Radiometal-theranostics: the first 20 years

• Published in: Journal of radioanalytical and nuclear chemistry Vol. 332; no. 5; pp. 1557 - 1576
• Main Authors: Roesch, Frank, Martin, Marcel
• Format: Journal Article
• Language: English
• Published: Cham Springer International Publishing 01.05.2023; Springer; Springer Nature B.V
• Subjects: Chemistry; Chemistry and Materials Science; Diagnostic Radiology; Dosimeters; Hadrons; Heavy Ions; Inorganic Chemistry; Nuclear Chemistry; Nuclear Physics; Phosphonates; Physical Chemistry; Radiation; Radiation dosage; Radiochemical separation; Yttrium isotopes; Radiometals; Positron emission tomography (PET); Peptide receptor radionuclide therapy (PRRT); Radiotracers; Radionuclide therapy (RNT); Endoradiotherapy (ERT); Radiopharmaceuticals; Theranostics
• ISSN: 0236-5731; 1588-2780
• DOI: 10.1007/s10967-022-08624-3

This review describes the basic principles of radiometal-theranostics and its dawn based on the development of the positron-emitting 86 Y and 86 Y-labeled radiopharmaceuticals to quantify biodistribution and dosimetry of 90 Y-labeled analogue therapeutics. The nuclear and inorganic development of 86 Y (including nuclear and cross section data, irradiation, radiochemical separation and recovery) led to preclinical and clinical evaluation of 86 Y-labeled citrate and EDTMP complexes and yielded organ radiation doses in terms of mGy/MBq 90 Y. The approach was extended to [ 86/90 Y]Y-DOTA-TOC, yielding again yielded organ radiation doses in terms of mGy/MBq 90 Y. The review further discusses the consequences of this early development in terms of further radiometals that were used ( 68 Ga, 177 Lu etc.), more chelators that were developed, new biological targets that were addressed (SSTR, PSMA, FAP, etc.) and subsequent generations of radiometal-theranostics that resulted out of that.