This 64Cu-labeling service gives theranostic agents for PET imaging and targeted radionuclide therapy due to the isotope's ideal 12.7-hour half-life and versatile chelation chemistry used in preclinical assessments of a wide range of molecules. Deep knowledge in coordination chemistry and modern facilities enables Alfa Cytology to provide high-purity, custom-conjugated 64Cu-radiopharmaceuticals to sophisticated research applications.
As a highly versatile cyclotron-produced radioisotope, copper-64 (64Cu) is used in radiopharmaceuticals, demonstrates a "theranostic" approach, and has a unique versatility. Its half-life is 12.7 hours and has a unique dual decay mode, which allows for the emission of positron (β+) particles for PET imaging or beta-minus (β-) particles for targeted radionuclide therapy. This means that a single compound labelled with 64Cu radioisotope is capable of both therapeutic and diagnostic functionalities. Its favorable half-life is particularly well-matched to the pharmacokinetics of peptides and antibody fragments, making it a premier choice for developing next-generation image-and-treat agents.
The uniqueness of copper-64 (64Cu) has made it one of the most commercially viable candidates for the development of radionuclide-based radiopharmaceuticals. As a result of the emission of two different ray types and a reasonably convenient half-life of approximately 12.7 hours, high-resolution PET imaging and therapeutic applications can be addressed simultaneously. The combination of the two makes 64Cu uniquely positioned as a theranostic agent. It's well-established coordination chemistry makes possible the use of robust chelators for stable attachment to peptides and antibodies, leading to broad applications in preclinical investigations.
Fig 1. Schematic of a 64Cu-labeled molecule interacting with a target cell.
| Name | Company | Application | Phase |
|---|---|---|---|
| LNTH-1363S | Lantheus | Tumor / Fibrosis assessment | |
| 64Cu-SAR-bisPSMA | Clarity Pharmaceuticals | Prostate Cancer |
Disclaimer: Alfa Cytology focuses on providing preclinical research services. 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.
Theranostic Potential in a Single Isotope
For PET imaging, 64Cu decays by way of positron emission, whilst for therapeutic purposes, it decays by emission of a beta minus particle. Having both types of decay gives 64Cu the distinct ability to use the same compound radiopharmaceutical for both diagnosis and therapy, thus exemplifying the theranostic concept.
Ideal Half-Life for Intermediate Pharmacokinetics
Its 12.7-hour half-life is perfectly suited for labeling peptides, antibody fragments, and larger small molecules. This timeframe is long enough for the agent to circulate, accumulate optimally at the target, and clear from the background (e.g., enabling 24-hour imaging), without the prolonged radiation exposure associated with longer-lived isotopes.
High-Resolution PET Imaging
The emitted positron from 64Cu is of low average energy, which leads to short travel distances in tissue. The physical property translates into sharper and higher resolution positron emission tomography (PET) images. This enables more precise localization and quantification of targets.
Versatile Coordination Chemistry
The coordination chemistry for copper is well-developed, with a variety of robust chelators available (e.g., DOTA or cage-like Sarcophagine derivatives). This ensures 64Cu remains stably bound to the targeting molecule in vivo, preventing radionuclide detachment and leading to reliable biodistribution data.
Alfa Cytology possesses great knowledge in radiometal coordination chemistry, which allows for the custom conjugation of 64Cu to a diverse range of targeting vectors, including small molecules and complex biologics. Through rigorous process optimization and quality control, our 64Cu labeled compounds are of the highest purity and specific activity to ensure the best and reliable preclinical data generation.
The specialized service on conjugation of 64Cu has to do with the stable attachment of copper-64 to various client-provided molecules such as peptides, antibodies, and other complex biologics. This process transforms the compound into a powerful and novel theranostic agent, thereby allowing high-resolution PET imaging in order to accurately assess the in vivo biodistribution and therapeutic potential of a compound on various research models.
The mixture resulting from radiolabeling is purified using SEC or HPLC to obtain monomeric 64Cu-antibody and get rid of impurities such as unbound 64Cu and aggregates. After 64Cu labeling, all compounds are checked to indicate successful labeling. For each compound, analytical methods such as LC-MS followed by scintillation counting are used to demonstrate that the isotopic labeling was performed accurately and the compound is pure and stable.
In vitro tests are performed to evaluate the biological properties of the 64Cu-labeled radiopharmaceutical. This includes studying its interaction with target receptors, cellular uptake, metabolic stability, and other pharmacological properties.
This critical phase first involves quantitative biodistribution and pharmacokinetic (PK) studies to meticulously measure the agent's uptake in various organs and its clearance rate from the body. Subsequently, PET imaging is performed in relevant disease models to visually confirm specific target engagement and to definitively validate the agent's diagnostic potential through in vivo blocking experiments.
Leveraging its unique theranostic decay properties for both PET imaging and therapy, coupled with a versatile 12.7-hour half-life ideal for tracking biologics, 64Cu-radiolabeling is broadly applied in preclinical research to evaluate the pharmacokinetics, target engagement, and therapeutic efficacy of next-generation radiopharmaceuticals.
Theranostic Agent Development
Biologic and Nanoparticle Development
We offer services that range from molecular design to preclinical testing, such that every stage of development is seamlessly integrated, ensuring efficiency, accuracy, and compliance with regulatory standards.
Experience in 64Cu Chemistry
Full-Service Development
State-of-the-Art Facilities
Application-Specific Tailored Solutions
Alfa Cytology's scientific team has mastered the intricate coordination chemistry of 64Cu, enabling us to consistently deliver high-purity, custom-labeled theranostic agents for a wide array of research applications. If you are interested in obtaining professional assistance in the enhancement of your program or in the solution of a particular problem you have, we encourage you to contact us to find out what we can offer.
For research use only. Not intended for any clinical use.
Alfa Cytology, a provider of RDC preclinical services, specializes in RDC design, conjugation, and analysis. Supported by a rich library of radionuclides, chelators, and linkers, we excel in targeting molecule design. We offer customized RDC services tailored to diverse requirements-your demand is our mission.
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