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.
