GMP Compliant Synthesis of [18F]Canagliflozin, a Novel PET Tracer for the Sodium-Glucose Cotransporter 2

Sjoukje van der Hoek, Inês F Antunes, Khaled A Attia, Olivier Jacquet, Andre Heeres, Marian Bulthuis, Rolf Zijlma, Hendrikus H Boersma, Harry van Goor, Ton J Visser, Hiddo J L Heerspink, Philip H Elsinga, Jasper Stevens*

*Corresponding author for this work

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Inhibition of the sodium-glucose cotransporter 2 (SGLT2) by canagliflozin in type 2 diabetes mellitus results in large between-patient variability in clinical response. To better understand this variability, the positron emission tomography (PET) tracer [18F]canagliflozin was developed via a Cu-mediated 18F-fluorination of its boronic ester precursor with a radiochemical yield of 2.0 ± 1.9% and a purity of >95%. The GMP automated synthesis originated [18F]canagliflozin with a yield of 0.5-3% (n = 4) and a purity of >95%. Autoradiography showed [18F]canagliflozin binding in human kidney sections containing SGLT2. Since [18F]canagliflozin is the isotopologue of the extensively characterized drug canagliflozin and thus shares its toxicological and pharmacological characteristics, it enables its immediate use in patients.

Original languageEnglish
Pages (from-to)16641-16649
Number of pages9
JournalJournal of Medicinal Chemistry
Issue number22
Early online date8-Nov-2021
Publication statusPublished - 25-Nov-2021

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