Purpose <p>This first-in-human positron emission tomography (PET) study evaluates [<sup>18</sup>F]OXD-2314, a radiopharmaceutical designed for imaging tau in non-Alzheimer’s disease tauopathies.</p> Methods <p>Synthesis of [<sup>18</sup>F]OXD-2314 was automated using a commercial module and validated for human use. Dynamic PET imaging was performed in healthy control subjects (2 female, 2 male, ages 49–65 years). Kinetic modelling was performed from brain time-activity curves and radiometabolite-corrected arterial input functions to estimate total distribution volumes (<i>V</i><sub>T</sub>) in each region of interest.</p> Results <p>[<sup>18</sup>F]OXD-2314 met all release criteria for human use. PET imaging revealed an initial whole brain peak of 2.3 standardized uptake value, followed by a steady washout. Distribution of radioactivity was uniform among brain regions (<i>V</i><sub>T</sub> range: 2.21 ± 0.29 to 2.81 ± 0.43 mL/cm<sup>3</sup>).</p> Conclusions <p>[<sup>18</sup>F]OXD-2314 was successfully translated to first-in-human PET imaging. No adverse events were reported and PET imaging in patient populations of non-AD tauopathies is underway.</p>

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First-in-human PET neuroimaging of [18F]OXD-2314

  • Emily Murrell,
  • Lucas Narciso,
  • Kimberly L. Desmond,
  • Caitlin Chow,
  • Anton Lindberg,
  • Armando Garcia,
  • Chester A. Mathis,
  • Samuel Svensson,
  • Antonio P. Strafella,
  • Neil Vasdev

摘要

Purpose

This first-in-human positron emission tomography (PET) study evaluates [18F]OXD-2314, a radiopharmaceutical designed for imaging tau in non-Alzheimer’s disease tauopathies.

Methods

Synthesis of [18F]OXD-2314 was automated using a commercial module and validated for human use. Dynamic PET imaging was performed in healthy control subjects (2 female, 2 male, ages 49–65 years). Kinetic modelling was performed from brain time-activity curves and radiometabolite-corrected arterial input functions to estimate total distribution volumes (VT) in each region of interest.

Results

[18F]OXD-2314 met all release criteria for human use. PET imaging revealed an initial whole brain peak of 2.3 standardized uptake value, followed by a steady washout. Distribution of radioactivity was uniform among brain regions (VT range: 2.21 ± 0.29 to 2.81 ± 0.43 mL/cm3).

Conclusions

[18F]OXD-2314 was successfully translated to first-in-human PET imaging. No adverse events were reported and PET imaging in patient populations of non-AD tauopathies is underway.