The preclinical study of 177Lu-DOTA-LTVSPWY as a potential therapeutic agent against HER2 overexpressed cancer

Background Peptide receptor radionuclide therapy (PRRT) has evolved in cancer therapy and diagnosis. LTVSPWY, as a peptide, can target HER2 receptor; on the other hand, 177Lu emits $ β^{−} $ which is helpful for cancer therapy. The radiolabeling of LTVSPWY with 177Lu results in a therapeutic agent (177Lu-DOTA-LTVSPWY) capable of cancer treatment. Methods 177Lu-DOTA-LTVSPWY was prepared with high radiochemical purity (RCP). The stability was investigated in saline and human serum. The radiotracer affinity toward the SKOV-3 cell line with overexpression of the HER2 receptor was evaluated. Then the impact of the radiotracer on the colony formation of the SKOV-3 cell line was investigated with colony assay. Moreover, the biodistribution of this radiotracer in SKOV-3 xenograft tumor-bearing nude mice were also studied to determine the radiotracer accumulation in the tumor site. The mice were treated with 177Lu-DOTA-LTVSPWY and subjected to histopathological evaluation. Results The RCP of 177Lu-DOTA-LTVSPWY after radiolabeling and stability tests was more than 97.7%. The radiotracer displayed high affinity toward the SKOV-3 cell line (KD = 6.6 ± 3.2 nM). Treatment of the SKOV-3 cell line with the radiotracer reduces the SKOV-3 colony survival to less than 3% for 5 MBq of the radiotracer. Tumor-to-muscle (T/M) ratio is the highest at 48 h and 1 h post-injection (2.3 and 4.75, respectively). The histopathological study also confirms the cellular damage to the tumor tissue. Conclusions 177Lu-DOTA-LTVSPWY can recognize HER2 receptors in vivo and in vitro; hence, it can serve as a therapeutic agent..

Medienart:

E-Artikel

Erscheinungsjahr:

2023

Erschienen:

2023

Enthalten in:

Zur Gesamtaufnahme - volume:37

Enthalten in:

Annals of nuclear medicine - 37(2023), 7 vom: 28. Apr., Seite 400-409

Sprache:

Englisch

Beteiligte Personen:

Molavipordanjani, Sajjad [VerfasserIn]
Mousavi, Tahoora [VerfasserIn]
Khorramimoghaddam, Alireza [VerfasserIn]
Talebpour Amiri, Fereshteh [VerfasserIn]
Abedi, Seyed Mohammad [VerfasserIn]
Hosseinimehr, Seyed Jalal [VerfasserIn]

Links:

Volltext [lizenzpflichtig]

BKL:

44.64$jRadiologie

Themen:

HER2
LTVSPWY
Lu
PRRT
Radiolabeled peptide
Therapy

Anmerkungen:

© The Author(s) under exclusive licence to The Japanese Society of Nuclear Medicine 2023. Springer Nature or its licensor (e.g. a society or other partner) holds exclusive rights to this article under a publishing agreement with the author(s) or other rightsholder(s); author self-archiving of the accepted manuscript version of this article is solely governed by the terms of such publishing agreement and applicable law.

doi:

10.1007/s12149-023-01839-8

funding:

Förderinstitution / Projekttitel:

PPN (Katalog-ID):

OLC2144016216

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