Radionuclide-Small Molecule Conjugation Service

Small molecule-based RDC (Radionuclide Drug Conjugate), a new type of drug for cancer treatment, has received a lot of attention. The conjugation of radionuclide-small molecule is a very professional process.

As a top CRO company, Rdcthera can provide a high-quality radionuclide-small molecule conjugation service for you.

Small Molecule Based RDC

The most widely developed small molecule-based RDC is the one targeting the PSMA (Prostate-Specific Membrane Antigen), a type-II transmembrane glycoprotein with several enzymatic functions overexpressed in prostate cancer. Prostate cancer is the second most prevalent type of cancer among men worldwide. The PSMA-directed radiopharmaceuticals are now used extensively for diagnostic imaging and treatment.

Fig.1 Chemical structure of two small molecule based RDC examples.
(Debnath, S., et al., 2022, International journal of molecular sciences)

Overview of Radionuclide-Small Molecule Conjugation

Conjugation is a chemical strategy to form a stable covalent link between two molecules/polymers or biomolecules/biopolymers together. With a connection between the targeting molecule and a cargo, effective targeted therapy for cancer becomes possible. A myriad of conjugated complexes for cancer treatment, including lung cancer, colorectal cancer, breast cancer, multiple myeloma, lymphoma, prostate cancer, and melanoma are newly discovered.

The chemical reaction condition for the conjugation process of small molecule and radionuclide-chelator complex is quite demanding and very sensitive to the temperature, pH, catalyst, and substrate concentration of the reaction. The most common chemical bonds in radionuclide-small molecule conjugation are the disulfide bond and amide bond by adding sulfhydryl or amine groups in a small molecule during synthesis.