Enhanced tumor retention of the novel LAT1-targeting PET probe [¹⁸F]FAMT-OMe: A comparative study with [¹⁸F]FAMT in glioma mouse models

Sampunta, Thosapol; Watabe, Tadashi; Naka, Sadahiro; Kaneda-Nakashima, Kazuko; Ohta, Yoichiro; Kobayashi, Takanori; Kurimoto, Kenta; Isohashi, Kayako; Tatsumi, Mitsuaki; Kato, Hiroki; Kanai, Yoshikatsu; Kirihata, Mitsunori; Tomiyama, Noriyuki

doi:https://doi.org/10.1016/j.nucmedbio.2026.109623

Enhanced tumor retention of the novel LAT1-targeting PET probe [¹⁸F]FAMT-OMe: A comparative study with [¹⁸F]FAMT in glioma mouse models

Sampunta, Thosapol; Watabe, Tadashi; Naka, Sadahiro et al.

Nuclear Medicine and Biology, 2026, 156–157, 109623

アクセス数:7件（2026-06-01 02:59 集計）

固定URL: https://hdl.handle.net/11094/104836

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タイトル	Enhanced tumor retention of the novel LAT1-targeting PET probe [¹⁸F]FAMT-OMe: A comparative study with [¹⁸F]FAMT in glioma mouse models
著者	著者名 Sampunta, Thosapol
	NRID 1000090648932 1000090648932 ORCID 0000-0001-8658-2395 0000-0001-8658-2395 researchmap permalink twosaka2018 twosaka2018 Scopus Author ID 57421862900 57421862900 著者名 Watabe, Tadashi
	NRID 1000060599843 1000060599843 researchmap permalink _sada_ _sada_ 著者名 Naka, Sadahiro
	NRID 1000000533209 1000000533209 ORCID 0000-0001-6657-5059 0000-0001-6657-5059 researchmap permalink read0131912 read0131912 著者名 Kaneda-Nakashima, Kazuko
	NRID 1000040716023 1000040716023 著者名 Ohta, Yoichiro
	著者名 Kobayashi, Takanori
	NRID 1000070868968 1000070868968 researchmap permalink kentakuri kentakuri Scopus Author ID 57223821707 57223821707 著者名 Kurimoto, Kenta
	NRID 1000050598604 1000050598604 ORCID 0000-0002-2081-3020 0000-0002-2081-3020 researchmap permalink researchmap5849 researchmap5849 Scopus Author ID 6505990065 6505990065 著者名 Isohashi, Kayako
	NRID 1000060397700 1000060397700 ORCID 0000-0003-1778-0421 0000-0003-1778-0421 researchmap permalink mtatsumi mtatsumi Scopus Author ID 7102266657 7102266657 著者名 Tatsumi, Mitsuaki
	NRID 1000020448054 1000020448054 ORCID 0000-0003-0838-6772 0000-0003-0838-6772 researchmap permalink kato-h kato-h Scopus Author ID 55585587900 55585587900 著者名 Kato, Hiroki
	NRID 1000060204533 1000060204533 researchmap permalink read0063550 read0063550 Scopus Author ID 55575124400 55575124400 著者名 Kanai, Yoshikatsu
	著者名 Kirihata, Mitsunori
	NRID 1000050294070 1000050294070 ORCID 0000-0001-9918-7327 0000-0001-9918-7327 researchmap permalink 3430 3430 Scopus Author ID 7006024942 7006024942 著者名 Tomiyama, Noriyuki
キーワード等	FAMT
	LAT1
