The Rising Impact of Radioligand Therapy CROs for Radioligand Development

Introduction

Radioligand therapy is an emerging treatment modality in oncology, in which radioactive materials, known as radioisotopes, deliver radiation directly to cancer cells. The radioligand therapy market, currently valued at $2.31 billion, is projected to reach a staggering $8.33 billion by 2031, driven by recognition of its potential for clinical impact and scientific innovation. Preclinical imaging has played an instrumental role in the understanding and development of radioligand therapy, giving researchers the ability to visualize and quantify how radioligands behave in living organisms prior to use in human clinical trials. With this sector set to experience significant growth, and the rising global adoption and expansion of radioligand therapy programs, it is no surprise that sponsors are increasingly relying on the expertise and specialized imaging infrastructure of clinical research organizations (CROs) to facilitate radioligand development, optimize study design, and support the translation of findings into real-world clinical practice. This article will explain radioligand therapy in more detail, considering its potential for oncology patient care and the rising impact of radioligand therapy CROs for radioligand development.

What is Radioligand Therapy?

According to the European Organisation for Research and Treatment of Cancer, a radioligand is a ‘cancer treatment that couples a therapeutic radioactive isotope with a cancer-specific cell-targeting molecule – the ligand.’ When a ligand attaches to a cancer cell, it delivers radioactive emissions directly to that cell, selectively destroying it. Radioligand therapy, therefore, uses radioligands to deliver targeted radiation directly to tumor-specific antigens or receptors, combining the targeting ability of the ligand with the therapeutic effects of the radioisotope.

This scientific discovery has been monumental due to its targeted mechanism, combining therapeutic radiation with minimal off-target effects. Three landmark clinical trials have moved radioligand therapy from an early experimental approach into an established treatment modality, resulting in the approval of both Pluvicto and Lutathera in certain oncological contexts, with the most recent update seeing the Pluvicto approval expand to use earlier in the treatment pathway.

Potential impact on oncology patient care

Through its precision and adaptability, radioligand therapy has the potential to completely transform oncology patient care, representing a transformative approach to precision oncology in which clinicians can treat tumors based not just on their location, but their molecular characteristics. Since its inception, radioligand therapy has evolved from an experimental treatment approach to a recognized and approved therapeutic intervention for a number of historically difficult-to-treat subsets of oncology, including metastatic castration-resistant prostate cancer (mCRPC) and gastroenteropancreatic neuroendocrine tumors (GEP-NETs). Such a diagnosis often leaves patients with very little in terms of treatment options, meaning radioligand therapy provides not only hope, but a tangible therapeutic pathway for patients with considerable unmet needs. The dual-action approach forms the basis of a new generation of cancer care and treatment, designed to minimize harm to healthy tissue while maximizing tumor destruction, minimizing side effects, and improving overall rates of survival.

The Critical Role of Preclinical Imaging in Radioligand Therapy Development

In anticipation of human clinical trials, which are essential for any new drug to reach real-world clinical use, regulatory authorities require an extensive body of information to confirm a thorough understanding of the benefits and risks of a potential treatment. Radioligand is a particularly complex molecule, or ligand, making this anticipatory information all the more important to aid understanding and application. There are a number of very key and specific ways in which preclinical imaging has contributed to the development and understanding of radioligand therapy, enabling insight and evaluation of biodistribution, pharmacokinetics, and radiation dosimetry, prior to its use in human clinical trials.

• Biodistribution – Biodistribution is ‘the reversible transfer of chemicals or drugs from one location to another in a biological system’. Within radioligand therapy, this means predicting where in the body the radioligand will travel, how specifically it targets tumor tissue, and what side effects, if any, this has on healthy tissue. Information on the biodistribution of cell therapy products is essential to predict and assess the viability and toxicity of potential treatments. Without preclinical imaging, it would be extremely difficult to gain this understanding, and the use of imaging modalities such as positron emission tomography (PET), single photon emission computed tomography (SPECT), and computed tomography (CT) have allowed researchers to monitor radioligand localization and retention over time in live animal models.
• Dosimetry – Dosimetry is ‘the process of relating the administered amount of radioactivity to the absorbed radiation dose in tumors, organs, or the whole body.’ Dosimetry investigations are among the preclinical safety data recommended by many regulatory authorities, ensuring not only patient safety, but accurate dose optimization and therapeutic efficacy. Dosimetry allows researchers to quantify the right balance of radiation to maximize therapeutic effect while preserving healthy tissue. Key preclinical modalities used to evaluate and estimate radiation dose include SPECT, PET, and CT.
• Pharmacokinetics – Pharmacokinetics is ‘the study of how the body interacts with administered substances for the entire duration of exposure’, namely its absorption, distribution, metabolization, and excretion. Non-invasive imaging modalities such as PET and SPECT are essential tools for the evaluation of pharmacokinetics in vivo, capturing real-time, dynamic images of radioligand distribution and clearance in experimental animal models.

The Rising Impact of Radioligand Therapy CROs

Radioligand therapy CROs are instrumental in bridging the gap between experimental treatment analysis and real-world therapeutic intervention. With expertise in radiochemistry, nuclear medicine, and oncology research models, they are accelerating the development of radioligand-based treatments around the world.

Radioligand therapy CROs have specialized infrastructure, including state-of-the-art imaging suites and isotope handling facilities, which support both the data collection and interpretation of results within radioligand therapy trials. Supporting sponsors through custom study design, regulatory guidance, and tailored protocols, including selection of radionuclide, tumor models, and imaging schedules, radioligand therapy CROs are an asset to radioligand therapy clinical trials. Partnering with a radioligand therapy CRO is no longer optional; it’s a strategic decision that can bolster clinical trial success.

One radioligand therapy CRO with experience across oncology, nuclear imaging, and radioligand therapies is Perceptive Discovery, having over 15 years of experience and supporting over 650 new drug approvals, making them an asset to your radioligand therapy trial.

Accelerate your R&D timeline, improve the quality of your data, and learn more about Perceptive Discovery Services today. Contact a Discovery solutions specialist.

Resources

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9. European Journal of Nuclear Medicine and Molecular Imaging. EANM guidance document: dosimetry for first-in-human studies and early phase clinical trials. https://pmc.ncbi.nlm.nih.gov/articles/PMC10957710/