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Comparison of the Therapeutic Effects of [211At]NaAt and [131I]NaI in an NIS-Expressing Thyroid Cancer Mouse Model

Tadashi Watabe, Yuwei Liu, Kazuko Kaneda‐Nakashima, Tatsuhiko Sato, Yoshifumi Shirakami, Kazuhiro Ooe, Atsushi Toyoshima, Eku Shimosegawa, Yang Wang, Hiromitsu Haba, T. Nakano, Atsushi Shinohara, Jun Hatazawa

2022International Journal of Molecular Sciences32 citationsDOIOpen Access PDF

Abstract

Astatine (211At) is an alpha-emitter with a better treatment efficacy against differentiated thyroid cancer compared with iodine (131I), a conventional beta-emitter. However, its therapeutic comparison has not been fully evaluated. In this study, we compared the therapeutic effect between [211At]NaAt and [131I]NaI. In vitro analysis of a double-stranded DNA break (DSB) and colony formation assay were performed using K1-NIS cells. The therapeutic effect was compared using K1-NIS xenograft mice administered with [211At]NaAt (0.4 MBq (n = 7), 0.8 MBq (n = 9), and 1.2 MBq (n = 4)), and [131I]NaI (1 MBq (n = 4), 3 MBq (n = 4), and 8 MBq (n = 4)). The [211At]NaAt induced higher numbers of DSBs and had a more reduced colony formation than [131I]NaI. In K1-NIS mice, dose-dependent therapeutic effects were observed in both [211At]NaAt and [131I]NaI. In [211At]NaAt, a stronger tumour-growth suppression was observed, while tumour regrowth was not observed until 18, 25, and 46 days after injection of 0.4, 0.8, and 1.2 MBq of [211At]NaAt, respectively. While in [131I]NaI, this was observed within 12 days after injection (1, 3, and 8 MBq). The superior therapeutic effect of [211At]NaAt suggests the promising clinical applicability of targeted alpha therapy using [211At]NaAt in patients with differentiated thyroid cancer refractory to standard [131I]NaI treatment.

Topics & Concepts

Thyroid cancerRadioiodine therapyMedicineCancer researchTherapeutic effectCancerPharmacologyNuclear medicineInternal medicineRadiopharmaceutical Chemistry and ApplicationsThyroid Cancer Diagnosis and TreatmentMedical Imaging and Pathology Studies