Improved Automated Radiosynthesis of [¹⁸F]Dolutegravir: Toward Clinical Applications.

ABSTRACT: Positron emission tomography imaging using radiolabeled dolutegravir (DTG) is an interesting approach to understand the biodistribution of this antiretroviral drug at HIV-1 sanctuary sites. In the course of clinical translation, we depict herein an improved and pharmaceutically compliant radiosynthesis of [¹⁸F]DTG from an original tin precursor. The radiosynthesis was achieved in two steps by copper-mediated radiofluorination, followed by enol ether deprotection using a kit-based AllInOne module. Ready-to-inject [¹⁸F]DTG was obtained in 20 ± 5% (n = 12) decay-corrected radiochemical yield within 90 min, representing a 4-fold increase compared to the previously published three-step radiosynthesis. Quality control was carried out with three consecutive [^18</

SUBMITTER: Huvelle S 

PROVIDER: S-EPMC11465247 | biostudies-literature | 2024 Oct

REPOSITORIES: biostudies-literature