Radiopharmaceuticals (RPTs) are rapidly transforming oncology drug development. These agents deliver targeted therapies — with radioactive payloads. They offer a unique blend of therapeutic precision and diagnostic clarity. RPTs are attracting growing interest from biotech and biopharma companies seeking differentiated assets and accelerated innovation.

A brief history of RPTs: from discovery to clinical impact

In the late 19th century, Henri Becquerel discovered radioactivity in uranium salts, which was soon followed by Marie and Pierre Curie’s isolation of radium and polonium. These discoveries laid the foundation for medical use of radioactive substances. The treatment of thyroid cancer with radioactive iodine in the 1940s was the first use of RPTs in oncology.

The 1970s ushered in a new era for RPTs with the introduction of technetium-99m and fluorodeoxyglucose, which have since revolutionized diagnostic imaging and expanded RPT use. Regulatory frameworks evolved in parallel as the U.S. Food and Drug Administration began treating RPTs as drugs that require formal approval. More recently, the approvals of radium-223 (Xofigo^®), lutetium-177 DOTATE (Lutathera^®) and lutetium-177 vipivotide tetraxetan (Pluvicto^®) have paved the way for modern RPTs and theranostic platforms.¹

RPTs are especially attractive in oncology

RPTs are well-suited to address complex cancer biology due to several compelling advantages, including:²

• Precision targeting: Targeted therapeutic radiopharmaceuticals can be engineered to bind selectively to tumor-specific targets, delivering cytotoxic radiation directly to malignant cells while sparing healthy tissue. In addition, the bystander killing effect is important to consider. When target expression is patchy or limited to subsets of tumor cells, this involves extension of radiation damage and diffusion of reactive oxygen species to adjacent, non-targeted tumor cells. Understanding and quantifying this bystander effect is key for optimizing radionuclide choice, linker chemistry, and dosing strategy to maximize tumor control while minimizing collateral toxicity.
• Theranostic integration: RPTs uniquely combine diagnostic imaging with therapeutic delivery. This combination enables real-time monitoring of drug distribution, tumor uptake, and treatment response to facilitate adaptive trial designs and personalized dosing.
• Resistance mitigation: Unlike traditional chemotherapy or targeted therapies, RPTs have a distinct mechanism of action that may overcome some resistance mechanisms that render other treatments ineffective. However, it is important to recognize that tumors may still develop RPT resistance through shared mechanisms such as efflux pumps, enhanced DNA repair, and altered drug targets.
• Broad applicability: RPTs have so far been used for prostate cancer and neuroendocrine tumors.They are now being explored for other solid tumors, including breast, pancreatic and hepatocellular cancer, as well as melanoma.
• Streamlined patient selection: Imaging-based diagnostics allow precise patient stratification, ensuring that only those likely to benefit are enrolled in trials—enhancing trial efficiency and regulatory success rates. This is the advantage to the theranostic approach over other cancer therapies.

Growing momentum

The RPT market is experiencing robust growth, projected to expand from $7.3 billion in 2024 to $13.5 billion by 2032. This momentum is driven by rising demand for targeted cancer therapies and the increasing adoption of theranostic approaches.³

Novartis’ Pluvicto^® exemplifies this trend with a 42% year-over-year increase that generated $1.39 billion in sales in 2024. These figures validate the commercial viability of RPTs and signal a strategic shift in oncology drug development strategy.⁴ Recent acquisitions underscore the strategic importance of RPTs, and include:⁵

• Bristol Myers Squibb acquired RayzeBio for $4.1 billion
• Eli Lilly acquiring Point Biopharma for $1.4 billion
• AstraZeneca acquiring Fusion Pharmaceuticals for $2.4 billion
• Novartis acquiring Mariana Oncology for $1 billion

These deals reflect growing recognition that RPTs are a high-value modality, not only for their therapeutic potential but also for their manufacturing and supply chain advantages.

