¹⁷⁷Lu-Radiolabeling Service

¹⁷⁷Lu-radiolabeling involves the lutetium-177 incorporation into biomolecules, focusing on therapeutic purposes and SPECT imaging due to its β emissions. Alfa Cytology is capable with the expertise and well-equipped to deliver high-quality ¹⁷⁷Lu radiolabeling services and ensuring accurate and effective labeling for successful preclinical application of targeted cancer therapy.

Introduction to ¹⁷⁷Lu Isotopes

Lutetium-177 (¹⁷⁷Lu) is a radionuclide that is produced in a reactor and has become the foremost isotope in targeted radionuclide therapy. It possesses ideal characteristics, which include the emission of medium-energy beta particles and low-energy gamma photons. The former allows for efficient local tumor therapy while the latter facilitates post-therapy SPECT imaging. The unique "theranostic" feature and a half-life of 6.7 days, which is perfectly matched with the pharmacokinetics of peptides and antibodies, and also its strong chelation chemistry are the reasons why ¹⁷⁷Lu is regarded as the best and most dependable option in the development of new therapies for cancer.

Overview of ¹⁷⁷Lu-Labeling for Radiopharmaceuticals

¹⁷⁷Lu-radiolabeling utilizes lutetium-177, a β emitter, to label biomolecules such as peptides, antibodies, and small molecules for targeted therapeutic applications. This one is mostly utilized in specific radionuclide therapy for its unique ability to target and treat neoplasms with great precision and little collateral damage to surrounding tissue. The incorporation of ¹⁷⁷Lu is employed in SPECT imaging as well to track the distribution and assess the response to therapy in preclinical models.

Fig 1. Chemical structure of [177Lu] Lu-PSMA-617. (HENNRICH U, et al., 2022)

¹⁷⁷Lu Radiopharmaceutical

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.

Advantages of ¹⁷⁷Lu -Labeling

Among radiopharmaceuticals being developed today, lutetium-177 stands out for its prized its almost unique combination of physical and chemical characteristics. With a superb balance of therapeutic effect and in vivo imaging, the lutetium-177 radionuclide serves as a vital component in developing the next generation of targeted theranostic agents.

Our Services

The preclinical research and the development of ¹⁷⁷Lu-radiolabeling solution and ¹⁷⁷Lu-based therapies are a key area of focus for our company, and we have extensive research capabilities. Alfa Cytology is committed to the development of novel approaches to targeted cancer therapies, and because of the development of a sophisticated technology platform, our company aims to facilitate the rapid and accurate development of ¹⁷⁷Lu-based therapeutics.

Small-Molecule Radionuclide Conjugate (SMRC)

Antibody-Radionuclide Conjugate (ARC)

Peptide-Radionuclide Conjugate (PRC)

siRNA-Radionuclide Conjugate

Radiolabeling Small Molecule with ¹⁷⁷Lu for SPECT Imaging

¹⁷⁷Lu Custom Radiosynthesis

To optimize the radiochemical yield while maintaining radiochemical integrity and minimizing variances on each batch, we take careful measures in the planning so that every project moves smoothly on the transition from the designing phase to application.

• Design Labeling Position: For every small molecule and its complexed chelator (e.g., DOTA), we analyze and assist in defining the labeling on each target. After which, a step-wise protocol is generated that adjusts each parameter designed specifically to achieve ¹⁷⁷Lu incorporation while retaining the bioactivity.
• Precursor Preparation: A specific amount of non-radioactive, chelator-functionalized small molecule is dissolved in a reaction buffer made according to a specific formulation. The high-purity buffer is designed in such a way that its pH and composition maximize chelation and minimize degradation of the precursor.
• Custom Radiosynthesis: Custom radiosynthesis is performed under carefully monitored and shielded circumstances. This procedure is accomplished by seasoned radiochemists who guarantee the repeatable generation of a high-activity ¹⁷⁷Lu-labeled product for your use.

Purification & Quality Control

Once the labeling of the compound has taken place, verification is performed for successful incorporation of ¹⁷⁷Lu. Correct isotopic labeling, purity, and compound stability are proven by analytical standards, such as liquid chromatography (LC), mass spectrometry (MS), and scintillation counting, so that the standards for biological study are satisfied.

In Vitro Evaluation

In vitro tests are performed to evaluate the biological properties of the ¹⁷⁷Lu-labeled radiopharmaceutical. This includes studying its interaction with target receptors, cellular uptake, metabolic stability, and other pharmacological properties.

In Vivo Evaluation

The last step is in vivo evaluation of distribution, metabolism, pharmacokinetics, and the overall behavior of the radiolabeled molecule in a living organism. This is done by using imaging and radiometric evaluation of the distribution of ¹⁷⁷Lu-labeled compound in various tissues, which helps derive data related to therapy, safety, and targeting of other tissues.

Applications of ¹⁷⁷Lu-Radiolabeling

As the premier radionuclide for modern radioligand therapy, the applications of ¹⁷⁷Lu-radiolabeling are overwhelmingly focused on creating powerful theranostic agents that can simultaneously treat and image metastatic cancers.

Alfa Cytology provides several development options for ¹⁷⁷Lu radiolabeling, which correspond to specific therapeutic applications. If you face difficulty with any part of your project, our team is on standby, ready to assist you to ensure project completion. Reach out to discuss your quest so as to enable us to provide you with the best solution for your research.

Reference

1. HENNRICH U, EDER M. [(¹⁷⁷)Lu]Lu-PSMA-617 (Pluvicto(TM)): The First FDA-Approved Radiotherapeutical for Treatment of Prostate Cancer [J]. Pharmaceuticals (Basel, Switzerland), 2022, 15(10).

For research use only. Not intended for any clinical use.