First-in-human ¹⁸F-SiFAlin-TATE PET/CT for NET imaging and theranostics

Excerpt

The over-expression of somatostatin receptors (SSTR) on the cell surface of NET is the basis for SSTR-targeted PET imaging and radionuclide therapy. The visualization of SSTR-positive tumor lesions by SSTR-PET/CT or ¹¹¹In-pentetreotide imaging (OctreoScan) is a mandatory prerequisite for peptide receptor radionuclide therapy (PRRT) using ¹⁷⁷Lu-DOTA-TATE [1]. SSTR-targeted PET/CT with ⁶⁸Ga-DOTA-conjugated somatostatin analogs, such as ⁶⁸Ga-DOTA-TATE or ⁶⁸Ga-DOTA-TOC, is considered as the gold standard for imaging of well-differentiated NET [2] and has been approved by the FDA and EMA, recently. While the synthesis of ⁶⁸Ga-DOTA-conjugated peptides for NET imaging is well-established and reliable with relatively simple chemistry, the requirement of a cost-intensive ⁶⁸Ge-/⁶⁸Ga-generator, low activity amounts after single elution, and the short half-life of ⁶⁸Ga-labeled compounds constitute certain disadvantages. The development of cyclotron-derived, ¹⁸F-labeled compounds for NET imaging might solve these drawbacks. In this context, ¹⁸F-SiFAlin-TATE has been introduced as a promising agent for imaging of NET lesions in AR42J tumor-bearing mice [3]. …