Key trends

• Isotope Innovation. Alpha-emitting isotopes offer high potency with limited radiation range. Experience with approved ¹⁷⁷Lu-based agents such as Lutathera and Pluvicto shows it is essential to address manufacturing and distribution constraints through strategic partnerships. Infrastructure investment will be critical to ensure the successful development and upscaling of alpha-emitting theranostics.⁶
• Indication expansion. Once reserved for late-stage or refractory disease, RPTs are increasingly used at earlier stages for a diverse range of cancer types. Examples being developed include:
  • ¹⁷⁷Lu-PSMA-617 for early metastatic and hormone-sensitive prostate cancer.
  • ²²³Ra-dichloride with enzalutamide as a first-line therapy for metastatic castration-resistant prostate cancer.
  • ¹³¹I as adjuvant therapy for differentiated thyroid cancer.
• Targeting advancement. Peptides, antibodies and small molecules are improving tumor specificity and reducing systemic toxicity.
• Novel combination therapy development. New combinations of targeted RPTs with immunotherapies, hormonal agents and chemotherapies are enhancing efficacy and overcoming resistance.⁷ Examples include:
  • ¹⁷⁷Lu-PSMA-617 with pembrolizumab or enzalutamide.
  • ²²³Ra-dichloride with abiraterone or docetaxel.
• Access improvement. The Centers for Medicare & Medicaid Services CY2025 HOPPS final rule introduces separate reimbursement, above $630 per day, for diagnostic RPTs. This rule is expected to increase patient access and sustainable use across care settings.⁸

Implications for clinical development leaders

For therapeutic area experts and clinical development executives, radiopharmaceuticals offer:

• Pipeline differentiation through novel mechanisms of action.
• Accelerated development timelines via theranostic approaches.
• Reduced biosimilar risk due to complex manufacturing.
• Opportunities for indications with high unmet needs in oncology.

Conclusion

RPTs are redefining the future of oncology and precision medicine. With strategic investment, infrastructure development, and clinical innovation, emerging biotech and pharma companies are well-positioned to lead in this dynamic space. Working with experienced partners can help manage the complexity of RPT clinical trials. IQVIA is a global leader in oncology clinical development who can help sponsors anticipate and manage risks appropriately.

References

1. Belge Bilgin G, Bilgin C, Burkett BJ, et al. Theranostics and artificial intelligence: new frontiers in personalized medicine. Theranostics. 2024;14(6):2367-2378.
2. National Cancer Institute Staff. Radiopharmaceuticals: radiation therapy enters the molecular age. NCI Cancer Currents Blog. U.S. Department of Health and Human Services, National Institutes of Health, National Cancer Institute. 2020. Accessed October 23, 2025. https://www.cancer.gov/news-events/cancer-currents-blog/2020/radiopharmaceuticals-cancer-radiation-therapy
3. Radiopharmaceuticals Market Size (USD 13515.27 M) by 2032 by types (diagnostic radioisotopes, therapeutic radioisotopes), applications (oncology, cardiology, other) and regional forecast to 2032. Global Growth Insights. 2024. Last updated October 6, 2025. Accessed October 2025. https://www.globalgrowthinsights.com/market-reports/radiopharmaceuticals-market-102594
4. Breakthrough in nuclear medicine as Novartis' Pluvicto sales soar to $1.39 billion in 2024. ECHEMI.com. 2025. Accessed October 23, 2025. https://www.cancer.gov/news-events/cancer-currents-blog/2020/radiopharmaceuticals-cancer-radiation-therapy
5. Dunleavy K. 2025 forecast: as companies rush to radiopharmaceuticals for oncology, what's next? Fierce Pharma. 2025. Accessed October 23, 2025. https://www.fiercepharma.com/pharma/2025-forecast-companies-rush-radiopharmaceuticals-oncology-whats-next
6. Actinium Pharmaceuticals Announces Supply Agreement with Eckert & Ziegler for Ac-225 Radioisotope to Support Comprehensive Development Activities [press release]. Actinium Pharmaceuticals. 2025. Accessed October 23, 2025. https://ir.actiniumpharma.com/press-releases/detail/496/actinium-pharmaceuticals-announces-supply-agreement-with
7. Chan TG, O'Neill E, Habjan C, Cornelissen B. Combination strategies to improve targeted radionuclide therapy. J Nucl Med. 2020;61(11):1544-1552.
8. FAQs on the Centers for Medicare & Medicaid Services (CMS) major payment policy reform for diagnostic radiopharmaceuticals under the hospital outpatient prospective payment system (HOPPS). Society of Nuclear Medical Molecular Imaging. 2024. Accessed October 23, 2025. https://snmmi.org/Web/News/Articles/FAQs-on-the-Centers-for-Medicare---Medicaid-Services--CMS--Major-Payment-Policy-Reform-for-Diagnosti.aspx