Radiopharmaceuticals: New Drug Development Process and the Importance of Preclinical Research

¹Li Yu Chen, ¹Ya Ting Huang, ¹ Hsin Jou Kuo, ¹Fan-Chieh Meng, ¹Arsyangela Verena,¹Chi-Wei Chang

¹ Primo Biotechnology Co., Ltd , Taipei, Taiwan.

Background:

Radiopharmaceuticals combine radioactive isotopes with targeting molecules and are widely used in the diagnosis and treatment of cancer, heart disease, and neurological disorders. These drugs utilize targeted carriers (such as small molecules, peptides, or antibodies) linked with radioactive nuclides, enabling not only “visualized diagnosis” but also “localized/systemic therapy,” making them a core tool in nuclear medicine precision diagnostics and radiotheranostics. With innovations in molecular targeting technology, imaging equipment, and radioactive isotopes, the development of nuclear medicine radiopharmaceuticals is rapidly growing. It is projected that by 2025, the global market size for nuclear medicine radiopharmaceuticals will reach $11.77 billion and is expected to surpass $42.03 billion by 2032, with a compound annual growth rate (CAGR) of 19.9%.

Literature Review:

The development process of radiopharmaceuticals can generally be divided into four main stages: drug discovery, preclinical evaluation, clinical trials, and regulatory approval. Among these, preclinical studies are a critical step, aimed at establishing target specificity, biodistribution, pharmacokinetics, dosimetry, and assessing potential toxicity and safety. These evaluations typically involve in vitro cell assays, in vivo animal imaging, and stability analyses. Radiopharmaceuticals must undergo preclinical evaluation that addresses both pharmacological effects and radiological safety, as guided by the IAEA and Taiwan’s Ministry of Health and Welfare. In Taiwan, developers are required to assess the pharmacological activity, pharmacokinetics, and toxicity of the non-radioactive component. Depending on the intended use, simplified toxicology strategies may be applied, especially for diagnostic agents that qualify as microdosing. For therapeutic radiopharmaceuticals, additional dosimetry studies and target organ risk assessments are required. In summary, preclinical studies are essential for confirming drug feasibility, ensuring safety, and supporting regulatory approval.