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89Zr-Radiolabeling Service

89Zr-radiolabeling represents a cutting-edge technology in molecular imaging, enabling the non-invasive visualization and quantification of biological processes in vivo via positron emission tomography (PET). Alfa Cytology is a dedicated provider of premium 89Zr-radiolabeling services, offering end-to-end solutions for the development and production of 89Zr-labeled conjugates, primarily antibodies and other targeting molecules.

Introduction to 89Zr Isotopes

Zirconium-89 (89Zr) is a positron-emitting radionuclide with exceptional properties for immuno-PET applications. Its primary appeal lies in its favorable physical properties: a half-life of 78.4 hours (approximately 3.25 days) is exceptionally well-matched to the biological half-lives of monoclonal antibodies and other large biomolecules, allowing for optimal tumor targeting and imaging over several days. The relatively low energy of the emitted positrons (395.5 keV) contributes to high image resolution.

89Zr-Labeling for PET Imaging

With a half-life of 78.4 hours and a low positron energy of 395.5 keV, 89Zr has ideal physical properties for antibody-based imaging. 89Zr labeling involves the conjugation of the radionuclide to a targeting vector, such as an antibody, using a bifunctional chelator. The stable complex allows the radiotracer to preferentially and efficiently accumulate at the target site (for example, a tumor with a specific antigen). The quantitative, real-time data obtained through subsequent PET imaging on biodistribution, target engagement, and pharmacokinetics is invaluable in the selection of doses and monitoring the therapy in trials.

Representative MIPs of [89Zr]ZrDFO-CR011 uptake in TNBC models.Fig 1. [89Zr]ZrDFO-CR011 uptake in TNBC models. (Lee, S., et al., 2022)

89Zr Radiopharmaceutical

Name Company Application Phase
89Zr-Df-IAB2M ImaginAb, Inc. CD8 ImmunoPET Imaging Phase II
89Zr-DFO-crefmirlimab ImaginAb, Inc. CD8 ImmunoPET Imaging Phase I
89Zr-DFO-girentuximab Telix Pharmaceuticals Diagnosis of Clear Cell Renal Cell Carcinoma Phase III
89Zr-ss-pertuzumab Genentech Imaging and Pharmacokinetic Studies in HER2-positive Breast Cancer Phase I
89Zr-DFO-REGN5054 Regeneron CD8 ImmunoPET Imaging Phase I

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 89Zr Labeling

Ideal Half-Life

The 78.4-hour physical half-life of 89Zr is ideally matched with the long circulation times of mAbs, allowing for imaging over several days when the target-to-background ratio is optimal.

Superior Image Quality

The favorable positron energy of 89Zr results in high-resolution PET images, providing precise anatomical localization and quantitative data on target density.

Robust Chemistry

The chelation chemistry between 89Zr and DFO is well-established, reliable, and produces stable complexes in vivo, minimizing off-target radiation exposure from free zirconium.

Quantitative Biodistribution Data

Enables precise, non-invasive measurement of tracer uptake in target tissues and clearance organs over time, critical for pharmacokinetic modeling.

Our Services

Alfa Cytology provides a comprehensive 89Zr-radiolabeling service designed to meet the rigorous standards of preclinical research. Our service encompasses everything from initial consultation and chelator conjugation to the final delivery of purified, quality-controlled 89Zr-labeled conjugates, and extends into a full suite of in vitro / in vivo evaluation and subsequent application research. This integrated approach from synthesis to functional validation provides a robust solution to accelerate your drug development and imaging agent validation.

Custom 89Zr Conjugation Service

Alfa Cytology offers a flexible custom 89Zr conjugation service, where we collaborate closely with you to develop and optimize a radiolabeling strategy for novel targeting molecules, including antibody fragments, peptides, and other biologics, ensuring the high specific activity and retained bioactivity for your unique application.

Workflow for Developing 89Zr-Radiolabeled Antibody Conjugates

89Zr Custom Radiosynthesis

  • Design Strategy: Involving a comprehensive assessment of the antibody's characteristics and the intended biological target to define the optimal conjugation and labeling approach.
  • Precursor Preparation: The bifunctional chelator (typically DFO-isothiocyanate or DFO-NCS) is covalently attached to the antibody via established bioconjugation chemistry, ensuring minimal impact on immunoreactivity.
  • Custom Radiosynthesis: Aimed at maximizing radiochemical yield and labeling efficiency, the 89Zr radiolabeling is performed under precisely controlled conditions of pH, buffer, temperature, and time by a dedicated radiochemistry team.

Purification & Quality Control

Following synthesis, the crude product undergoes rigorous purification to remove unincorporated 89Zr and other impurities, typically via size-exclusion chromatography or others. A comprehensive suite of quality control assays is then employed to confirm critical parameters, including radiochemical purity, pH, endotoxin levels, and sterility, ensuring the final product meets all predefined specifications for research use.

  • Stability Study Services
    Stability is assessed under defined conditions, including in vitro stability in buffer and serum to monitor for decomposition, ensuring conjugate integrity throughout the experimental timeline.
  • Radiochemical Purity Evaluation
    Radiochemical purity is determined using validated analytical methods such as iTLC and radio-HPLC, confirming that the immunoconjugate meets the required specifications for reliable application.

In Vitro Evaluation

In vitro evaluation provides critical validation of the fundamental integrity and functionality of the 89Zr-radiolabeled conjugate under controlled laboratory conditions. This stage focuses on confirming radiochemical purity and stability, supported by a suite of cell-based assays.

In Vivo Evaluation

To establish a comprehensive preclinical profile, in vivo pharmacokinetics and biodistribution are assessed in relevant animal models. These studies evaluate the tracer's behavior in living systems through quantitative biodistribution analysis and PET imaging. Key objectives include measuring target tissue uptake and confirming specific tumor targeting.

Applications of 89Zr-Radiolabeling

89Zr-radiolabeling is a powerful tool with broad applications across biomedical research and development. It is extensively used to develop PET tracers that facilitate non-invasive, quantitative, and longitudinal imaging of biological processes. This technology provides critical insights into the in vivo behavior of therapeutics, thereby fundamentally guiding drug development and therapeutic strategy.

Pharmaceutical and Biochemical Research

  • Pharmacokinetic and ADME Analysis
  • Immuno-PET for Biodistribution Profiling
  • Antibody-Drug Conjugate (ADC) Development & Bioanalysis
  • Target Engagement and Occupancy Studies
  • Nanomedicine and Drug Delivery System Evaluation
  • Cell Tracking (e.g., CAR-T, Stem Cells)
  • Disease Diagnosis, Staging, and Heterogeneity Assessment
  • More

Why Choose Us?

Driven by an unwavering commitment to quality, precision, and collaborative partnership, we deliver comprehensive, end-to-end radiopharmaceutical development solutions. Our client-focused approach is designed to generate robust, reliable data on time, accelerating your critical R&D programs.

Experience in 89Zr
Chemistry

Full-Service
Development

State-of-the-Art
Facilities

Application-Specific
Tailored Solutions

Alfa Cytology's specialized 89Zr-radiolabeling service provides access to expert methodology and rigorous analytical support for the successful development of your 89Zr-radiolabeled conjugates. For detailed discussions regarding your specific project requirements and to initiate a collaboration, please contact us to explore how our capabilities can contribute to your program's success.

Reference

  1. Lee, Supum et al. "[89Zr]ZrDFO-CR011 PET Correlates with Response to Glycoprotein Nonmetastatic Melanoma B-targeted Therapy in Triple-negative Breast Cancer." Molecular cancer therapeutics 21.3 (2022): 440-447.

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

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