2. Academic Validation
  3. Development of [18F]AldoView as the First Highly Selective Aldosterone Synthase PET Tracer for Imaging of Primary Hyperaldosteronism

Development of [18F]AldoView as the First Highly Selective Aldosterone Synthase PET Tracer for Imaging of Primary Hyperaldosteronism

  • J Med Chem. 2021 Jul 8;64(13):9321-9329. doi: 10.1021/acs.jmedchem.1c00539.
Kerstin Sander 1,  Thibault Gendron 1,  Klaudia A Cybulska 1,  Fatih Sirindil 1,  Junhua Zhou 2,  Tammy L Kalber 3,  Mark F Lythgoe 3,  Tom R Kurzawinski 4,  Morris J Brown 2,  Bryan Williams 4 5,  Erik Årstad 1
Affiliations

Affiliations

  • 1 Centre for Radiopharmaceutical Chemistry, University College London, 5 Gower Place, London WC1E 6BS, U.K.
  • 2 William Harvey Research Institute, Barts & The London School of Medicine & Dentistry, Queen Mary University of London, Charterhouse Square, London EC1M 6BQ, U.K.
  • 3 Centre for Advanced Biomedical Imaging, University College London, 72 Huntley Street, London WC1E 6DD, U.K.
  • 4 NIHR University College London Hospitals Biomedical Research Centre, 149 Tottenham Court Road, London W1T 7DN, U.K.
  • 5 Institute of Cardiovascular Sciences, University College London, Gower Street, London WC1E 6BT, U.K.
PMID: 34137616 DOI: 10.1021/acs.jmedchem.1c00539
Abstract

The purpose of this study was to synthesize a fluorine-18 labeled, highly selective aldosterone synthase (hCYP11B2) inhibitor, [18F]AldoView, and to assess its potential for the detection of aldosterone-producing adenomas (APAs) with positron emission tomography in patients with primary hyperaldosteronism (PHA). Using dibenzothiophene sulfonium salt chemistry, [18F]AldoView was obtained in high radiochemical yield in one step from [18F]fluoride. In mice, the tracer showed a favorable pharmacokinetic profile, including rapid distribution and clearance. Imaging in the adrenal tissue from patients with PHA revealed diffuse binding patterns in the adrenal cortex, avid binding in some adenomas, and "hot spots" consistent with aldosterone-producing cell clusters. The binding pattern was in good visual agreement with the antibody staining of hCYP11B2 and distinguished areas with normal and excessive hCYP11B2 expression. Taken together, [18F]AldoView is a promising tracer for the detection of APAs in patients with PHA.

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