Whetter Jennifer N, Vaughn Brett A, Koller Angus J, Boros Eszter
Department of Chemistry, Stony Brook University, 100 Nicolls Road, Stony Brook, New York, 11794, USA.
Angew Chem Int Ed Engl. 2022 Feb 7;61(7):e202114203. doi: 10.1002/anie.202114203. Epub 2021 Dec 27.
Fluorine-18 remains the most widely clinically utilized radionuclide globally for positron emission tomography (PET). The emergence of therapeutic isotopes for the management of disease has produced a pronounced interest in matched, theranostic isotope pairs that can be employed in tandem for the diagnosis and stratification of patients for subsequent radiotherapy. F, however, does not have a suitable therapeutic isotopologue. Here, we demonstrate that the formation of [ F][Sc-F] ternary complexes is feasible under mild, aqueous conditions, producing chemically robust radiopharmaceuticals in high radiochemical yield and specific activity. A corresponding in vivo study with a cancer-targeting [ F][Sc-F] tracer indicates excellent in vivo stability and produces exquisite PET image quality, rendering the F/ Sc isotope pair an unusual, yet chemically matched theranostic pair with excellent potential for clinical translation.
氟-18仍然是全球临床上用于正电子发射断层扫描(PET)的最广泛使用的放射性核素。用于疾病治疗的治疗性同位素的出现引发了人们对匹配的诊疗同位素对的浓厚兴趣,这些同位素对可串联用于患者的诊断和分层,以便后续进行放射治疗。然而,氟没有合适的治疗性同位素类似物。在此,我们证明了在温和的水性条件下形成[氟-18][钪-氟]三元络合物是可行的,能以高放射化学产率和比活度生产出化学性质稳定的放射性药物。一项针对靶向癌症的[氟-18][钪-氟]示踪剂的相应体内研究表明其在体内具有出色的稳定性,并产生了精美的PET图像质量,使氟/钪同位素对成为一对不同寻常但化学性质匹配的诊疗对,具有出色的临床转化潜力。