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RDC Development for Prostate Cancer
In recent years, several radionuclide drug conjugates (RDCs) have demonstrated their strong therapeutic potential in the field of oncology. Especially in the field of prostate cancer, the integration of diagnosis and therapy has been realized. With extensive experience and professional team, Alfa Cytology is committed to providing one-stop radionuclide drug conjugate (RDC) development services.
Introduction to Radionuclide Drug Conjugates (RDCs)
Radionuclide Drug Conjugate (RDC) is a drug form designed and developed by coupling a precision targeting molecule ligand (monoclonal antibody, peptide or small molecule) and a potent killing factor (nuclide, Radioisotope) with a linker and chelator. It can highly concentrate the energy released by radionuclides within a few times the diameter of the cancer cells, thus minimizing damage to the surrounding normal tissues. A variety of targeted radionuclide therapies have been applied in the treatment of prostate cancer, revealing the great therapeutic potential in addition to RDC.
Fig.1 Chemical structures of the various targeted radionuclide therapeutic agents for metastatic castration-resistant prostate cancer. (Hébert, K., et al., 2024)
Structures to RDCs
Similar to ADCs, SMDCs, etc., RDCs are mainly composed of an antibody or small molecule (ligand) that mediates the targeting action, a linker, a chelator, and a radiation/imaging factor (radioisotope).
Linker
Since the nuclide does not necessarily need to break off during the drug's action, and does not need to be endocytosed into the cell in order to exert a radiation killing effect. Therefore, RDC drugs often use non-cleavable linkers, which can reduce the shedding of radionuclides in the blood circulation and off-target toxicity.
Radioisotope
Considering the physical properties and availability of radionuclides, chelation methods, imaging possibilities, as well as patient safety and oncology treatment objectives, most targeted radioligand therapy clinical development programs involve the use of beta-decay radionuclides.
Chelator
The starting group of RDC drug is radioactive metal nuclide, so compared with ADC, RDC has more chelating agent structure. According to the different valence states of the nuclide, different chelating agents need to be selected, and common chelating agents include DOTA, NOTA, etc.
Ligand
Targeting ligand acts as a precision localizer, guiding the radionuclide to the target. Ligands can be peptides, antibodies or small molecules, etc. Different types of ligands have different pharmacological profiles, and attention needs to be paid to the blood clearance of the drug, its plasma half-life, and its uptake in tumor and non-target tissues.
RDC Development for Prostate Cancer
| Name | Target | Payload | Company | Approval Date |
| TLX591-CDx | PSMA | 68Ga | Telix Pharmaceuticals | December 2021 |
| 68Ga-PSMA-11 | PSMA | 68Ga | Novartis | December 2020 |
| 177Lu-PSMA-617/Pluvicto | PSMA | 177Lu | Novartis | March 2022 |
Disclaimer: Alfa Cytology focuses on providing preclinical research service. This table is for information exchange purposes only. This table is not a treatment plan recommendation. For guidance on treatment options, please visit a regular hospital.
Our Services
At Alfa Cytology, our team of experts provides customized RDC drug development, including antibody radionuclide conjugate (ARC), peptide radionuclide conjugate (PRC), and small molecule radionuclide conjugate (SMRC), based on the individual needs of our clients. We also provide preclinical development services, including efficacy evaluation, DMPK/ADME and safety assessment.
- Antibody Radionuclide Conjugate (ARC)
- Peptide Radionuclide Conjugate (PRC)
- Small Molecule Radionuclide Conjugate (SMRC)
One-Stop Solutions for RDC Development
The biggest difference between RDC and other coupled drugs is the drug load. Different radionuclides can be used to perform different functions of visualization or treatment, and some even perform both; because radionuclides do not need to be in direct contact with the cell, the linker of the RDC does not need to be broken during the onset of action, and chelation of the radioactive element to the ligand requires the use of a Chelator. the following table shows the common radionuclides as well as the Chelator.
| Radionuclides | 225Ac, 111In, 177Lu, 90Y, 213Bi. |
| Chelator | DOTA, TETA, NOTA, DAPA, TRAP, HBED. |
At Alfa Cytology, we are committed to providing you with comprehensive radionuclide drug conjugate (RDC) development services to support your research and drug development needs. If you are interested in our services, please don't hesitate to contact us for further information and pricing details.
Reference
- Hébert, K., et al. New Drugs for Targeted Radionuclide Therapy in Metastatic Prostate Cancer. European urology focus. 2024, 10(4): 514-517.
For research use only.