[Advances in Cardiac Sympathetic PET Imaging: Development and Clinical Translation of ¹⁸F-fluproxadine (¹⁸F-AF78)].

Authors

Naoko Nose, Takahiro Higuchi

Published in

Kaku igaku. The Japanese journal of nuclear medicine. Volume 63. Issue 1. Pages 61-68.

Abstract

The cardiac sympathetic nervous system plays an important role in the pathophysiology and prognosis of heart failure, ischemic heart disease, and arrhythmias. Cardiac sympathetic innervation has traditionally been assessed using ¹²³I-meta-iodobenzylguanidine (¹²³I-MIBG) SPECT and ¹¹C-hydroxyephedrine (¹¹C-HED) PET. However, these approaches have limitations related to spatial resolution, quantitative capability, physical half-life, and dependence on specialized facilities. ¹⁸F-fluproxadine, formerly known as ¹⁸F-AF78, is a novel PET tracer targeting the norepinephrine transporter (NET) at sympathetic nerve terminals. Preclinical studies have demonstrated its high NET affinity, favorable myocardial uptake, and potential to reflect intravesicular neuronal dynamics. In addition, structure-activity relationship analyses, investigations of interactions with organic cation transporters (OCTs), development of a clinical radiosynthesis method, and First-in-Human evaluation have provided a foundation for clinical translation. This review summarizes the development of ¹⁸F-fluproxadine PET and discusses future perspectives for cardiac sympathetic nerve imaging.

PMID:
42907381
Bibliographic data and abstract were imported from PubMed on 23 Oct 2026.

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