida, Hiroyuki</au><au>Shimizu, Keiji</au><au>Matsumoto, Keiichi</au><au>Aita, Kazuki</au><au>Sasaki, Masahiro</au><au>Yamamoto, Yasuji</au><au>Yamane, Tomohiko</au><au>Senda, Michio</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Dosimetry and efficacy of a tau PET tracer [18F]MK-6240 in Japanese healthy elderly and patients with Alzheimer’s disease</atitle><jtitle>Annals of nuclear medicine</jtitle><stitle>Ann Nucl Med</stitle><addtitle>Ann Nucl Med</addtitle><date>2023-02-01</date><risdate>2023</risdate><volume>37</volume><issue>2</issue><spage>108</spage><epage>120</epage><pages>108-120</pages><issn>0914-7187</issn><eissn>1864-6433</eissn><abstract>Objective
A new tau PET tracer [
18
F]MK-6240 has been developed; however, its dosimetry and pharmacokinetics have been published only for a European population. This study investigated the safety, radiation dosimetry, pharmacokinetics and biodistribution of [
18
F]MK-6240 in Japanese elderly subjects. Also, the pattern and extent of brain retention of [
18
F]MK-6240 in Japanese healthy elderly subjects and patients with Alzheimer’s disease (AD) were investigated. These Japanese results were compared with previous reports on non-Japanese.
Methods
Three healthy elderly subjects and three AD patients were enrolled. Dynamic whole-body PET scans were acquired for up to 232 min after starting injection of [
18
F]MK-6240 (370.4 ± 27.0 MBq) for the former, while a dynamic brain scan was performed from 0 to 75 min post injection for the latter. For both groups, brain PET scans were conducted from 90 to 110 min post injection. Sequential venous blood sampling was performed to measure the radioactivity concentration in the whole blood and plasma as well as the percentages of parent [
18
F]MK-6240 and radioactive metabolites in plasma. Organ doses and effective doses were estimated using the OLINDA Ver.2 software. Standardized uptake value ratios (SUVRs) and distribution volume ratios (DVRs) by Logan reference tissue model (LRTM) were measured in eight brain regions using the cerebellar cortex as the reference. Blood tests, urine analysis, vital signs and electrocardiography were performed for safety assessments.
Results
No adverse events were observed. The highest radiation doses were received by the gallbladder (257.7 ± 74.9 μGy/MBq) and the urinary bladder (127.3 ± 11.7 μGy/MBq). The effective dose was 26.8 ± 1.4 μSv/MBq. The parent form ([
18
F]MK-6240) was metabolized quickly and was less than 15% by 35 min post injection. While no obvious accumulation was found in the brain of healthy subjects, focal accumulation of [
18
F]MK-6240 was observed in the cerebral cortex of AD patients. Regional SUVRs of the focal lesions in AD patients increased gradually over time, and the difference of SUVRs between healthy subjects and AD patients became large and stable at 90 min after injection. High correlations of SUVR and DVR were observed (
p
< 0.01).
Conclusion
The findings supported safety and efficacy of [
18
F]MK-6240 as a tau PET tracer for Japanese populations. Even though the number of subjects was limited, the radiation dosimetry profiles, pharmacokinetics, and biodistribution of [
18
F]MK-6240 were consistent with those for non-Japanese populations.
Trial registration
Japan Pharmaceutical Information Center ID, JapicCTI-194972.</abstract><cop>Singapore</cop><pub>Springer Nature Singapore</pub><pmid>36411357</pmid><doi>10.1007/s12149-022-01808-7</doi><tpages>13</tpages><orcidid>https://orcid.org/0000-0002-7520-0942</orcidid><oa>free_for_read</oa></addata></record> |
| fulltext | fulltext |
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| ispartof | Annals of nuclear medicine, 2023-02, Vol.37 (2), p.108-120 |
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| language | eng |
| recordid | cdi_pubmedcentral_primary_oai_pubmedcentral_nih_gov_9902412 |
| source | MEDLINE; SpringerLink Journals |
| subjects | Accumulation Aged Alzheimer Disease - diagnostic imaging Alzheimer Disease - metabolism Alzheimer's disease Biodistribution Blood Blood levels Brain Cerebellum Cerebral cortex Dosimeters Dosimetry Effectiveness EKG Electrocardiography Gallbladder Humans Imaging Information centers Injection Isoquinolines - metabolism Medicine Medicine & Public Health Metabolites Neurodegenerative diseases Nuclear Medicine Older people Original Original Article Pharmacokinetics Pharmacology Population studies Populations Positron emission Positron-Emission Tomography - methods Radiation Radiation dosage Radioactivity Radiology Radiometry Safety Tau protein Tissue Distribution |
| title | Dosimetry and efficacy of a tau PET tracer [18F]MK-6240 in Japanese healthy elderly and patients with Alzheimer’s disease |
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