Isotopic Radiolabeling of the Antiretroviral Drug [¹⁸F]Dolutegravir for Pharmacokinetic PET Imaging.

ABSTRACT: Deciphering the drug/virus/host interactions at infected cell reservoirs is a key leading to HIV-1 remission for which positron emission tomography (PET) imaging using radiolabeled antiretroviral (ARV) drugs is a powerful asset. Dolutegravir (DTG) is one of the preferred therapeutic options to treat HIV and can be isotopically labeled with fluorine-18. [18F]DTG was synthesized via a three-step approach of radiofluorination/nitrile reduction/peptide coupling with optimization for each step. Radiofluorination was performed on 2-fluoro-4-nitrobenzonitrile in 90% conversion followed by nitrile reduction using sodium borohydride and aqueous nickel(II) chloride with 72% conversion. Final peptide coupling reaction followed by HPLC purification and formulation afforded ready-to-inject [18F]DTG in

SUBMITTER: Tisseraud M 

PROVIDER: S-EPMC9143889 | biostudies-literature | 2022 May

REPOSITORIES: biostudies-literature