Preclinical and preliminary clinical evaluation of [18F]Florbetazine for non-invasive PET detection of cardiac amyloidosis
Abstract
Purpose: Early detection of cardiac amyloidosis (CA) remains challenging, and a PET tracer capable of directly visualizing amyloid deposits could improve diagnosis. Given the shared β-sheet structure of amyloid deposits in CA and Alzheimer's disease (AD), this study aimed to evaluate the suitability of the AD amyloid tracer [18F]Florbetazine for non-invasive detection of CA via preclinical assessments and preliminary clinical evaluation.
Methods: Specific binding and affinity of [18F]Florbetazine to amyloid light-chain (AL) and transthyretin (ATTR) deposits were assessed via in vitro autoradiography on human myocardial sections. Pharmacokinetics and biodistribution were characterized by dynamic micro-PET/CT imaging in healthy Sprague Dawley (SD) rats. Whole-body PET/CT imaging was performed in two healthy volunteers to estimate normal-organ background, and in a single patient with biopsy-proven AL amyloidosis to preliminarily explore diagnostic feasibility.
Results: Autoradiography confirmed specific binding of [18F]Florbetazine to both AL and ATTR deposits with high binding affinities (Kd = 20.85 nM and 54.10 nM, respectively). In rats, [18F]Florbetazine exhibited rapid myocardial and renal uptake followed by efficient clearance from normal tissues. In healthy volunteers, background myocardium and renal activity was minimal by 40 min post-injection. In the AL amyloidosis patient, delayed-phase PET/CT imaging (60-70 min) revealed intense myocardium and renal uptake,…
How strong is the evidence?
Evidence Hub reads this as a clinical trial, done in people. Its evidence level is 3 of 5 (Moderate · trial / cohort / secondary analysis). Trials without a large randomized design, cohorts and secondary analyses give moderate evidence.
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