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Receptor Occupancy Assay

Welcome to Rdcthera, a pioneering preclinical CRO dedicated to supporting the advancement of radiopharmaceutical research. We specialize in providing comprehensive receptor occupancy services, designed to enhance the development and evaluation of radiopharmaceuticals. Our expert team offers a suite of ex vivo services tailored to meet the unique needs of your research projects, ensuring precise and reliable data to drive your discoveries forward.

Understanding Receptor Occupancy

Flow cytometry is indeed a powerful tool in the development of new therapies and very likely to be one of the best tools in studies focused on monoclonal-based therapies, immunomodulators, and small molecules because of its ability to detect therapeutic binding as well as free receptors on multiple cellular targets simultaneously.
Receptor occupancy is defined as the qualitative and/or quantitative assessment of drug binding to its target receptor at a given concentration. Receptor occupancy studies in assessing the efficacy of radiopharmaceuticals targeting specific receptors could be important in understanding their potential clinical efficacy and safety.

Receptor occupancy assays.Fig.1. The three basic RO assay formats. (Liang M, et al., 2016)

Our Receptor Occupancy Services

Rdcthera offers a comprehensive receptor occupancy services, each meticulously designed to support your research objectives.

Free Receptor Expression Detection Services

Our free receptor expression detection service evaluates the quantity of receptors unbound to the therapeutic agent, which is useful for identifying the baseline status of the receptors within the biological tissues. We do this by employing either a detection antibody that competitively binds to the target epitope of the therapeutic agent or fluorescent labeling of the therapeutic agent.

Total Receptor Expression Detection Services

We provide total receptor expression detection services for the integral receptor density—both bound and unbound. Our service could allow the setting of a perfect receptor expression profile to allow one to understand receptor dynamics following the administration of radiopharmaceuticals.

Bound Receptor Expression Detection Services

Our bound-receptor expression detection services focus on providing quantification of receptors occupied by a radiopharmaceutical, which directly shows the evidence of the interaction of a drug with its target. This is really very important since it would quantify the effectiveness and selectivity of the radioligand, which informs dose studies and therapeutic strategies.

Receptor Modulation Assessment Services

Rdcthera's receptor modulation assessment quantifies the effects of radiopharmaceuticals on receptor activity and function. In doing so, we can start to elucidate mechanisms behind drug action and potential therapeutic benefit through the assessment of changes in receptor expression and activity of their signaling pathways.

Receptor Occupancy Assessment Services

Our receptor occupancy assessment services offer comprehensive evaluations of radiopharmaceutical binding across different conditions and concentrations. Utilizing state-of-the-art techniques, we provide detailed occupancy profiles that inform drug development decisions and clinical trial design.

Receptor Occupancy Assay Development Services

We offer a wide range of services related to the development of receptor occupancy assays and help create personalized assays based on your need. Our experts collaborate with you in the design and validation of assays to provide accurate, reproducible results that would enhance the effectiveness and reliability of your receptor occupancy studies.

  • Selection of a suitable antibody clone
  • Selection of the appropriate fluorescent dye based on the assay requirements
  • Rigorous reagent QC to ensure saturation of the target reagent while maximising the signal-to-noise ratio
  • Consistency of reagents between batches used for longitudinal quantitative assays.
  • Rigorous instrumental quality control to ensure longitudinal consistency of data.
  • Stability of receptors after collection and its impact on assay design.

Ready to take the next step in your radiopharmaceutical research? Contact Rdcthera today to learn more about our receptor occupancy services and how we can support your projects.

Reference

  1. Liang M, Schwickart M, Schneider AK, et al. (2016). Receptor occupancy assessment by flow cytometry as a pharmacodynamic biomarker in biopharmaceutical development. Cytometry B Clin Cytom. 90(2):117-127.
For research use only. Not intended for any clinical use.

Rdcthera RDC

Rdcthera offers efficient, customized, and professional R&D services related to radionuclide drug conjugates.

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