[18F]알루미늄 플루오라이드 표지 방사성의약품: 18F, 68Ga 제제 한계를 극복하기 위한실용적인 대안

Abstract

Fluorine-18 (18F) is a radioisotope commonly used in positron emission tomography (PET), characterizedby a long half-life (109.7 minutes) and high resolution. However, traditional 18F-labeling requires harsh conditions,such as anhydrous, high-temperature, multi-step synthesis, which results in a low radiochemical yield (RCY) and isunsuitable for heat-sensitive biomolecules. To address these challenges, metal chelation-based [18F]AlF labeling wasintroduced. [18F]AlF chelation can provide a higher RCY compared to direct 18F-labeling, as [18F]AlF2+ is formed inaqueous solutions through a relatively short-step synthesis. Although formation is restricted to pH 4-5, it is a morepractical and efficient alternative to conventional direct 18F-labeling methods. Furthermore, [18F]AlF is prepared undermild, aqueous conditions, enabling chelation to biomaterials. It has also been formed into stable complexes, whichmay offer advantages in overcoming the production restrictions of 68Ga, which has a short half-life (68 minutes). [18F]AlF-labeled radiopharmaceuticals have also shown potential as a next-generation diagnostic agent by detectingmicro-lesions on PET/CT imaging that are missed by 68Ga radiopharmaceuticals. In this review, we have explainedpreclinical PET/CT imaging and biodistribution studies of [18F]AlF-labeled radiopharmaceuticals that would replaceconventional 18F and 68Ga-labeled agents. Furthermore, we evaluated the feasibility of clinical translation for thesepreclinical [18F]AlF-labeled radiopharmaceuticals.