A research team from Soochow University published an important study in the renowned pharmaceutical journal Molecular Pharmaceutics (IF 4.5), successfully developing a novel CD9-targeted theranostic radiopharmaceutical, DOTA-M-P. This study represents the first development of a radiopharmaceutical precursor targeting CD9 and further demonstrates the feasibility of CD9-targeted radionuclide therapy for glioma. The team used the Elite P3500 to prepare high-purity precursor compounds for subsequent radiolabeling, with ¹⁷⁷Lu-DOTA-M-P achieving a labeling efficiency of 99.0% and a radiochemical purity of 99.5%, while showing good stability in PBS and serum. In further in vivo therapeutic studies, the high-dose group achieved a tumor growth inhibition (TGI) rate of 69.3%, providing valuable experimental evidence for the potential of CD9-targeted radiopharmaceuticals in the precise diagnosis and treatment of glioma.
Figure. Therapeutic experiment of 177 Article Lu-DOTA-M-P in U87-CD9 tumor-bearing mice.
In the development of small‑molecule peptide drugs, the preparation of compounds with high purity is a prerequisite for subsequent radiolabeling and biological activity evaluation. In this study, the authors used an Elite EClassical P3500 semi‑preparative HPLC system (equipped with a UV3100 UV‑Vis detector and P3500 pump, coupled with a CST Daiso C18 preparative column, using methanol/water containing 0.1% trifluoroacetic acid as the mobile phase) to perform preparative‑scale purification of the synthesized precursors DOTA‑P and DOTA‑M‑P (see Supplementary Figure S7). With its stable gradient elution performance, precise flow rate control, and reliable UV detection, the Elite P3500 system successfully increased the purity of the target compounds to over 95%, meeting the stringent requirements for precursor purity in radionuclide (⁶⁸Ga, ¹⁷⁷Lu) labeling.
Figure. Quality control of radiolabeling compounds and pharmacokinetic analysis.
High-purity precursors are critical for ensuring efficient radiolabeling and reliable in vivo performance. With the high-purity compounds provided by the Elite P3500 system, the authors were able to successfully prepare ¹⁷⁷Lu-DOTA-M-P with a labeling yield exceeding 99% and a radiochemical purity greater than 99%. The Elite P3500 and Waters analytical HPLC system were further used in combination, supporting reliable data generation in subsequent cell uptake, SPECT/CT imaging, and radionuclide therapy experiments. These results ultimately confirmed the good CD9-targeting capability of the agent and demonstrated its potential for precise diagnosis and radionuclide therapy of CD9-Positive Glioma.
Further Reading -
“Preparative liquid chromatography is a purification tool widely used in laboratories and industrial production, with applications in pharmaceutical R&D, natural product extraction, biologics purification, and other fields. By efficiently separating target components from mixtures, it helps researchers obtain high-purity substances, providing reliable support for subsequent research and applications.“ - Learn more about the principles, classifications, and applications of Preparative LC.
Title: Development of a CD9‑Targeted Radiopharmaceutical for Imaging and Radionuclide Therapy in CD9‑Positive Glioma
Journal: Molecular Pharmaceutics, 2025, 22 (10), 6368-6380
