Synthesis, preclinical evaluation and a pilot clinical imaging study of [18F]AlF-NODA-JR11 for neuroendocrine neoplasms compared with [68Ga]Ga-DOTA-TATE

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Introduction: [68Ga]Ga (87% β+, 0.83Mev, T1/2=68min) is widely used associate with SSTR agonist and antagonist in molecular imaging of NETs. [18F]F (97% β+, 0.64Mev, T1/2=109min) has suitable half-life for peptide and lower β+-trajectory (<2mm) leading to excellent imaging resolution. Moreover, [18F]F provided by cyclotron can cover enough radiolabelling requirement.

Aim(s): A [18F]AlF-labelled SSTR antagonist was developed for imaging of neuroendocrine neoplasms (NENs), evaluated and compared with [68Ga]Ga-DOTA-TATE.

Materials and methods: [18F]AlF-NODA-JR11 was synthesized manually and qualified with HPLC and LC-MS. The cell uptake, internalization, saturation binding and biodistribution were performed with HEK293-SSTR2 cells and tumor-bearing mice. PET/CT and PET/MR imaging with [18F]AlF-NODA-JR11 and [68Ga]Ga-DOTA-TATE were performed with ten NEN patients.

Conference: 18th Annual ENETS Concerence (2021)

Presenting Author: Yu J

Authors: Yu J, X Q, Lu M, Li J, Y Z,

Keywords: neuroendocrine neoplasm, somatostatin receptor, [18F]AlF, JR11, TATE, PET imaging,