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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 [ 18 F]canagliflozin was developed via a Cu-mediated 18 F-fluorination of its boronic ester precursor with a radiochemical yield of 2.0 ± 1.9% and a purity of &gt;95%. The GMP automated synthesis originated [ 18 F]canagliflozin with a yield of 0.5-3% ( n = 4) and a purity of &gt;95%. Autoradiography showed [ 18 F]canagliflozin binding in human kidney sections containing SGLT2. Since [ 18 F]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.

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

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