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90Y-Radiolabeling Service

The ability to arm targeting molecules with beta-emitter, Yttrium-90, creates potent, purely therapeutic agents that are ideal for bigger tumors due to the powerful long-range crossfire effect. Alfa Cytology has the specialized radiochemistry expertise and infrastructure and the ability to stably conjugate Yttrium-90 to multiple targeting vectors to provide high-purity, therapeutic-grade radiopharmaceuticals for impactful preclinical research.

Introduction to 90Y Isotopes

Yttrium-90 (90Y) is a high-energy, pure beta-emitting radionuclide that serves as a powerful workhorse for targeted radionuclide therapy. 90Y delivers a potent, cytotoxic dose via beta particles with a half-life of 64.1 hours. The beta particles have a long range of several millimeters, and thus, the 90Y is able to reach and treat larger and solid tumors. Its marked crossfire effect allows it to kill adjacent, non-targeted cancer cells. 90Y is primarily therapeutic as it possesses no useful gamma emission for imaging, and is most prominently employed in the radioembolization of liver malignancies and radioimmunotherapy.

90Y-Labeling for Radiopharmaceuticals

Therapeutics based on the yttrium-90 isotope, with the name 90Y radiopharmaceuticals, are primarily used for applying targeted therapy for certain kinds of malignancies. 90Y emits energetic beta particles and has a half-life of nearly 2.67 days, providing ideal therapeutic doses in vivo. Precisely targeting cancer markers for tumor-specific therapy is possible through the 90Y radiolabeling of appropriate antibodies, ligands, or other carriers. Probably the greatest benefit of this approach is the protection of normal tissue with a concomitant increase of radiative energy concentration in cancer cells.

Yttrium-90 ibritumomab tiuxetan.Fig. 1 Yttrium-90 ibritumomab tiuxetan. (ALHAJ MOUSTAFA M, et al., 2023)

90Y Radiopharmaceutical

Name Company Application Phase
Zevalin® Acrotech Biopharma LLC - Approved FDA
Hematology CD66 Telix Pharmaceuticals -

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.

Key Features of 90Y Radiopharmaceuticals

  • Beta-Particle Radiation: The emission of high-energy β particles from 90Y effectively exterminates cancer cells within range (1-2 mm) for localized tumor therapy.
  • Optimal Half-Life: Its 2.67-day half-life ensures effective radiation delivery while minimizing long-term effects on nearby healthy tissues.
  • Precise Targeting: The ability of 90Y to bind with targeting molecules like antibodies enables precise tumor targeting, improving therapy effect while protecting healthy tissues.
  • Reduced Radiation Hazard: Without significant gamma radiation, 90Y reduces radiation exposure to the surrounding environment during therapy.

Our Services

Alfa Cytology is focused on creating cutting-edge 90Y radiopharmaceuticals and intends to construct precision oncology therapeutics using targeted molecular technology together with radioisotope yttrium-90. Our 90Y radiopharmaceutical development service, which encompasses the entire range from drug design and synthesis to preclinical evaluation and ensures the therapeutic agents are both effective and safe.

Custom 90Y Conjugation Service

90Y conjugation leverages advanced chelation chemistry to arm novel targeting vectors with Yttrium-90, creating potent radiotherapeutics designed to eradicate large or poorly vascularized tumors through a powerful crossfire effect.

Workflow for Developing 90Y-Radiolabeled Antibody Conjugates

90Y Custom Antibody Labeling

  • Strategy & Reagent Selection: We begin with a cooperative consultation to outline essential elements like targeted specific activity and the intended final use. Then, we identify the best antibody and a bifunctional chelator (e.g., DOTA) to complex 90Y without losing immunoreactivity.
  • Antibody Conjugation & Characterization: The specific chelator is attached to the antibody through established chemistry that focuses on particular amino acids. After this step, the conjugate is thoroughly characterized and validated to ensure an appropriate chelator-to-antibody ratio (CAR) and structural integrity.
  • Protocol Optimization: For your particular conjugate, we ensure the highest possible radiochemical yield and reproducibility by optimizing essential factors, including pH, temperature, incubation time, and the antigen-to-antibody ratio.
  • Custom Radiosynthesis: Purified conjugates are radiolabeled to high standards with [90Y] Yttrium chloride in a controlled environment. A specialized radiochemistry team takes care of the 90Y-labeling synthesis.

Purification & Quality Control

Verification of the successful incorporation of 90Y is necessary after the labeling is done. It is done through a variety of checks; liquid chromatography (LC), mass spectrometry (MS), and scintillation counting are all analytical methods. These all help to quantify the labeling and check the correct isotopic labeling, purity, and composition of the compound to ensure it is fit for biological studies.

  • Stability Study Services
    Our dedicated team conducts an in-vitro stability assessment of the final product to confirm that the 90Y-antibody conjugate remains stable throughout its appropriate shelf-life and intended applications.
  • Radiochemical Purity Evaluation Services
    To ascertain the proportion of 90Y integrated into the antibody as opposed to the free radiocontaminants, we use advanced analytical techniques, including radio-iTLC and radio-HPLC.
  • Other Services
    To provide a comprehensive product profile, we perform other analyses that include the lipophilicity study and the immunoreactivity assay, which determine the conjugate binding affinity and functional specificity.

In Vitro Evaluation

In vitro tests are performed to evaluate the biological properties of the 90Y-labeled radiopharmaceutical. This includes studying its interaction with target receptors, cellular uptake, metabolic stability, and other pharmacological properties.

In Vivo Evaluation

The last part encompasses testing within an organism to examine pharmacokinetics and biodistribution while monitoring the compound's behavior as a whole. Imaging and radiometric techniques enable tracking of the tissue distribution of the 90Y-labeled compound to gain an understanding of its therapeutic potential and safety profile, and tissue targeting.

Applications of 90Y-Radiolabeling

The applications of 90Y-radiolabeling are centered on the development of potent radiotherapeutics. Yttrium-90's high-energy beta particles are suitable for the radiotherapeutic therapy of large, solid, or poorly vascularized tumor burdens through the powerful crossfire effect.

Systemic Targeted Radionuclide Therapy

  • Radioimmunotherapy (RIT) with Labeled Monoclonal Antibodies
  • Peptide Receptor Radionuclide Therapy (PRRT)
  • Small Molecule-Based Radioligand Therapy
  • Development of Radioconjugates with a Beta-Emitting Payload
  • Targeting of Cell Surface Antigens (e.g., CD20, PSMA)
  • High-Dose Consolidation Therapy
  • More

Preclinical Research & Development

  • In Vivo Efficacy and Proof-of-Concept Studies
  • Dose-Response and Therapeutic Window Determination
  • Biodistribution and Pharmacokinetic (PK) Modeling
  • Development of Novel Chelators and Conjugation Chemistries
  • Comparative Efficacy Studies vs. Other Radionuclides
  • Radiobiology and Crossfire Effect Modeling
  • More

Dedicated to pioneering cancer therapeutics through advances in medical technology, Alfa Cytology is a top specialist in the development of 90Y radiopharmaceuticals. Enhanced precision oncology therapeutics are incorporated in our range of innovative services, from designing a targeted molecule to conducting detailed preclinical studies. If you would like to learn more about our advanced 90Y radiopharmaceutical development services, do not hesitate to contact us directly.

Reference

  1. ALHAJ MOUSTAFA M, BORAH B J, MORIARTY J P, et al. Yttrium-90 Ibritumomab Tiuxetan is Cost-Effective Compared to Bendamustine + Rituximab in Low-grade Lymphomas [J]. Clinical lymphoma, myeloma & leukemia, 2023, 23(4): 259-65.

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

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