Abstract:
The research and development of radiopharmaceuticals is very important for the early diagnosis and treatment of major diseases such as heart, brain, and tumors. In 2021, the Chinese government issued the 《Medium- and Long-Term Development Plan for Medical Isotopes (2021—2035)》, which has played a positive role in promoting the industrial development of radiopharmaceuticals in China. This paper mainly reviewed the latest progress in radiopharmaceutical research, and put forward suggestions on the problems encountered in the developments of radiopharmaceuticals and the future direction in China. In the section “latest progress in the radiopharmaceutical research”, we introduced the latest progress in the research of “radiopharmaceuticals related to cancer”, “radiopharmaceuticals related to central nervous system(CNS) diseases”, and “radiopharmaceuticals related to cardiovascular diseases”, with a special emphasis on the latest progress in the research of “radiopharmaceuticals related to cancer”. Among them, in the research progress of “radiopharmaceuticals related to cancer”, we introduced the latest progress from three perspectives, namely, “radiopharmaceuticals targeting popular targets such as prostate surface membrane antigen(PSMA) and fibroblast activation protein(FAP)”, “radiopharmaceuticals targeting new cancer-specific biomarkers”, and “dual-target radiopharmaceuticals”. In the research progress of “radiopharmaceuticals related to central nervous system(CNS) diseases”, we introduced radiopharmaceuticals targeting tau protein, Aβ plaques, α7-nicotinic acetylcholine receptor(α7-nAChR), synaptobrevin glycoprotein 2A(SV2A), α-synuclein(α-syn), dopamine D3 receptor(D3R), dopamine sigma-1 receptor, and transporter 18kDa(TSPO) receptor, and monoamine oxidase-B(MAO-B) receptor, respectively. In terms of the research progress of “radiopharmaceuticals related to cardiovascular diseases”, we introduced three aspects, namely radiopharmaceuticals targeting riboflavin transporter 3(RFVT3) encoded by SLC52A3, angiotensin converting enzyme 2(ACE2), and myocardial fatty acid metabolism imaging agents. Finally, we looked into the development trend of radiopharmaceuticals in China. In particularly, it was pointed out that we must pay attention to the role of emerging drug screening technologies such as artificial intelligence drug discovery(AIDD), computer-aided drug design(CADD), and DNA-encoded compound libraries(DEL) in the development of radiopharmaceuticals. And we also pointed out that we must strengthen basic research on new targets such as GRPR and NTSR-1 and new mechanisms such as radioactive hybridization, dual targets, and multi-targets, and pay attention to the combined use of radioactive drugs with other treatment or diagnostic methods such as PROTAC and fluorescent probes in major diseases such as tumors, as well as the synergistic effects and important significance cause by them. With this, the homogeneity problem of radiopharmaceutical development could be avoided from the root, and the radiopharmaceutical development can be accelerated.