	Oncology
	PET
	Small animal imaging
内容	Sampunta T., Watabe T., Naka S., et al. Enhanced tumor retention of the novel LAT1-targeting PET probe [¹⁸F]FAMT-OMe: A comparative study with [¹⁸F]FAMT in glioma mouse models. Nuclear Medicine and Biology 156–157, 109623 (2026); https://doi.org/10.1016/j.nucmedbio.2026.109623.
抄録	Introduction: [¹⁸F]fluoro-L-α-methyltyrosine ([¹⁸F]FAMT) has been reported as a positron-emission tomography (PET) probe that has high specificity for L-type amino acid transporter 1 (LAT1), which is overexpressed in various malignant tumors. However, [¹⁸F]FAMT showed rapid washout from the tumor and high retention in the kidney. This study aimed to develop and evaluate a novel LAT1-targeting PET probe, [¹⁸F]FAMT-OMe, and compare its performance with [¹⁸F]FAMT in glioma xenograft mice. Methods: [¹⁸F]-FAMT-OMe was synthesized via nucleophilic substitution. The uptake of [¹⁸F]FAMT-OMe and [¹⁸F]FAMT was compared in in vitro studies using C6 glioma and U-87MG cells. PET scans were performed on C6 glioma- and U-87MG tumor-bearing mice (n = 20 each) following intravenous administration of either [¹⁸F]FAMT-OMe or [¹⁸F]FAMT. After PET/computed tomography (CT) imaging, the organs were weighed and the radioactivity present was measured using a gamma counter. Results: In vitro analyses demonstrated higher uptake of [¹⁸F]FAMT-OMe compared with [¹⁸F]FAMT in both C6 and U-87MG cells. PET imaging demonstrated significantly greater tumor retention of [¹⁸F]FAMT-OMe than [¹⁸F]FAMT (SUVmax at 60 min in C6 glioma: 2.13 ± 0.39 vs. 1.09 ± 0.79, P < 0.05). The kidneys and urine showed significantly lower uptake and excretion of [¹⁸F]FAMT-OMe than [¹⁸F]FAMT (kidney uptake: SUVmean 3.75 ± 0.89 vs. 5.55 ± 2.44, P < 0.05 urine excretion: SUVmean 16.50 ± 7.65 vs. 34.38 ± 8.74, P < 0.05), while blood retention of [¹⁸F]FAMT-OMe was significantly increased (SUVmean 1.78 ± 0.85 vs. 1.20 ± 0.82, P < 0.05). Conclusion: [¹⁸F]FAMT-OMe showed improved tumor retention on PET compared with [¹⁸F]FAMT in the C6 glioma tumor model, suggesting its potential utility for future applications in LAT1-targeted PET.
出版者	Elsevier Inc.
収録物名	Nuclear Medicine and Biology
巻(号)	156–157
ページ	109623
刊行年月	2026-03-18
言語	英語
ハンドルURL	https://hdl.handle.net/11094/104836
PISSN	09698051
eISSN	18729614
関連情報 (isIdenticalTo)	DOI (出版社版) https://doi.org/10.1016/j.nucmedbio.2026.109623
アクセス権	open access
権利情報	This article is licensed under a Creative Commons Attribution 4.0 International License.
出版タイプ	Version of Record
カテゴリ	学術雑誌論文 Journal Article

