Bench to Bedside Development of [¹⁸F]Fluoromethyl-(1,2-²H₄)choline ([¹⁸F]D4-FCH).

ABSTRACT: Malignant transformation is characterised by aberrant phospholipid metabolism of cancers, associated with the upregulation of choline kinase alpha (CHKα). Due to the metabolic instability of choline radiotracers and the increasing use of late-imaging protocols, we developed a more stable choline radiotracer, [¹⁸F]fluoromethyl-[1,2-²H₄]choline ([¹⁸F]D4-FCH). [¹⁸F]D4-FCH has improved protection against choline oxidase, the key choline catabolic enzyme, via a ¹H/²D isotope effect, together with fluorine substitution. Due to the promising mechanistic and safety profiles of [¹⁸F]D4-FCH in vitro and preclinically, the radiotracer has transitioned to clinical development. [¹⁸F]D4-FCH is a safe posit

SUBMITTER: Challapalli A 

PROVIDER: S-EPMC10745874 | biostudies-literature | 2023 Dec

REPOSITORIES: biostudies-literature