Development of [18F]AldoView as the First Highly Selective Aldosterone Synthase PET Tracer for Imaging of Primary Hyperaldosteronism
K Sander, T Gendron, KA Cybulska… - Journal of medicinal …, 2021 - ACS Publications
The purpose of this study was to synthesize a fluorine-18 labeled, highly selective
aldosterone synthase (h CYP11B2) 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 …
aldosterone synthase (h CYP11B2) 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 …
Development of [18F] AldoView as the first highly selective aldosterone synthase PET tracer for imaging of patients with Primary Hyperaldosteronism.
K Sander, T Gendron, KA Cybulska… - Endocrine …, 2021 - endocrine-abstracts.org
Background: Inappropriately high aldosterone in patients with primary hyperaldosteronism
(PHA) is due to increased aldosterone synthase (CYP11B2) activity. Selective in vivo
imaging of overexpressed CYP11B2 in adrenals with positron emission tomography (PET)
has not yet been achieved due to close homology of enzymes involved in aldosterone and
cortisol (CYP11B1) synthesis. Aim: Synthesize a fluorine-18 labelled highly selective
CYP11B2 inhibitor,[18F] AldoView, and assess its potential for the detection of aldosterone …
(PHA) is due to increased aldosterone synthase (CYP11B2) activity. Selective in vivo
imaging of overexpressed CYP11B2 in adrenals with positron emission tomography (PET)
has not yet been achieved due to close homology of enzymes involved in aldosterone and
cortisol (CYP11B1) synthesis. Aim: Synthesize a fluorine-18 labelled highly selective
CYP11B2 inhibitor,[18F] AldoView, and assess its potential for the detection of aldosterone …
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