資源タイプ	学術雑誌論文
ローカル資源タイプ	学術雑誌論文
DCMI資源タイプ	text
DCTERMS.bibliographicCitation	Nuclear Medicine and Biology. 2026, 156–157, p. 109623
DC.title	Enhanced tumor retention of the novel LAT1-targeting PET probe [¹⁸F]FAMT-OMe: A comparative study with [¹⁸F]FAMT in glioma mouse models
DC.creator	Sampunta, Thosapol
	Watabe, Tadashi
	Naka, Sadahiro
	Kaneda-Nakashima, Kazuko
	Ohta, Yoichiro
	Kobayashi, Takanori
	Kurimoto, Kenta
	Isohashi, Kayako
	Tatsumi, Mitsuaki
	Kato, Hiroki
	Kanai, Yoshikatsu
	Kirihata, Mitsunori
	Tomiyama, Noriyuki
DC.publisher	Elsevier Inc.
DC.language' scheme='DCTERMS.RFC1766	英語
DC.type' scheme='DCTERMS.DCMIType	text
DCTERMS.issued' scheme='DCTERMS.W3CDTF	2026-03-18
DC.identifier	https://doi.org/10.1016/j.nucmedbio.2026.109623
DC.subject	FAMT
	LAT1
	Oncology
	PET
	Small animal imaging
DC.description	Sampunta T., Watabe T., Naka S., et al. Enhanced tumor retention of the novel LAT1-targeting PET probe [¹⁸F]FAMT-OMe: A comparative study with [¹⁸F]FAMT in glioma mouse models. Nuclear Medicine and Biology 156–157, 109623 (2026); https://doi.org/10.1016/j.nucmedbio.2026.109623.
DCTERMS.abstract	Introduction: [¹⁸F]fluoro-L-α-methyltyrosine ([¹⁸F]FAMT) has been reported as a positron-emission tomography (PET) probe that has high specificity for L-type amino acid transporter 1 (LAT1), which is overexpressed in various malignant tumors. However, [¹⁸F]FAMT showed rapid washout from the tumor and high retention in the kidney. This study aimed to develop and evaluate a novel LAT1-targeting PET probe, [¹⁸F]FAMT-OMe, and compare its performance with [¹⁸F]FAMT in glioma xenograft mice. Methods: [¹⁸F]-FAMT-OMe was synthesized via nucleophilic substitution. The uptake of [¹⁸F]FAMT-OMe and [¹⁸F]FAMT was compared in in vitro studies using C6 glioma and U-87MG cells. PET scans were performed on C6 glioma- and U-87MG tumor-bearing mice (n = 20 each) following intravenous administration of either [¹⁸F]FAMT-OMe or [¹⁸F]FAMT. After PET/computed tomography (CT) imaging, the organs were weighed and the radioactivity present was measured using a gamma counter. Results: In vitro analyses demonstrated higher uptake of [¹⁸F]FAMT-OMe compared with [¹⁸F]FAMT in both C6 and U-87MG cells. PET imaging demonstrated significantly greater tumor retention of [¹⁸F]FAMT-OMe than [¹⁸F]FAMT (SUVmax at 60 min in C6 glioma: 2.13 ± 0.39 vs. 1.09 ± 0.79, P < 0.05). The kidneys and urine showed significantly lower uptake and excretion of [¹⁸F]FAMT-OMe than [¹⁸F]FAMT (kidney uptake: SUVmean 3.75 ± 0.89 vs. 5.55 ± 2.44, P < 0.05 urine excretion: SUVmean 16.50 ± 7.65 vs. 34.38 ± 8.74, P < 0.05), while blood retention of [¹⁸F]FAMT-OMe was significantly increased (SUVmean 1.78 ± 0.85 vs. 1.20 ± 0.82, P < 0.05). Conclusion: [¹⁸F]FAMT-OMe showed improved tumor retention on PET compared with [¹⁸F]FAMT in the C6 glioma tumor model, suggesting its potential utility for future applications in LAT1-targeted PET.
DC.rights	This article is licensed under a Creative Commons Attribution 4.0 International License.
DC.format	104836
citation_title	Enhanced tumor retention of the novel LAT1-targeting PET probe [¹⁸F]FAMT-OMe: A comparative study with [¹⁸F]FAMT in glioma mouse models
citation_author	Sampunta, Thosapol
	Watabe, Tadashi
	Naka, Sadahiro
	Kaneda-Nakashima, Kazuko
	Ohta, Yoichiro
	Kobayashi, Takanori
	Kurimoto, Kenta
	Isohashi, Kayako
	Tatsumi, Mitsuaki
	Kato, Hiroki
	Kanai, Yoshikatsu
	Kirihata, Mitsunori
	Tomiyama, Noriyuki
citation_publisher	Elsevier Inc.
citation_language	英語
citation_date	2026-03-18
citation_journal_title	Nuclear Medicine and Biology
citation_volume	156–157
citation_firstpage	109623
citation_doi	https://doi.org/10.1016/j.nucmedbio.2026.109623
citation_public_url	https://hdl.handle.net/11094/104836

Enhanced tumor retention of the novel LAT1-targeting PET probe [¹⁸F]FAMT-OMe: A comparative study with [¹⁸F]FAMT in glioma mouse models

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